标签归档：egfr

EGFR-IN-44

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

EGFR-IN-44 

EGFR-IN-44 (Compound 6a) 是一种有效的、具有口服活性的 EGFR tyrosine kinase 抑制剂，其 IC50 值为 4.11 nM。EGFR-IN-44 诱导细胞凋亡 (apoptosis)，口服生物利用度为33.57%。EGFR-IN-44 可以用于非小细胞肺癌的研究。

EGFR-IN-44

EGFR-IN-44 Chemical Structure

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生物活性

EGFR-IN-44 (Compound 6a) is a potent, orally active EGFR tyrosine kinase inhibitor with an IC50 of 4.11 nM. EGFR-IN-44 induces cell apoptosis and shows an oral bioavailability value of 33.57%. EGFR-IN-44 can be studied for non-small-cell lung cancers[1].

IC50 & Target

IC50: 0.26 nM (EGFR T790M/L858R), 1.33 nM (EGFR L858R), 4.11 nM (EGFR)[1]
体外研究
(In Vitro)

EGFR-IN-44 (Compound 6a) (0-10 µM, 72 h) shows anti-proliferative activities against tumor cell lines[1].
EGFR-IN-44 binds to the ATP binding site of EGFR[1].
EGFR-IN-44 (0-10 nM, 48 h) induces H1975 cell apoptosis via the mitochondrial pathway, arrests cell cycle in G0/G1 phase, and suppresses cell migration[1].
EGFR-IN-44 (0-10 nM, 48 and 72h) shows hypotoxicity against normal cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: H1975 (EGFRT790M/L858R), PC9 (EGFRdel19), and H292 (EGFRWT)
Concentration: 0-10 µM
Incubation Time: 72 h
Result: Showed anti-proliferative activities with IC50 values of 0.0022 ± 0.001, 0.0048 ± 0.001, and 4.499 ± 0.057 µM against H1975, PC9, and H292 cells, respectively.

Apoptosis Analysis[1]

Cell Line: H1975
Concentration: 1, 5, and 10 nM
Incubation Time: 48 h
Result: Effectively induced cell apoptosis in a dose-dependent manner. Resulted in 33.7%, 52.4%, and 56.2% apoptosis at 1, 5, and 10 µM, respectively, compared to 5.81% apoptosis in the control group.

Western Blot Analysis[1]

Cell Line: H1975
Concentration: 5, 10, and 25 nM
Incubation Time: 48 h and 72 h
Result: Dose-dependently upregulated the expression levels of the proapoptotic proteins Bad and Bax and downregulated the expression level of the antiapoptotic protein Bcl-2. Sufficiently reduced the phosphorylation of EGFR and AKT.

Cell Cycle Analysis[1]

Cell Line: H1975
Concentration: 5 nM
Incubation Time: 0, 12, 24, or 48 h
Result: Exhibited a significant increase in the G0/G1 cell population and a dramatic decrease in G2/M phase.

Cell Cytotoxicity Assay[1]

Cell Line: LO2, HK2, HLF, and 293A
Concentration: 0.1, 1, 5, and 10 µM
Incubation Time: 48 h and 72 h
Result: Showed hypotoxicity with IC50 values of 7.247, 4.586, 3.787, and 2.925 µM against LO2, HK2, HLF, and 293A cells, respectively. The cell morphology was changed compared to the control.

体内研究
(In Vivo)

EGFR-IN-44 (Compound 6a) (25 mg/kg; i.g.; daily, 7days) shows strong antitumor activity without obvious toxicity[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male BALB/c nude mice (5 weeks old, 18 – 20 g), H1975 xenograft model[1]
Dosage: 25 mg/kg
Administration: Intragastric administration, daily, 7 days
Result: Showed strong tumor inhibition (TGI = 90.24%) without obvious toxicity.
Animal Model: Male Sprague–Dawley (SD) rats[1]
Dosage: 1 mg/kg and 5 mg/kg
Administration: Intravenous injection and oral administration (Pharmacokinetic Analysis)
Result: In Vivo PK parameters of EGFR-IN-44 [1]

Parameters
Dose(mg/kg)		 EGFR-IN-44
5 (po)		 1 (iv)
t1/2 (h) 8.60 ± 1.8 1.42 ± 0.1
Tmax (h) 4.00 ± 0.002 /
Cmax (ng/mL) 80.40 ± 2.7 /
Vz F_pred (L/kg) 220.80 ± 41.2 6.83 ± 08
AUC0-t (H.ng/mL) 490.41 ± 29.9 291.91 ± 38.2
AUC0-∞ (H.ng/mL) 491.02 ± 44.2 295.76 ± 38.8
MRT0-last (h) 7.93 ± 0.8 1.35 ± 01
CL (mL/h/kg) 17.79 ± 3.9 3.12 ± 0.4
F(%) 33.57 ± 5.9 /


F = (AUC0-inf-PO × DOSEIV)/(AUC0-inf-IV × DOSE PO)*100%.

分子量

537.08

Formula

C27H29ClN6O2S
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Baijiao An, et al. Novel third-generation pyrimidines-based EGFR tyrosine kinase inhibitors targeting EGFR T790M mutation in advanced non-small cell lung cancer. Bioorg Chem. 2022 May;122:105743.

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EGFR-IN-49

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

EGFR-IN-49 

EGFR-IN-49 是一种有效的选择性 EGFR 抑制剂，对 EGFRT790M 和 EGFRT790M/L858R 的IC50 值分别为 65.0 nM 和 13.6 nM。EGFR-IN-49 以剂量依赖性方式诱导细胞凋亡 (apoptosis)。

EGFR-IN-49

EGFR-IN-49 Chemical Structure

CAS No. : 2459932-81-9

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生物活性

EGFR-IN-49 is a potent and selective EGFR inhibitor with IC50s of 65.0 nM and 13.6 nM for EGFRT790M and EGFRT790M/L858R, respectively. EGFR-IN-49 induces cell apoptosis in a dose-dependent manner[1].

IC50 & Target[1]

EGFRT790M

65.0 nM (IC50)

EGFRL858R/T790M

13.6 nM (IC50)

体外研究
(In Vitro)

EGFR-IN-49 (compound 13a) (1, 10 µM) shows inhibition activity for H1975 cells with an IC50 of 699.2 nM[1].
EGFR-IN-49 (1 µM) shows an strong inhibitory activity to EGFRT790M, EGFRT790M/L858R, EGFRWT with IC50s of 65.0, 13.6, >1000 nM, respectively[1].
EGFR-IN-49 (0.2, 4, 8 µM; 48 h) induces cell apoptosis in a dose-dependent manner in A431 cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: A549, A431, Hela, MCF7, LO2 cells
Concentration: 0-50 µM
Incubation Time:
Result: Showed excellent anti-proliferative activities with IC50s of 4.34, 3.79, 6.39, 18.99, >50 µM for A549, A431, Hela, MCF7, LO2 cells, respectively.

Apoptosis Analysis[1]

Cell Line: A431 cells
Concentration: 0.2, 4, 8 µM
Incubation Time: 48 h
Result: Induced cell apoptosis in a low concentration (0.33 µM) and exhibited higher percent of 16.41% % in the stage of late apoptotic at concentration of 4 µM.

