标签归档：gnf

GNF5-amido-Me(Synonyms: PROTAC ABL binding moiety 2)

发表于由
回复

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。

GNF5-amido-Me (Synonyms: PROTAC ABL binding moiety 2)

GNF5-amido-Me 是一种基于 GNF5 (ABL 抑制剂) 的配体，可通过 linker 与 IAP 配体结合从而形成 SNIPER 分子。

GNF5-amido-Me(Synonyms: PROTAC ABL binding moiety 2)

GNF5-amido-Me Chemical Structure

CAS No. : 778277-37-5

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

* Please select Quantity before adding items.

生物活性

GNF5-amido-Me, the GNF5 (ABL inhibitor) based moiety, binds to IAP ligand via a linker to form SNIPER[1].

分子量

388.34

Formula

C19H15F3N4O2
CAS 号

778277-37-5
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]. Shibata N, et al. Development of protein degradation inducers of oncogenic BCR-ABL protein by conjugation of ABL kinase inhibitors and IAP ligands. Cancer Sci. 2017 Aug;108(8):1657-1666.

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

GNF-5837

发表于由
回复

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。

GNF-5837  纯度: 99.45%

GNF-5837 是一种有效的，选择性的，口服生物利用的泛 TRK 抑制剂，在 Ba/F3 细胞中显示出抗增殖作用 (对 Tel-TrkC, Tel-TrkB 和 Tel-TrkA 的 IC50 值分别为 7 nM，9 nM 和 11 nM)。 .

GNF-5837

GNF-5837 Chemical Structure

CAS No. : 1033769-28-6

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 ￥589 In-stock
5 mg ￥500 In-stock
10 mg ￥900 In-stock
25 mg ￥1500 In-stock
50 mg ￥2400 In-stock
100 mg ￥4000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

GNF-5837 相关产品

•相关化合物库:

  • Covalent Screening Library Plus
  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • Neuronal Signaling Compound Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Covalent Screening Library
  • Orally Active Compound Library
  • Chemical Probe Library
  • Targeted Diversity Library

生物活性

GNF-5837 is a potent, selective, and orally bioavailable pan-tropomyosin receptor kinase (TRK) inhibitor which display antiproliferative effects in cellular Ba/F3 assays ( IC50 values of 7 nM, 9 nM and 11 nM for cells containing the fusion proteins Tel-TrkC, Tel-TrkB and Tel-TrkA, respectively) [1].

IC50 & Target

TrkB

9 nM (IC50)

TrkC

7 nM (IC50)

TrkA

11 nM (IC50)

体外研究
(In Vitro)

GNF-5837 (0.1-500 nM; 72-144 hours; GOT1 cells) treatment decreases cell viability in a time- and dose-dependent manner in GOT1 cells[2].
GNF-5837 (5-500 nM; 24 hours; GOT1 cells) causes downregulation of PI3K-Akt-mTOR signaling, Ras-Raf-MEK-ERK signaling[2].
GNF-5837 (5-500 nM; 72 hours; GOT1 cells) treatment induces G1 cell cycle arrest[2].
GNF-5837 (500 nM; 144 hours; GOT1 cells) treatment increases apoptotic cell death[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 Viability Assay[2]

Cell Line: GOT1 cells
Concentration: 0.1 nM , 0.5 nM , 1 nM , 5 nM , 10 nM , 50 nM , 100 nM and 500 nM
Incubation Time: 72 hours, 96 hours and 144 hours
Result: Cell viability assay determined a clear decrease of GOT1 cell viability in a time- and dose- dependent manner.

Western Blot Analysis[2]

Cell Line: GOT1 cells
Concentration: 5 nM, 50 nM and 500 nM
Incubation Time: 24 hours
Result: Significant levels of TrkA expression, faint TrkC expression and no TrkB expression.

Cell Cycle Analysis[2]

Cell Line: GOT1 cells
Concentration: 5 nM, 500 nM
Incubation Time: 72 hours
Result: Induced G1 cell cycle arrest.

Apoptosis Analysis[2]

Cell Line: GOT1 cells
Concentration: 500 nM
Incubation Time: 144 hours
Result: Induced apoptosis.

体内研究
(In Vivo)

GNF-5837 (25-100 mg/kg; oral administration; once daily; for 10 days; mice) treatment inhibits tumor growth in a mouse xenograft model derived from RIE cells expressing both TRKA and NGF[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 xenograft model[1]
Dosage: 25 mg/kg, 50 mg/kg, 100 mg/kg
Administration: Oral administration; once daily; for 10 days
Result: 72 and 100% tumor regression was observed at 50 and 100 mg/kg, respectively. At 25 mg/kg, only partial tumor growth inhibition was achieved.

分子量

535.49

Formula

C28H21F4N5O2
CAS 号

1033769-28-6
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 : ≥ 32 mg/mL (59.76 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 1.8674 mL 9.3372 mL 18.6745 mL
5 mM 0.3735 mL 1.8674 mL 3.7349 mL
10 mM 0.1867 mL 0.9337 mL 1.8674 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 (4.67 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.67 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 (4.67 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (4.67 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
*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]. Albaugh, P. et al. Discovery of GNF-5837, a Selective TRK Inhibitor with Efficacy in Rodent Cancer Tumor Models. ACS MEDICINAL CHEMISTRY LETTERS, 2012; 3 (2): 140

    [2]. Aristizabal Prada ET, et al. Tropomyosin receptor kinase: a novel target in screened neuroendocrine tumors. Endocr Relat Cancer. 2018 May;25(5):547-560.

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

LCH-7749944(Synonyms: GNF-PF-2356)

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。

LCH-7749944 (Synonyms: GNF-PF-2356) 纯度: 99.43%

LCH-7749944 (GNF-PF-2356) 是一种有效的 PAK4 抑制剂，IC50 为 14.93 μM。LCH-7749944通过下调 PAK4/c-Src/EGFR/cyclin D1 途径有效抑制人胃癌细胞的增殖，并诱导凋亡 (apoptosis)。

LCH-7749944(Synonyms: GNF-PF-2356)

LCH-7749944 Chemical Structure

CAS No. : 796888-12-5

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 ￥2500 In-stock
5 mg ￥2200 In-stock
10 mg ￥3500 In-stock
50 mg ￥10500 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

LCH-7749944 相关产品

•相关化合物库:

  • Covalent Screening Library Plus
  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Cell Cycle/DNA Damage Compound Library
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Covalent Screening Library
  • Cytoskeleton Compound Library

生物活性

LCH-7749944 (GNF-PF-2356) is a potent PAK4 inhibitor with an IC50 of 14.93 μM. LCH-7749944 effectively suppresses the proliferation of human gastric cancer cells through downregulation of PAK4/c-Src/EGFR/cyclin D1 pathway and induces apoptosis[1].

IC50 & Target[1]

PAK4

14.93 μM (IC50)

体外研究
(In Vitro)

LCH-7749944 (GNF-PF-2356; 5-50 μM; 24 hours) inhibits the proliferation of MKN-1, BGC823, SGC7901 and MGC803 cells in a concentration dependent manner[1].
LCH-7749944 (5-20 μM; 12-48 hours) induces apoptosis of SGC7901 cells[1].
LCH-7749944 (5-20 μM; 12-48 hours) prominently induces a dose-dependent increase in the percentage of cells in G1 phase and decrease in S phase[1].
LCH-7749944 (5-30 μM; 24 hours) dramatically decreases levels of phosphoPAK4, phospho-c-Src, phospho-EGFR and cyclin D1 protein expression in a dose-dependent manner[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: MKN-1, BGC823, SGC7901 and MGC803 human gastric cancer cells
Concentration: 5, 10, 15, 20, 25, 30, 35, 40, 45, 50 μM
Incubation Time: 24 hours
Result: Inhibited the proliferation of MKN-1, BGC823, SGC7901 and MGC803 cells in a concentration dependent manner.

Apoptosis Analysis[1]

Cell Line: SGC7901 cells
Concentration: 5, 10, 20 μM
Incubation Time: 12, 24, 48 hours
Result: Induced apoptosis of SGC7901 cells.