分子量

413.45

Formula

C22H15N5O2S
CAS 号

2459932-81-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Xiao Z, et al. Design, synthesis and antitumor activity of novel thiophene-pyrimidine derivatives as EGFR inhibitors overcoming T790M and L858R/T790M mutations. Eur J Med Chem. 2020 Oct 1;203:112511.

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EGFR-IN-2

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

EGFR-IN-2 

EGFR-IN-2 是一种非共价的，不可逆的，突变选择性的二代 EGFR 抑制剂。

EGFR-IN-2

EGFR-IN-2 Chemical Structure

CAS No. : 1643497-70-4

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生物活性

EGFR-IN-2 is a a noncovalent, irreversible, mutant-selective second generation EGFR inhibitor.

IC50 & Target

EGFR[1]
体外研究
(In Vitro)

EGFR-IN-2 (Compound 21) inhibits EGFR autophosphorylation with IC50s of 0.027 μM, 0.009 μM ,0.033 μM , and 0.218 μM in double mutant TMLR cell line H1975, double mutant TMdel cell line PC9-ER, activating mutant del cell line PC9, and wild type cell line H292. In addition, EGFR-IN-2 demonstrats strong antiproliferative effect on the T790M mutant carrying H1975 cell line (IC50=0.361 μM) and the single activating mutant PC9 cell line (IC50=0.151 μM). Furthermore, EGFR-IN-2 also shows good selectivity against other kinases when evaluated in a 225-kinase panel (12/225 kinases inhibited at >70% when tested at 0.1 μM, 61-fold over the TMLR Ki and 63-fold over the TMdel Ki)[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

To examine its inhibitory effect on pEGFR levels in vivo, EGFR-IN-2 (Compound 21) is studied in a mouse H1975 (TMLR) xenograft model. After a single oral dose of 21 at 50 mg/kg, free plasma concentrations of EGFR-IN-2 at or exceeding the in vitro p-EGFR IC50 of 0.027 μM are sustained over 8 h. When administered at 100 mg/kg, the coverage of p-EGFR IC50 is extended to the last measured time point of 16 h postdose. Corresponding knockdown of p-EGFR and the downstream effectors pERK1/2 and AKT levels are observed at those time points, suggesting target engagement in vivo. In mouse, after intravenous and oral administration, the plasma clearance of EGFR-IN-2 is determined to be 104 mL/kg per min with a bioavailability of 19%. In dogs, the plasma clearance is 13 mL/kg per min with an oral bioavailability of 30%[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

551.66

Formula

C26H33N9O3S
CAS 号

1643497-70-4
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Chan BK, et al. Discovery of a Noncovalent, Mutant-Selective Epidermal Growth Factor Receptor Inhibitor. J Med Chem. 2016 Oct 13;59(19):9080-9093.
Animal Administration
[1]

Mice[1]
Eight week old female SCID beige mice are inoculated subcutaneously with 5×106 NCI-H1975 cells. When tumors reach a mean volume of 300 to 500 mm3, mice with similarly sized tumors are randomized into treatment groups. EGFR-IN-2 at 50 mg/kg or 100 mg/kg is administered orally as a single dose. Tumor and plasma samples are collected at 2, 8 or 16 h post dose[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Chan BK, et al. Discovery of a Noncovalent, Mutant-Selective Epidermal Growth Factor Receptor Inhibitor. J Med Chem. 2016 Oct 13;59(19):9080-9093.

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EGFR-IN-5

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

EGFR-IN-5 

EGFR-IN-5是 EGFR 的抑制剂，对EGFR，EGFRL858R，EGFRL858R/T790M和EGFRL858R/T790M/C797S的IC50分别为10.4，1.1，34，7.2 nM。

EGFR-IN-5

EGFR-IN-5 Chemical Structure

CAS No. : 2225887-26-1

规格 价格 是否有货
10 mM * 1 mL in DMSO ￥4020 询问价格 & 货期
5 mg ￥3200 询问价格 & 货期
10 mg ￥5100 询问价格 & 货期
25 mg ￥9800 询问价格 & 货期

* Please select Quantity before adding items.

生物活性

EGFR-IN-5 is a EGFR inhibitor with IC50s of 10.4, 1.1, 34, 7.2 nM for EGFR, EGFRL858R, EGFRL858R/T790M, and EGFRL858R/T790M/C797S, respectively.

IC50 & Target[1]

EGFR

10.4 nM (IC50)

EGFRL858R

1.1 nM (IC50)

EGFRL858R/T790M

34 nM (IC50)

EGFRL858R/T790M/C797S

7.2 nM (IC50)

分子量

571.69

Formula

C31H38FN9O
CAS 号

2225887-26-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
溶解性数据
In Vitro: 

DMSO : 125 mg/mL (218.65 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7492 mL 8.7460 mL 17.4920 mL
5 mM 0.3498 mL 1.7492 mL 3.4984 mL
10 mM 0.1749 mL 0.8746 mL 1.7492 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.64 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.64 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Zhang H, et al. Discovery of 2,4,6-trisubstitued pyrido[3,4-d]pyrimidine derivatives as new EGFR-TKIs. Eur J Med Chem. 2018 Mar 25;148:221-237.

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EGFR-IN-8

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

EGFR-IN-8  纯度: 98.31%

EGFR-IN-8 是 EGFR 和 c-Met 双重抑制剂，化合物 48。EGFR-IN-8 有望成为进一步开发靶向 EGFR TKI 抗性 NSCLC 药物的靶点。

EGFR-IN-8

EGFR-IN-8 Chemical Structure

CAS No. : 2407957-87-1

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥5100 In-stock
5 mg ￥3500 In-stock
10 mg ￥5800 In-stock
50 mg ￥16500 In-stock
100 mg ￥25500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

EGFR-IN-8 相关产品

•相关化合物库:

  • Covalent Screening Library Plus
  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • JAK/STAT Compound Library
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Covalent Screening Library
  • Differentiation Inducing Compound Library
  • Anti-Hepatitis C Virus Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

EGFR-IN-8 is a dual EGFR and c-Met inhibitor, compound 48. EGFR-IN-8 can be a promising candidate for further development to target EGFR TKI-resistant NSCLC[1].

IC50 & Target

EGFR; c-Met[1]
体外研究
(In Vitro)

EGFR-IN-8 (0-20 μM; 24-72 hours) exhibits a time- and dose-dependent inhibitory effect on the viability of A549, PC9, H1975, CL68, and CL97 cells at different time intervals, with IC50 values ranging from 0.3 to 0.6 μM and 0.2-0.5 μM after 48 and 72 h of treatment respectively[1].
EGFR-IN-8 (0-0.6 μM; 48 hours) suppresses the expression of EGFR and c-Met in these five cell lines irrespective of their mutational status[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: A549, PC9, H1975, CL68, and CL97 cells
Concentration: 0-20 μM
Incubation Time: 24 hours, 48 hours, 72 hours
Result: Showed inhibitory effects on different cells.

Western Blot Analysis[1]

Cell Line: A549, PC9, H1975, CL68, and CL97 cells
Concentration: 0-0.6 μM
Incubation Time: 48 hours
Result: Decreased EGFR and c-Met expression.

体内研究
(In Vivo)

EGFR-IN-8 (oral gavage; 50 and 150 mg/kg; once daily; 20 days) exhibits a dose-dependent suppression (29% and 60%, respectively) of H1975 xenograft tumor growth at 50 and 150 mg/kg[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Nude mice H1975 xenograft tumor model[1]
Dosage: 50 and 150 mg/kg
Administration: Oral gavage; 50 and 150 mg/kg; once daily; 20 days
Result: Inhibited H1975 xenograft tumor growth.