Cell Cycle Analysis[1]

Cell Line: SGC7901 cells
Concentration: 5, 10, 20 μM
Incubation Time: 12, 24, 48 hours
Result: Prominently induced a dose-dependent increase in the percentage of cells in G1 phase and decrease in S phase.

Western Blot Analysis[1]

Cell Line: SGC7901 cells
Concentration: 5, 10, 20, 30 μM
Incubation Time: 24 hours
Result: Dramatically decreased levels of phosphoPAK4, phospho-c-Src, phospho-EGFR and cyclin D1 protein expression in a dose-dependent manner.

分子量

350.41

Formula

C20H22N4O2
CAS 号

796888-12-5
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 (713.45 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.8538 mL 14.2690 mL 28.5380 mL
5 mM 0.5708 mL 2.8538 mL 5.7076 mL
10 mM 0.2854 mL 1.4269 mL 2.8538 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: ≥ 2.17 mg/mL (6.19 mM); Clear solution

    此方案可获得 ≥ 2.17 mg/mL (6.19 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 21.7 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: ≥ 2.17 mg/mL (6.19 mM); Clear solution

    此方案可获得 ≥ 2.17 mg/mL (6.19 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 21.7 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
*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 J, et al. LCH-7749944, a novel and potent p21-activated kinase 4 inhibitor, suppresses proliferation and invasion in human gastric cancer cells. Cancer Lett. 2012 Apr 1;317(1):24-32.

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

GNF-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。

GNF-7  纯度: 98.93%

GNF-7 是一种多重激酶抑制剂。GNF-7 是 Bcr-Abl 的抑制剂，对 Bcr-AblWT 和 Bcr-AblT315I 作用的 IC50 值分别为 133 nM 和 61 nM。GNF-7 对 ACK1 和 GCK 也具有抑制活性，IC50 分别为 25 nM 和 8 nM。GNF-7 可用于血液恶性肿瘤的研究。

GNF-7

GNF-7 Chemical Structure

CAS No. : 839706-07-9

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 ￥1301 In-stock
5 mg ￥1080 In-stock
10 mg ￥1800 In-stock
25 mg ￥3500 In-stock
50 mg ￥6000 In-stock
100 mg ￥10500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

GNF-7 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Cytoskeleton Compound Library
  • Anti-Alzheimer’s Disease Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Parkinson’s Disease Compound Library
  • Neurodegenerative Disease-related Compound Library
  • Targeted Diversity Library

生物活性

GNF-7 is a multikinase inhibitor. GNF-7 is a Bcr-Abl inhibitor, with IC50s of 133 nM and 61 nM for Bcr-AblWT and Bcr-AblT315I, respectively. GNF-7 also possesses inhibitory activity against both ACK1 (activated CDC42 kinase 1) and GCK (germinal center kinase) with IC50s of 25 nM and 8 nM, respectively. GNF-7 can be used for the research of hematologic malignancies[1][2][3].

IC50 & Target

IC50: 133 nM (Bcr-AblWT)[1], 61 nM (Bcr-AblT315I)[1], 25 nM (ACK1)[3], 8 nM (GCK)[3]
体外研究
(In Vitro)

GNF-7 potently inhibits wild-type Bcr-Abl (IC50<5 nm) and bcr-abl mutants such as t315i (ic50=11 nM), G250E (IC50<5 nm), e255v (ic50=10 nM), F317L (IC50<5 nm) and m351t (ic50<5 nm) in cellular assays[2].
GNF-7 (1 μM; 2 hours) suppresses AKT/mTOR signaling and GCK downstream[3].
GNF-7 (1 μM; 24 hours) induces of apoptosis and cell cycle arrest in NRAS mutant cell lines[3].

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.

Western Blot Analysis[3]

Cell Line: Ba/F3-NRAS-G12D cells, OCI-AML3 cells
Concentration: 1 μM
Incubation Time: 2 hours
Result: Caused a decreased level of phosphorylation of p70S6K1, AKT (S473), JNK, and p38.

Apoptosis Analysis[3]

Cell Line: OCI-AML3 cells
Concentration: 1 μM
Incubation Time: 24 hours
Result: Increased the levels of both cleaved PARP and cleaved caspase 3 and diminished bcl-2 and MCL1.

Cell Cycle Analysis[3]

Cell Line: OCI-AML3 cells
Concentration: 1 μM
Incubation Time: 24 hours
Result: Induced of G0-G1 arrest.

体内研究
(In Vivo)

GNF-7 (10-20 mg/kg; o.p.; daily; for 7 days) displays significant in vivo efficacy against T315I Bcr-Abl in the bioluminescent xenograft mouse model[2].
GNF-7 exhibits moderate oral bioavailability (mice 36%) and Cmax (mice 3616 nM) following oral administration (mice 20 mg/kg)[2].
GNF-7 exhibits terminal elimination half-lives (mice 3.8 h) due to high plasma clearance (8.6 mL/min/kg) following intravenous injection (mice 5 mg/kg)[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.

Animal Model: 6-8 weeks old SCID beige female mice, with Ba/F3-T315I-Bcr-Abl cells xenograft[2]
Dosage: 10 mg/kg, 20 mg/kg
Administration: Oral administration, daily, for 7 days
Result: Effectively inhibited tumor growth of T315I-Bcr-Abl-Ba/F3 cells in mice at low doses (10 mg/kg).
Animal Model: 5-6 weeks old male Balb/c mice (20-25 g)[2]
Dosage: 5 mg/kg for i.v.; 20 mg/kg for i.g. (Pharmacokinetic Analysis)
Administration: Intravenous injection and oral gavage
Result: Oral bioavailability (36%), Cmax (3616 nM), T1/2 (3.2 h).

分子量

547.53

Formula

C28H24F3N7O2
CAS 号

839706-07-9
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 : ≥ 33 mg/mL (60.27 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 1.8264 mL 9.1319 mL 18.2638 mL
5 mM 0.3653 mL 1.8264 mL 3.6528 mL
10 mM 0.1826 mL 0.9132 mL 1.8264 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 mg/mL (3.65 mM); Clear solution

    此方案可获得 ≥ 2 mg/mL (3.65 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.0 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 mg/mL (3.65 mM); Clear solution

    此方案可获得 ≥ 2 mg/mL (3.65 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.0 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
*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]. Lu X, et al. Hybrid pyrimidine alkynyls inhibit the clinically resistance related Bcr-Abl(T315I) mutant. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3458-63.

    [2]. Choi HG, et al. A type-II kinase inhibitor capable of inhibiting the T315I “gatekeeper” mutant of Bcr-Abl. J Med Chem. 2010 Aug 12;53(15):5439-48.

    [3]. Cho, H., et al. First SAR study for overriding NRAS mutant driven acute myeloid leukemia. Journal of Medicinal Chemistry.

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

ML348(Synonyms: GNF-Pf-1127)

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。

ML348 (Synonyms: GNF-Pf-1127) 纯度: 99.96%

ML348 (GNF-Pf-1127) 是一个选择性的和可逆的 酰基蛋白硫酯酶 1 (APT1)/溶血磷脂酶 1 (LYPLA1) 抑制剂, IC50 值为 210 nM。

ML348(Synonyms: GNF-Pf-1127)

ML348 Chemical Structure

CAS No. : 899713-86-1

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥935 In-stock
5 mg ￥850 In-stock
10 mg ￥1400 In-stock
25 mg ￥2800 In-stock
50 mg ￥4800 In-stock
100 mg ￥7800 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

ML348 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Lipid Metabolism Compound Library

生物活性

ML348 (GNF-Pf-1127) is a selective and reversible acyl-protein thioesterase 1 (APT1)/lysophospholipase 1 (LYPLA1) inhibitor with an IC50 of 210 nM, and barely inhibits LYPLA2[1].

IC50 & Target

IC 50: 210 nM (LYPLA1)
体外研究
(In Vitro)

ML348 (5 µM; 3 hours ) selectively inhibits LYPLA1 in cultured 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.

Cell Viability Assay[1]

Cell Line: HEK293T cells, murine T-cells
Concentration: 5 µM
Incubation Time: 3 hours
Result: Show potent, selective inhibition of LYPLA1.