分子量

662.02

Formula

C32H23ClF3N7O4
CAS 号

2407957-87-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 8.33 mg/mL (12.58 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.5105 mL 7.5526 mL 15.1053 mL
5 mM 0.3021 mL 1.5105 mL 3.0211 mL
10 mM 0.1511 mL 0.7553 mL 1.5105 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Dokla EME, et al. 1,2,4-Oxadiazole derivatives targeting EGFR and c-Met degradation in TKI resistant NSCLC. Eur J Med Chem. 2019 Aug 9;182:111607.

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EGFR-IN-11

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

EGFR-IN-11  纯度: 99.81%

EGFR-IN-11 是第四代 EGFR-酪氨酸激酶抑制剂 (EGFR-TKI)，对三重突变的 EGFRL858R/T790M/C797S 的 IC50 为 18 nM。EGFR-IN-11 显著抑制 EGFR 磷酸化，诱导细胞凋亡，将细胞周期阻滞在 G0/G1处。

EGFR-IN-11

EGFR-IN-11 Chemical Structure

CAS No. : 2463200-44-2

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥5050 In-stock
5 mg ￥4000 In-stock
10 mg ￥6800 In-stock
25 mg ￥13500 In-stock
50 mg ￥22000 In-stock
100 mg ￥34000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

EGFR-IN-11 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Immunology/Inflammation Compound Library
  • JAK/STAT Compound Library
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Differentiation Inducing Compound Library
  • Anti-Hepatitis C Virus Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

EGFR-IN-11 is a fourth-generation EGFR-tyrosine kinase inhibitor (EGFR-TKI) with an IC50 of 18 nM for triple mutant EGFRL858R/T790M/C797S. EGFR-IN-11 significantly suppresses the EGFR phosphorylation, induce the apoptosis, and arrest cell cycle at G0/G1[1].

IC50 & Target[1]

EGFRL858R/T790M/C797S

18 nM (IC50)

体外研究
(In Vitro)

EGFR-IN-11 (Compound D9; 0.0001-10 µM; 72 hours) shows significantly potent anti-proliferation against HCC827 and H1975 cell lines with IC50s of 0.88 nM and 0.20 µM, respectively[1].
EGFR-IN-11 (0.01-1.00 µM for HCC827 cells; 0.1-10.00 µM for H1975 and A549 cells; 8 hours) suppresses EGFR phosphorylation in a concentration-dependent manner in the HCC827, H1975 and A549 cell line[1].
EGFR-IN-11 (1 µM; 24 h) potently induces the apoptosis of HCC827 cells.[1]
EGFR-IN-11 (1 µM; 24 h) induces cell cycle arrests in HCC827 cell[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: Human lung cancer cell lines HCC827 (EGFRDel E746-A750), H1975 (EGFRL858R/T790M) and A549 (EGFRWT); epidermoid carcinoma cell line A431 (EGFRWT)
Concentration: 0.0001, 0.0003, 0.001, 0.003, 0.01, 0.1, 1, 10 µM
Incubation Time: 72 hours
Result: Inhibited HCC827 H1975 A549 cells proliferation with IC50s of 0.88±0.09 nM, 0.20±0.01 μM, 2.91±0.61 μM, and >10 μM, respectively.

Western Blot Analysis[1]

Cell Line: HCC827, H1975 and A549 cells
Concentration: 1.00, 0.10 and 0.01 µM for HCC827 cells; 10.00, 1.00 and 0.10 µM for H1975 and A549 cells
Incubation Time: 8 hours
Result: Suppressed EGFR phosphorylation in a concentration-dependent manner. EGFR phosphorylation in the HCC827 cell line was more remarkably suppressed than in the H1975 and A549 cell lines.

Apoptosis Analysis[1]

Cell Line: HCC827 cells
Concentration: 1 µM
Incubation Time: 24 hours
Result: The percentages of apoptotic cells is 56.91%.

Cell Cycle Analysis[1]

Cell Line: HCC827 cells
Concentration: 1 µM
Incubation Time: 24 hours
Result: The number of HCC827 cells in G0/G1 phase was increased significantly.

分子量

573.71

Formula

C29H35N9O2S
CAS 号

2463200-44-2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 125 mg/mL (217.88 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7430 mL 8.7152 mL 17.4304 mL
5 mM 0.3486 mL 1.7430 mL 3.4861 mL
10 mM 0.1743 mL 0.8715 mL 1.7430 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.63 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.63 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.63 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.63 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Lei H, et al. Discovery of novel 9-heterocyclyl substituted 9H-purines as L858R/T790M/C797S mutant EGFR tyrosine kinase inhibitors. Eur J Med Chem. 2019 Nov 16:111888.

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Mutated EGFR-IN-3

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Mutated EGFR-IN-3 

Mutated EGFR-IN-3，化合物 3，是 EGFR(L858R/T790M) 和 EGFR(L858R/T790M/C797S) 突变体的有效，具有 ATP 竞争性和高选择性的变构二苯并二氮杂酮抑制剂，抑制 EGFR(L858R/T790M) 和 EGFR(L858R/T790M/C797S) 的 IC50 值分别为 12 nM 和 13 nM。

Mutated EGFR-IN-3

Mutated EGFR-IN-3 Chemical Structure

CAS No. : 2375107-27-8

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

Mutated EGFR-IN-3 (compound 3) is a potent, ATP-competitive and highly selective allosteric dibenzodiazepinone inhibitor of the EGFR(L858R/T790M) and EGFR(L858R/T790M/C797S) mutants with IC50 values of 12 nM and 13 nM, respectively[1].

IC50 & Target[1]

EGFRL858R/T790M

12 nM (IC50)

EGFRC797S

13 nM (IC50)

体外研究
(In Vitro)

Mutated EGFR-IN-3 inhibits EGFR through an allosteric mechanism, biochemical IC50 values at varying ATP concentrations: 10 µM, 10.0 µM, 100.0 µM, 1000.0 µM are 15 nM, 8.3nM,11.0 nM and 8.3 nM, respectively for L858R/T790M cells[1].
Mutated EGFR-IN-3 exhibits antiproliferative activities of a panel of EGFR allosteric inhibitors are 7.0 µM, 3.3 µM, 3.8 µM, 4.0 µM and 4.5 µM for parental, WT, L858R, L858R/T790M and L858R/T790M/C797S, respectively in the absence of Cetuximab in Ba/F3 cells[1].
Mutated EGFR-IN-3 exhibits antiproliferative activities of a panel of EGFR allosteric inhibitors are 3.2 µM, 2.7 µM, 0.36 µM and 0.20 µM for WT,L858R, L858R/T790M and L858R/T790M/C797S, respectively in the presence of Cetuximab in Ba/F3 cells[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

508.59

Formula

C31H29FN4O2
CAS 号

2375107-27-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. De Clercq DJH，et al. Discovery and Optimization of Dibenzodiazepinones as Allosteric Mutant-Selective EGFR Inhibitors.ACS Med Chem Lett. 2019 Oct 22;10(11):1549-1553.