体内研究
(In Vivo)

ML348 (50 mg/kg, i.p., 3 hours) shows potent and selective activity in vivo, inhibits LYPLA1 enzymes in heart, kidney and lung 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: C57BL6 male mice (3-4 months)[1]
Dosage: 50 mg/kg
Administration: Intraperitoneal injection; 3 hours
Result: Potent and selective inhibited LYPLA1 enzymes in heart, kidney and lung in vivo.

分子量

415.79

Formula

C18H17ClF3N3O3
CAS 号

899713-86-1
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 : 25 mg/mL (60.13 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4051 mL 12.0253 mL 24.0506 mL
5 mM 0.4810 mL 2.4051 mL 4.8101 mL
10 mM 0.2405 mL 1.2025 mL 2.4051 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    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.01 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.01 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]. Adibekian A et al. Characterization of a Selective, Reversible Inhibitor of Lysophospholipase 1 (LYPLA1). National Center for Biotechnology Information (US); 2010- 2013 Apr 08.

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

GNF-5

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。

GNF-5  纯度: 99.42%

GNF-5是GNF-2的类似物，具有更好的药物动力学活性，是非ATP竞争性的Bcr-Abl抑制剂，IC50为0.22uM。

GNF-5

GNF-5 Chemical Structure

CAS No. : 778277-15-9

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 ￥550 In-stock
10 mg ￥500 In-stock
50 mg ￥1485 In-stock
100 mg ￥2100 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

GNF-5 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Anti-Infection Compound Library
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Antiviral Compound Library
  • Cytoskeleton Compound Library
  • Chemical Probe Library
  • Anti-Alzheimer’s Disease Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Parkinson’s Disease Compound Library
  • Neurodegenerative Disease-related Compound Library

生物活性

GNF-5, an analogue of GNF-2 with improved pharmacokinetic properties, is a selective non-ATP competitive inhibitor of Bcr-Abl with an IC50 value of 0.22±0.1 uM (Wild type Abl). IC50 Value: 0.22±0.1 uM (Wild type Abl) [1] Target: Abl GNF-5 is a cell-permeable GNF-2 N-hydroxyethyl carboxamide analog that exhibits in vivo efficacy in suppressing the proliferation of Bcr-abl-expressing Ba/F3 (93% and 83% of no-treatment control, respectively, on days 5 and 7 post treatment; 100 mg/kg b.i.d.) and bone marrow cells (~75% of no-treatment control in both WBC counts and spleen weight on day 7 post treatment; 50 mg/kg b.i.d.) in murine xenograft models of leukemia. Similar to GNF-2, GNF-5 exerts its effect via an allosteric mechanism (IC50 = 0.22 M against wild-type Abl) by targeting the myristate-binding pocket near the c-terminus of Abl kinase domain and thereby altering the conformational dynamics of the ATP-binding pocket. GNF-5 is ineffective toward the myristate-binding site mutant E505K and the ATP-binding site ‘gatekeeper’ mutant T315I.

分子量

418.37

Formula

C20H17F3N4O3
CAS 号

778277-15-9
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 : ≥ 49 mg/mL (117.12 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 2.3902 mL 11.9511 mL 23.9023 mL
5 mM 0.4780 mL 2.3902 mL 4.7805 mL
10 mM 0.2390 mL 1.1951 mL 2.3902 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 (5.98 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.98 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 (5.98 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.98 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 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 (5.98 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.98 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]. Zhang J, et al. Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors. Nature. 2010 Jan 28;463(7280):501-6.

    [2]. Meirson T, et al. Targeting invadopodia-mediated breast cancer metastasis by using ABL kinase inhibitors. Oncotarget. 2018 Apr 24;9(31):22158-22183.

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

GNF-2

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。

GNF-2  纯度: 98.73%

GNF-2 是一种具有高度选择性、变构的、非 ATP 竞争性 Bcr-Abl 抑制剂。 GNF-2 抑制 Ba/F3.p210 增殖， IC50 为 138 nM。

GNF-2

GNF-2 Chemical Structure

CAS No. : 778270-11-4

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥770 In-stock
5 mg ￥700 In-stock
10 mg ￥1200 In-stock
50 mg ￥4500 In-stock
100 mg ￥7500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

GNF-2 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Anti-Infection Compound Library
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Antiviral Compound Library
  • Cytoskeleton Compound Library
  • Anti-Alzheimer’s Disease Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Parkinson’s Disease Compound Library
  • Neurodegenerative Disease-related Compound Library

生物活性

GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC50 of 138 nM [1].