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EGFR-IN-1

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EGFR-IN-1 

EGFR-IN-1 (compound 24) 是一种具有口服活性的，不可逆的突变体选择性 L858R/T790M EGFR 抑制剂。与野生型 EGFR 相比，EGFR-IN-1 对 Gefitinib 耐药的 EGFR L858R/T790M 有 100 倍的抑制作用。EGFR-IN-1 对 H1975 细胞和 HCC827 细胞具有较强的抗增殖活性。具有抗肿瘤活性。

EGFR-IN-1

EGFR-IN-1 Chemical Structure

CAS No. : 1625677-63-5

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

EGFR-IN-1 的其他形式现货产品:

EGFR-IN-1 TFA

生物活性

EGFR-IN-1 (compound 24) is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity[1].

IC50 & Target[1]

EGFRL858R/T790M

 

体外研究
(In Vitro)

EGFR-IN-1 (10 μM; 72 hours) displays strong antiproliferative activity against the H1975 and HCC827 cells with IC50s of 4 and 28 nM, respectively[1].
EGFR-IN-1 inhibits p-EGFR in H1975 and HCC827 cells with IC50s of 4 and 9 nM, respectively. EGFR-IN-1 highly selective against a panel of 100 kinases[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: NSCLC cell lines H1975 (T790M/L858R), HCC827 (∆746-750)
Concentration: 10 μM
Incubation Time: 72 hours
Result: Inhibited H1975 nonsmall cell lung cancer cell line and the first line mutant HCC827 cell line with IC50s of 4 and 28 nM, respectively.

体内研究
(In Vivo)

EGFR-IN-1 (30 mg/kg; p.o.; daily for 2 weeks) displays significant tumor growth inhibition with no observed loss in body weight[1].
EGFR-IN-1 evaluates in a time course PD experiment upon oral dosing at 30 mg/kg. EGFR-IN-1 shows a >50% inhibition of phosphorylation of EGFR for >12 h. EGFR-IN-1 reaches maximal concentration of 0.10 μM at 2 h and systemic exposure (AUC0-inf.) is 0.33 μM. h[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female athymic nude mice (H1975 Tumor Xenograft)[1]
Dosage: 30 mg/kg
Administration: p.o.; daily for 2 weeks
Result: Led to significant tumor growth inhibition with no observed loss in body weight.

分子量

514.58

Formula

C28H30N6O4
CAS 号

1625677-63-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Wurz RP, et al. Oxopyrido[2,3-d]pyrimidines as Covalent L858R/T790M Mutant Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors. ACS Med Chem Lett. 2015 Jul 27;6(9):987-92.

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Mutant EGFR inhibitor

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Mutant EGFR inhibitor  纯度: 99.10%

Mutant EGFR inhibitor是有效，选择性的 EGFR 突变体抑制剂，来自专利WO 2013014448 A1；可抑制EGFRL858R，EGFRExon 19 deletion，EGFRT790M。

Mutant EGFR inhibitor

Mutant EGFR inhibitor Chemical Structure

CAS No. : 1421373-62-7

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥2170 In-stock
5 mg ￥1900 In-stock
10 mg ￥2800 In-stock
50 mg ￥8500 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

Mutant EGFR inhibitor 相关产品

•相关化合物库:

  • Covalent Screening Library Plus
  • Bioactive Compound Library Plus
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  • Angiogenesis Related Compound Library
  • Targeted Diversity Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

Mutant EGFR inhibitor is a potent and selective mutant EGFR inhibitor extracted from patent WO 2013014448 A1; inhibits EGFRL858R, EGFRExon 19 deletion and EGFRT790M.

IC50 & Target

EGFRL858R

 

EGFRExon 19 deletion

 

EGFRT790M

 

分子量

520.03

Formula

C27H30ClN7O2
CAS 号

1421373-62-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 50 mg/mL (96.15 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9230 mL 9.6148 mL 19.2297 mL
5 mM 0.3846 mL 1.9230 mL 3.8459 mL
10 mM 0.1923 mL 0.9615 mL 1.9230 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.81 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.81 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.81 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.81 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. WO 2013014448 A1

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Osimertinib(Synonyms: 奥希替尼; AZD-9291; Mereletinib)

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Osimertinib (Synonyms: 奥希替尼; AZD-9291; Mereletinib) 纯度: 99.90%

Osimtinib (AZD9291) 是一种共价结合、具有口服活性、不可逆和突变选择性的 EGFR 抑制剂，其有效抑制 L858R (IC50=12 nM) 和 L858R/T790M (IC50=1 nM) EGFR。Osimtinib 解决了肺癌 T790M 突变介导的 EGFR 抑制剂耐药。

Osimertinib(Synonyms: 奥希替尼; AZD-9291; Mereletinib)

Osimertinib Chemical Structure

CAS No. : 1421373-65-0

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥715 In-stock
5 mg ￥650 In-stock
10 mg ￥980 In-stock
50 mg ￥1700 In-stock
100 mg ￥2400 In-stock
200 mg ￥3850 In-stock
500 mg   询价  
1 g   询价  

* Please select Quantity before adding items.

Osimertinib 相关产品

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  • FDA Approved & Pharmacopeial Drug Library
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  • Targeted Therapy Drug Library
  • Angiogenesis Related Compound Library
  • Targeted Diversity Library
  • Anti-Liver Cancer Compound Library
  • Rare Diseases Drug Library
  • Anti-Colorectal Cancer Compound Library

生物活性

Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer[1].

IC50 & Target[1]

EGFRL858R

12 nM (IC50, Enzyme assays)

EGFRL858R/T790M

1 nM (IC50, Enzyme assays)

体外研究
(In Vitro)

Osimertinib (AZD9291) (0-10 μM; 72 hours) dramatically inhibits cell proliferation with IC50s of 41, 26, 41, and 31 nM, respectively[2].
Osimertinib (0-10 μM; 72 hours) inhibits cell proliferation (Ba/F3 cells harboring a T790M mutation, exon 19del+T790M, or L858R+T790M) with IC50s of 6, 7, and 74 nM, respectively[2].
Osimertinib (0-10 μM; 72 hours) inhibits Ba/F3 cells harboring EGFR exon 20 insertion mutations (IC50 ranging from 16 to 701 nM for A763_Y764insFQEA (FQEA), Y764_V765insHH (HH), A767_V769dupASV (ASV), and D770_N771insNPG (NPG) cells)[2].
Osimertinib shows high levels of phenotype potency in both sensitizing-mutant (mean IC50 of 8 nM in PC-9) and T790M (mean IC50s of 11 and 40 nM in H1975 and PC-9VanR respectively) EGFR cell lines. Osimertinib has much less activity towards wild-type EGFR (mean IC50s of 650 and 461 nM in Calu3 and H2073 respectively)[1].
Osimertinib (0.1 μM; 48 hours) induces apoptosis in Ba/F3 cells (apoptosis rates of 40.9% and 90% in EGFR exon 19del+T790M, EGFR L858R+T790M respectively) [2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[2]

Cell Line: Ba/F3 cells (harboring a T790M mutation, exon 19del+T790M, or L858R+T790M)
Concentration: 0.0001, 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time: 72 hours
Result: Inhibited cell proliferation (IC50s=6, 7, 74 nM, respectively)

Cell Proliferation Assay[2]

Cell Line: PC-9, H3255, PC-9ER, and H1975 cells
Concentration: 0.0001, 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time: 72 hours
Result: Dramatically inhibited cell proliferation (IC50s=41, 26, 41, 31 nM, respectively)

Cell Proliferation Assay[2]

Cell Line: Ba/F3 cells (harboring EGFR exon 20 insertion mutations: FQEA, HH, ASV, NPG )
Concentration: 0.0001, 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time: 72 hours
Result: Inhibited cell proliferation (IC50s=16, 701, 230, 38 nM, respectively)

Apoptosis Analysis[2]

Cell Line: Ba/F3 cells (harboring EGFR exon 19del+T790M or EGFR L858R+T790M)
Concentration: 0.1 μM
Incubation Time: 48 hours
Result: Induced apoptosis with the rates of 40.9% and 90% in EGFR T790M positive mutations cells, respectively.

体内研究
(In Vivo)

Osimertinib (0.1-25 mg/kg; p.o.; daily for 14 days) induces significant dose-dependent regression in both PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models[1]
Dosage: 0.1-10 mg/kg (PC-9 xenograft models); 0.5- 25 mg/kg (H1975 xenograft models)
Administration: p.o.; daily for 14 days
Result: Induced significant dose-dependent regression in both PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models.

Clinical Trial

分子量

499.61

Formula

C28H33N7O2
CAS 号

1421373-65-0
中文名称

奥斯替尼；奥希替尼
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 125 mg/mL (250.20 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0016 mL 10.0078 mL 20.0156 mL
5 mM 0.4003 mL 2.0016 mL 4.0031 mL
10 mM 0.2002 mL 1.0008 mL 2.0016 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 0.5%HPMC  1%Tween80

    Solubility: 5 mg/mL (10.01 mM); Suspened solution; Need ultrasonic and warming and heat to 60°C

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.00 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.00 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

  • 3.

    请依序添加每种溶剂： 5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: ≥ 2.5 mg/mL (5.00 mM); Clear solution

  • 4.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.16 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.16 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Cross DA, et al. AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Cancer Discov. 2014 Sep;4(9):1046-61.

    [2]. Hirano T, et al. Pharmacological and Structural Characterizations of Naquotinib, a Novel Third-Generation EGFR Tyrosine Kinase Inhibitor, in EGFR-Mutated Non-Small Cell Lung Cancer. Mol Cancer Ther. 2018 Apr;17(4):740-750.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

EGFR-IN-7

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

EGFR-IN-7  纯度: 99.76%

EGFR-IN-7 (compound 34) 是一种有效选择性的 EGFR 激酶抑制剂，对 EGFR (WT) 和 EGFR (mutant C797S/T790M/L858R) 的 IC50 值分别为 7.92 nM 和 0.218 nM，具有抗肿瘤活性，详细信息请参考专利 WO2019015655A1。

EGFR-IN-7

EGFR-IN-7 Chemical Structure

CAS No. : 2267329-76-8

规格 价格 是否有货 数量
5 mg ￥2950 In-stock
10 mg ￥4950 In-stock
50 mg ￥13000 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

EGFR-IN-7 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus

生物活性

EGFR-IN-7 (compound 34) is a selective and potent EGFR kinase inhibitor extracted from patent WO2019015655A1, has IC50s of 7.92 nM and 0.218 nM for EGFR (WT) and EGFR (mutant C797S/T790M/L858R) respectively, and shows anti-tumor activity[1].

IC50 & Target[1]

EGFR (WT)

7.92 nM (IC50)

EGFR (C797S/T790M/L858R)

0.218 nM (IC50)

分子量

694.60

Formula

C32H41BrN9O2P
CAS 号

2267329-76-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 5 mg/mL (7.20 mM; ultrasonic and warming and adjust pH to 5 with 0.1 M HCL and heat to 60°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.4397 mL 7.1984 mL 14.3968 mL
5 mM 0.2879 mL 1.4397 mL 2.8794 mL
10 mM — — —

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.25 mg/mL (1.80 mM); Clear solution

    此方案可获得 ≥ 1.25 mg/mL (1.80 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1.25 mg/mL (1.80 mM); Clear solution

    此方案可获得 ≥ 1.25 mg/mL (1.80 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 1.25 mg/mL (1.80 mM); Clear solution

    此方案可获得 ≥ 1.25 mg/mL (1.80 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Aryl-phosphorus-oxygen compound as egfr kinase inhibitor.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

EAI045

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

EAI045  纯度: 98.90%

EAI045是突变体 EGFR 的第四代变构抑制剂，在10 μM ATP时抑制EGFR，EGFRL858R，EGFRT790M 和 EGFRL858R/T790M 的IC50 值分别为1.9，0.019，0.19 和 0.002 μM。

EAI045

EAI045 Chemical Structure

CAS No. : 1942114-09-1

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥1650 In-stock
50 mg ￥1500 In-stock
100 mg ￥2500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

EAI045 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • JAK/STAT Compound Library
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Differentiation Inducing Compound Library
  • Anti-Hepatitis C Virus Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Targeted Diversity Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

EAI045 is an allosteric and the fourth-generation inhibitor of mutant EGFR with IC50s of 1.9, 0.019, 0.19 and 0.002 μM for EGFR, EGFRL858R, EGFRT790M and EGFRL858R/T790M at 10 μM ATP, respectively.

IC50 & Target

EGFR

1.9 μM (IC50)

EGFRL858R

0.019 μM (IC50)

EGFRT790M

0.19 μM (IC50)

EGFRL858R/T790M

0.002 μM (IC50)

体外研究
(In Vitro)

EAI045 potently inhibits EGFR Y1173 phosphorylation in H1975 cells (EC50=2 nM), but not in HaCaT cells. EAI045 is an inhibitor of the L858R/T790M mutant with 1000-fold selectivity versus wild type EGFR at 1 mM ATP. Profiling of EAI045 against a panel of 250 protein kinases reveals exquisite selectivity; no other kinases are inhibited by more than 20% at 1 μM EAI045[1]. EAI045 has high potency and selectivity for L858R/T790M mutation. In L858R/T790M-mutant NSCLC cell line H1975 cells, EAI045 decreases but does not completely abolish the EGFR autophosphorylation. In stably transfected NIH-3T3 cells harboring the L858R/T790M EGFR mutant, EAI045 shows the same activity. In L858R-mutant H3255 cells, EAI045 exhibits moderate activity. In the HaCaT cells, a keratinocyte cell line with wild-type EGFR, EAI045 does not show any activity of inhibiting EGFR phosphorylation. It confirms the selectivity of EAI045 for mutant EGFR[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

In a genetically engineered mouse model of L858R/T790Mmutant-driven lung cancer , remarkable tumor regression is observed in L858R/T790M-mutant mice treated with the combination of EAI045 and cetuximab. No response is seen in those mice treated with EAI045 alone. The same effect is seen in both L858R/T790M/C797S- engineered Ba/F3 cells and in mice carrying the L858R/T790M/C797S tumor xenografts. These assays clearly show that EAI045 can overcome resistance from acquired T790M and C797S mutations[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

383.40

Formula

C19H14FN3O3S
CAS 号

1942114-09-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (260.82 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6082 mL 13.0412 mL 26.0824 mL
5 mM 0.5216 mL 2.6082 mL 5.2165 mL
10 mM 0.2608 mL 1.3041 mL 2.6082 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.52 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.52 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (6.52 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (6.52 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.52 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.52 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Jia Y, et al. Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors. Nature. 2016 Jun 2;534(7605):129-32.

    [2]. Wang S, et al. EAI045: The fourth-generation EGFR inhibitor overcoming T790M and C797S resistance. Cancer Lett. 2017 Jan 28;385:51-54.
Cell Assay
[1]

For the experiment studying the effect of EGF pre-treatment on EAI045 target modulation, H1975 cells are harvested and plated in 0.5% FBS/RPMI Pen/Strep. On the following day, cells are pre-treated with 0.5% FBS/RPMI media with or without 10 ng EGF/mL for 5 minutes. Compound is added and assay is carried out[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice: Cetuximab is administrated at 1 mg/mouse every other day by intraperitoneal injection. The TL, TD and TLCS mice are monitored by MRI to quantify lung tumor burden before being assigned to various study treatment cohorts, which are non-blinded and not formally randomized. All treated mice had an equal initial tumor burden. MRI evaluation is repeated every 2 weeks during treatment. The animals are imaged with a rapid acquisition with relaxation enhancement sequence in the coronal and axial planes with a 1-mm slice thickness gating with respiratory rates. The tumor burden volumes are quantified[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Jia Y, et al. Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors. Nature. 2016 Jun 2;534(7605):129-32.

    [2]. Wang S, et al. EAI045: The fourth-generation EGFR inhibitor overcoming T790M and C797S resistance. Cancer Lett. 2017 Jan 28;385:51-54.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

PD168393

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PD168393  纯度: 98.60%

PD168393 是有效、选择性和细胞渗透性的 EGFR 酪氨酸激酶 (EGFR tyrosine kinase) 和 ErbB2 的抑制剂。PD168393 不可逆转地失活 EGF 受体 (IC50=0.7 nM)，但对胰岛素受体、PDGFR、FGFR 和 PKC 无作用。

PD168393

PD168393 Chemical Structure

CAS No. : 194423-15-9

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥625 In-stock
2 mg ￥550 In-stock
5 mg ￥770 In-stock
10 mg ￥1300 In-stock
25 mg ￥2600 In-stock
50 mg ￥4600 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

PD168393 相关产品

•相关化合物库:

  • Covalent Screening Library Plus
  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Immunology/Inflammation Compound Library
  • JAK/STAT Compound Library
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Covalent Screening Library
  • Differentiation Inducing Compound Library
  • Anti-Hepatitis C Virus Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

PD168393 is a potent, selective and cell-permeable inhibitor of EGFR tyrosine kinase and ErbB2. PD168393 irreversiblely inactivates EGF receptor ( IC50=0.7 nM) and is inactive against insulin receptor, PDGFR, FGFR and PKC[1].

IC50 & Target[1]

EGFR

0.7 nM (IC50)

体外研究
(In Vitro)

PD168393 inhibits ligand-dependent receptor phosphorylation and inhibits EGF-induced tyrosine phosphorylation in A431 cells and Heregulin-induced tyrosine phosphorylation in MDA-MB-453 cells with IC50 values of 4.3  nM and 5.7  nM, respectively[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

PD168393 (intraperitoneal injection; 58 mg/kg; once daily; days 10-14, 17-21, and 24-28) is effective in vivo, and produces tumor growth inhibition of 115% after 15 days’ treatment in human epidermoid carcinoma xenografts in mice[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: A431 human epidermoid carcinoma grown as a xenograft in nude mice[1]
Dosage: 58 mg/kg
Administration: Intraperitoneal injection; 58 mg/kg; once daily; days 10-14, 17-21, and 24-28
Result: Suppressed the growth of human epidermoid carcinoma xenografts.

分子量

369.22

Formula

C17H13BrN4O
CAS 号

194423-15-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 30 mg/mL (81.25 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7084 mL 13.5421 mL 27.0841 mL
5 mM 0.5417 mL 2.7084 mL 5.4168 mL
10 mM 0.2708 mL 1.3542 mL 2.7084 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.77 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.77 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. D W Fry, et al. Specific, irreversible inactivation of the epidermal growth factor receptor and erbB2, by a new class of tyrosine kinase inhibitor. Proc Natl Acad Sci U S A. 1998 Sep 29;95(20):12022-7.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

ONO-7475

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

ONO-7475  纯度: 99.38%

ONO-7475 是一种有效的、选择性的、具有口服活性的 Axl/Mer 抑制剂，IC50 值分别为 0.7 nM 和 1.0 nM。ONO-7475 使 AXL 过表达的 EGFR 突变型 NSCLC 细胞对 EGFR-TKIs 敏感，抑制耐药细胞的产生和耐药性的维持。ONO-7475 联合 Osimertinib (HY-15772) 为 EGFR 突变非小细胞肺癌 (NSCLC) 的研究提供了一个光明的前景。

ONO-7475

ONO-7475 Chemical Structure

CAS No. : 1646839-59-9

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥3090 In-stock
5 mg ￥2500 In-stock
10 mg ￥3500 In-stock
50 mg ￥7800 In-stock
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  • Neuronal Signaling Compound Library
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  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Drug Repurposing Compound Library
  • Orally Active Compound Library
  • Anti-Lung Cancer Compound Library

生物活性

ONO-7475 is a potent, selective, and orally active Axl/Mer inhibitor with IC50 values of 0.7 nM and 1.0 nM, respectively. ONO-7475 sensitizes AXL-overexpressing EGFR-mutant NSCLC cells to the EGFR-TKIs, suppresses the emergence and maintenance of tolerant cells. ONO-7475 combines with Osimertinib (HY-15772) provides a bright promise for the study of EGFR-mutated non-small cell lung cancer (NSCLC)[1].

IC50 & Target

IC50: 0.7 nM (AXL)[1]
IC50: 1.0 nM (MER tyrosine kinase)[2]
体外研究
(In Vitro)

ONO-7475 is against recombinant human AXL with IC50 values of 0.414 nM and 0.7 nM in off-chip MSA and ACD cell-based tyrosine kinase assay, respectively. It is against AXL, MER, TYRO3, TRKB, PDGFR alpha, TRKA, and FLT3 activities with IC50 values of 0.7 nM, 1.0 nM, 8.7 nM, 15.8 nM, 28.9 nM, 35.7 nM and 147 nM, respectively in a Cell-based Tyrosine Kinase assay[2].
ONO-7475 (0.0001 μM-1 μM; 72 hours) increases the sensitivity to Osimertinib and Dacomitinib and reduces the viability of high AXL-expressing PC-9 and HCC4011 cells, but not of low-AXL-expressing HCC827 cells. Besides, ONO-7475 enhances Osimertinib efficacy on the viability of cell lines PC-9, PC-9KGR, and HCC4011, and H1975, all of which express high levels of AXL. But it has a marginal effect on the viability of cell lines HCC827, HCC4006, and H3255 with low levels of AXL[1].
ONO-7475 (1 μM; 4 or 48 hours) combines with Osimertinib markedly inhibits the phosphorylation of AXL, AKT, and p70S6K compared with the treatment of the high-AXL-expressing cell lines treated with Osimertinib alone at 4 hours. It combines with osimertinib increases cleaved PARP in PC-9 and HCC4011 cells compared with the treatment with Osimertinib alone[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: High AXL-expressing cell: PC-9,HCC4011,H1975, PC-9KGR cells
Low AXL-expressing cell: HCC827, HCC4006, and H3255 cells
Concentration: 0.0001 μM; 0.001 μM; 0.01 μM; 0.1 μM; 1 μM
Incubation Time: 72 hours
Result: Increased the sensitivity and efficacy to Osimertinib in AXL-high level cells.

Western Blot Analysis[1]

Cell Line: PC-9, HCC4011 cells
Concentration: 1 μM
Incubation Time: 4 or 48 hours
Result: Increased p-AXL, AKT, and p70S6K expression at 4 hours and increases p-PARP expression at 48 hours when combindes with Osimertinib.

体内研究
(In Vivo)

ONO-7475 (oral gavage; 10 mg/kg or combines with 5 mg/kg Osimertinib; 29 days) treatment alone has little effect on the tumor growth. Besides, Osimertinib alone causes tumor regression within one week, but the tumors reappear within three weeks. The combined initial treatment causes tumor regression and the size of tumors is maintained for 4 weeks. No apparent adverse events, including weight loss are observed during these treatments[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Mouse CDX model using high-AXL-expressing PC-9KGR cells (exon 19 deletion and the exon21-T790M mutation in EGFR)[1]
Dosage: 10 mg/kg; once daily; 19 days
Administration: oral gavage
Result: Had little effects alone, but combined treatments significantly decreased tumor volume without reappear.

Clinical Trial

分子量

562.57

Formula

C32H26N4O6
CAS 号

1646839-59-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 250 mg/mL (444.39 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7776 mL 8.8878 mL 17.7756 mL
5 mM 0.3555 mL 1.7776 mL 3.5551 mL
10 mM 0.1778 mL 0.8888 mL 1.7776 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Okura N, et al. ONO-7475, a Novel AXL Inhibitor, Suppresses the Adaptive Resistance to Initial EGFR-TKI Treatment in EGFR-Mutated Non-Small Lung Cancer.Clin Cancer Res. 2020 Jan 17.

    [2]. Ruvolo PP, et al. Anexelekto/MER tyrosine kinase inhibitor ONO-7475 arrests growth and kills FMS-like tyrosine kinase 3-internal tandem duplication mutant acute myeloid leukemia cells by diverse mechanisms.Haematologica. 2017 Dec;102(12):2048-2057.

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CHMFL-EGFR-202

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CHMFL-EGFR-202 

CHMFL-EGFR-202 是一种有效、不可逆的表皮生长因子受体 (EGFR) 突变型激酶抑制剂， 对 耐药突变型 EGFR T790M 和 WT EGFR 激酶作用的 IC50 值分别为 5.3 nM 和 8.3 nM。在细胞中，CHMFL-EGFR-202 对 EGFR L858R/T790M 的选择性是 EGFR 野生型的 10 倍。CHMFL-EGFR-202 以 “DFG-in-C-helix-out” 的不活跃结合构象形式共价结合 EGFR，对 EGFR 突变体驱动的非小细胞肺癌 (NSCLC) 细胞株具有较强的抗增殖作用。

CHMFL-EGFR-202

CHMFL-EGFR-202 Chemical Structure

CAS No. : 2089381-40-6

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生物活性

CHMFL-EGFR-202 is a potent, irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant kinase, with IC50s of 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases, respectively. CHMFL-EGFR-202 exhibits ∼10-fold selectivity for EGFR L858R/T790M against the EGFR wild-type in cells. CHMFL-EGFR-202 adopts a covalent “DFG-in-C-helix-out” inactive binding conformation with EGFR, with strong antiproliferative effects against EGFR mutant-driven nonsmall-cell lung cancer (NSCLC) cell lines[1].

IC50 & Target

EGFRT790M

5.3 nM (IC50)

EGFR

8.3 nM (IC50)

ErbB2

8.1 nM (IC50)

ErbB4

3.2 nM (IC50)

MEK1

161 nM (IC50)

Btk

24.5 nM (IC50)

BLK

8.1 nM (IC50)

BMX

111 nM (IC50)

体外研究
(In Vitro)

CHMFL-EGFR-202 potently inhibits EGFR primary mutants (L858R, del19) and drug-resistant mutant L858R/T790M[1].
CHMFL-EGFR-202 displays strong binding affinities against wild-type, G719C/S, L858R, L858R/T790M, L861Q, and T790M among EGFR wild-type and mutant kinases[1].
CHMFL-EGFR-202 also exhibits strong binding affinities against BLK, BMX, BTK, ERBB2, ERBB4, LOK, MEK1, and MEK5 kinases (percent of control score less than 1% at 1 μM)[1].
CHMFL-EGFR-202 trongly inhibits BLK, BTK, ERBB2 and ERBB4 with IC50s of 8.1 nM, 24.5 nM, 8.1 nM and 3.2 nM, respectively[1].
CHMFL-EGFR-202 moderately inhibits BMX and MEK1 kinases with IC50 of 111.0 nM and 161.0 nM[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

489.96

Formula

C25H24ClN7O2
CAS 号

2089381-40-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Wang A, et al. Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode.

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Mutated EGFR-IN-2

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Mutated EGFR-IN-2 

Mutated EGFR-IN-2 (compound 91) 突变选择性的 EGFR 抑制剂，有效抑制单突变体 EGFR (T790M) 和双突变体 EGFR (包括 L858R/T790M (IC50=＜1nM) 和 ex19del/T790M)，并且可以抑制单一功能获得性突变 EGFR (包括 L858R 和 ex19del) 的活性。Mutated EGFR-IN-2 具有抗肿瘤活性。

Mutated EGFR-IN-2

Mutated EGFR-IN-2 Chemical Structure

CAS No. : 2050906-97-1

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生物活性

Mutated EGFR-IN-2 (compound 91) is a mutant-selective EGFR inhibitor extracted from patent WO2017036263A1, which potently inhibits single-mutant EGFR (T790M) and double-mutant EGFR (including L858R/T790M (IC50=＜1nM) and ex19del/T790M), and can suppress activity of single gain-of-function mutant EGFR (including L858R and ex19del) as well. Mutated EGFR-IN-2 shows anti-tumor antivity[1].

IC50 & Target[1]

EGFRT790M

 

EGFRL858R

 

EGFRex19del

 

EGFR (L858R/T790M)

<1 nM (IC50)

EGFR (ex19del/T790M)

 

分子量

562.64

Formula

C29H35FN8O3
CAS 号

2050906-97-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. 2, 4-di-(nitrogen containing group) substituted pyrimidine compound and preparation method and use thereof.

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BI-4020

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

BI-4020  纯度: ≥99.0%

BI-4020 是一种第四代，具有口服活性，非共价的 EGFR 酪氨酸激酶抑制剂。BI-4020 不仅抑制三联突变的 EGFR del19 T790M C797S 突变体 (在 BaF3 细胞系中，IC50=0.2 nM)，也抑制双重突变的 EGFR del19 T790M 和单突变的 EGFR del19 (IC50=1 nM)。BI-4020 同时保留了针对 EGFR wt 的活性 (IC50=190 nM)。BI-4020 显示高激酶组选择性和良好的 DMPK 特性。

BI-4020

BI-4020 Chemical Structure

CAS No. : 2664214-60-0

规格 价格 是否有货 数量
1 mg ￥3500 In-stock
5 mg ￥11000 In-stock
10 mg   询价  
50 mg   询价  

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BI-4020 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Macrocyclic Compound Library

生物活性

BI-4020 is a fourth-generation, orally active, and non-covalent EGFR tyrosine kinase inhibitor. BI-4020 inhibits not only the triple mutant EGFR del19 T790M C797S variant (IC50=0.2 nM in BaF3 cell lines) but also the double mutant EGFR del19 T790M and primary mutant EGFR del19 (IC50=1 nM). BI-4020 also shows activity against EGFR wt (IC50=190 nM). BI-4020 shows high kinome selectivity and good DMPK properties[1].

IC50 & Target[1]

EGFRdel19 T790M C797S

0.2 nM (IC50)

EGFRdel19 T790M

 

EGFRdel19

1 nM (IC50)

EGFRWT

190 nM (IC50)

体外研究
(In Vitro)

BI-4020 inhibits p-EGFR del19 T790M C797S with an IC50 of 0.6 nM[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

BI-4020 leads to tumor regressions in the human PC-9 (EGFR del19 T790M C797S) triple mutant NSCLC xenograft model in mice[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

542.68

Formula

C30H38N8O2
CAS 号

2664214-60-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 250 mg/mL (460.68 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8427 mL 9.2135 mL 18.4271 mL
5 mM 0.3685 mL 1.8427 mL 3.6854 mL
10 mM 0.1843 mL 0.9214 mL 1.8427 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.83 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.83 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.83 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.83 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.83 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.83 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Engelhardt H,et al. Start selective and rigidify: The discovery path towards a next generation of EGFR tyrosine kinase inhibitors. J Med Chem. 2019 Nov 5.

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EGFR-IN-1 hydrochloride

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

EGFR-IN-1 hydrochloride 

EGFR-IN-1 hydrochloride 是一种口服活性不可逆的突变型选择性 L858R/T790M EGFR 抑制剂。与野生型 EGFR 相比，EGFR-IN-1 hydrochloride 对 Gefitinib 耐药的 EGFR L858R/T790M 有 100 倍的抑制作用。EGFR-IN-1 hydrochloride 对 H1975 细胞和 HCC827 细胞具有较强的抗增殖活性。具有抗肿瘤活性。

EGFR-IN-1 hydrochloride

EGFR-IN-1 hydrochloride Chemical Structure

CAS No. : 2227455-78-7

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EGFR-IN-1 hydrochloride 的其他形式现货产品:

EGFR-IN-1 TFA

生物活性

EGFR-IN-1 hydrochloride is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 hydrochloride potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 hydrochloride displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity[1].

IC50 & Target[1]

EGFRL858R/T790M

 

体外研究
(In Vitro)

EGFR-IN-1 hydrochloride (compound 24) (10 μM; 72 hours) displays strong antiproliferative activity against the H1975 and HCC827 cells with IC50s of 4 and 28 nM, respectively[1].
EGFR-IN-1 hydrochloride inhibits p-EGFR in H1975 and HCC827 cells with IC50s of 4 and 9 nM, respectively. EGFR-IN-1 highly selective against a panel of 100 kinases[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: NSCLC cell lines H1975 (T790M/L858R), HCC827 (∆746-750)
Concentration: 10 μM
Incubation Time: 72 hours
Result: Inhibited H1975 nonsmall cell lung cancer cell line and the first line mutant HCC827 cell line with IC50s of 4 and 28 nM, respectively.

体内研究
(In Vivo)

EGFR-IN-1 hydrochloride (30 mg/kg; p.o.; daily for 2 weeks) displays significant tumor growth inhibition with no observed loss in body weight[1].
EGFR-IN-1 hydrochloride evaluates in a time course PD experiment upon oral dosing at 30 mg/kg. EGFR-IN-1 shows a >50% inhibition of phosphorylation of EGFR for >12 h. EGFR-IN-1 reaches maximal concentration of 0.10 μM at 2 h and systemic exposure (AUC0-inf.) is 0.33 μM. h[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female athymic nude mice (H1975 Tumor Xenograft)[1]
Dosage: 30 mg/kg
Administration: p.o.; daily for 2 weeks
Result: Led to significant tumor growth inhibition with no observed loss in body weight.

分子量

551.04

Formula

C28H31ClN6O4
CAS 号

2227455-78-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Wurz RP, et al. Oxopyrido[2,3-d]pyrimidines as Covalent L858R/T790M Mutant Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors. ACS Med Chem Lett. 2015 Jul 27;6(9):987-92.

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EMI48

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

EMI48  纯度: 99.02%

EMI48 是 EMI1 的衍生物，EMI48 比 EMI1 对突变型 EGFR 具有更大的效力。EMI48 抑制 EGFR 三重突变体。

EMI48

EMI48 Chemical Structure

CAS No. : 34564-13-1

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3300 In-stock
5 mg ￥3000 In-stock
10 mg ￥4800 In-stock
50 mg ￥14000 In-stock
100 mg ￥20000 In-stock
200 mg   询价  
500 mg   询价  

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EMI48 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • JAK/STAT Compound Library
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Differentiation Inducing Compound Library
  • Anti-Hepatitis C Virus Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Targeted Diversity Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

EMI48, the derivative of EMI1, displays greater potency toward mutant EGFR than EMI1. EMI48 inhibits EGFR triple mutants[1].

IC50 & Target[1]

EGFRL858R/T790M/C797S

 

EGFRdel19 T790M C797S

 

体外研究
(In Vitro)

EMI48 inhibits EGFR ex19del/T790M/C797S and EGFR L858R/T790M/C797S. EMI48 can be used in the research of mutant EGFR-associated, drug-resistant non-small-cell lung cancer (NSCLC)[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

348.40

Formula

C21H20N2O3
CAS 号

34564-13-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 9.26 mg/mL (26.58 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.8703 mL 14.3513 mL 28.7026 mL
5 mM 0.5741 mL 2.8703 mL 5.7405 mL
10 mM 0.2870 mL 1.4351 mL 2.8703 mL

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储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Punit Saraon , et al. A Drug Discovery Platform to Identify Compounds That Inhibit EGFR Triple Mutants.Nat Chem Biol. 2020 May;16(5):577-586.

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EGFR mutant-IN-1

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

EGFR mutant-IN-1 

EGFR mutant-IN-1 是一种 5-甲基嘧啶吡啶酮衍生物，是有效的，选择性 EGFRL858R/T790M/C797S 突变抑制剂，IC50 为 27.5 nM，对 EGFRWT 的抑制作用明显较低 (IC50 >1.0 μM)。

EGFR mutant-IN-1

EGFR mutant-IN-1 Chemical Structure

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生物活性

EGFR mutant-IN-1, a 5-methylpyrimidopyridone derivative, is a potent and selective EGFRL858R/T790M/C797S mutant inhibitor with an IC50 of 27.5 nM, while being a significantly less potent for EGFRWT (IC50 >1.0 μM)[1].

IC50 & Target

IC50: 27.5 nM (EGFRL858R/T790M/C797S) and >1.0 μM (EGFRWT)[1]
分子量

632.17

Formula

C34H39ClFN7O2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Shen J, et al. Structure-Based Design of 5-Methylpyrimidopyridone Derivatives as New Wild-Type SparingInhibitors of the Epidermal Growth Factor Receptor Triple Mutant (EGFRL858R/T790M/C797S). J Med Chem. 2019 Aug 8;62(15):7302-7308.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务