IC50 & Target[1]

Bcr-Abl

 

体外研究
(In Vitro)

GNF-2 selectively inhibits Bcr-abl-dependent cell proliferation. GNF-2 (0.005-10 μM; 48 hours) specifically inhibits the proliferation of the Bcr-abl-expressing cells with an IC50 of 138 nM and not show any cytotoxic effects on the nontransformed cells at concentrations of up to 10 μM. GNF-2 (0.005-10 μM; 48 hours) causes a dose-dependent growth inhibition of the Bcr-abl-positive cell lines with IC50 values of 273 nM (K562) and 268 nM (SUP-B15). GNF-2 (0.005-10 μM; 48 hours) inhibits E255V and Y253H mutant Bcr-abl cell growth (IC50 values of 268 and 194 nM, respectively)[1].
GNF-2 (1-10 μM; 48 hours) induces apoptosis of Bcr-abl-transformed cells[1].
GNF-2 (0.1-10 μM; 90 minutes) inhibits the cellular tyrosine phosphorylation of Bcr-abl in a dose-dependent manner with an IC50 of 267 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.

Cell Proliferation Assay[1]

Cell Line: Ba/F3.p210, Ba/F3.p210E255V and Ba/F3.p185Y253H cells
Concentration: 0.005, 0.01, 0.1, 1, 10 μM
Incubation Time: 48 hours
Result: Inhibited Bcr-abl-transformed cells proliferation.

Apoptosis Analysis[1]

Cell Line: Ba/F3.p210 and Ba/F3.p210E255V cells
Concentration: 1, 10 μM
Incubation Time: 48 hours
Result: Increased number of Ba/F3.p210 cells undergoing apoptosis at 1 μM for 48 h.
Ba/F3.p210E255V underwent apoptotic death after 48 h incubation in the presence of 1 μM or higher concentration.

Western Blot Analysis[1]

Cell Line: Ba/F3.p210 and Ba/F3.p210E255V cells
Concentration: 0.1, 1, 10 μM
Incubation Time: 90 minutes
Result: Decreased the autophosphorylation levels at a concentration of 1 μM and were barely detectable at 10 μM, whereas the level of total Bcr-abl remained unchanged.
Induced a significant decrease in the levels of p-Stat5 (at Y694) at 1 μM in Ba/F3.p210 and Ba/F3.p210E255V cells.

体内研究
(In Vivo)

GNF-2 (10 mg/kg; i.p. for 8 days) protects LPS (5 mg/kg) induced bone erosion in mice. GNF-2 protects the LPS induced bone loss and abrogates the LPS-induced decreases of bone volume/tissue volume (BV/TV) of LPS-treated mice[2].
GNF-2 prevents the LPS-induced increases of N.Oc/B.Pm, the percentage of Oc.S/BS, and the percentage of ES/BS[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.

Animal Model: Eight-week-old C57/BL6 mice were administered i.p. injections of LPS (5 mg/kg)[2]
Dosage: 10 mg/kg
Administration: I.p. injections for 8 days; 1 day before and every day after the LPS injection
Result: Prevented inflammatory bone destruction in vivo.

分子量

374.32

Formula

C18H13F3N4O2
CAS 号

778270-11-4
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 (267.15 mM)

H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

* “≥” 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 2.6715 mL 13.3576 mL 26.7151 mL
5 mM 0.5343 mL 2.6715 mL 5.3430 mL
10 mM 0.2672 mL 1.3358 mL 2.6715 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 (6.68 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.68 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 (6.68 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.68 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 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 (6.68 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.68 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]. Adrián FJ, et al. Allosteric inhibitors of Bcr-abl-dependent cell proliferation. Nat Chem Biol. 2006 Feb;2(2):95-102.

    [2]. Kim HJ, et al. The tyrosine kinase inhibitor GNF-2 suppresses osteoclast formation and activity. J Leukoc Biol. 2013 Oct 15.

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

GNF-6231

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。

GNF-6231  纯度: 99.81%

GNF-6231是一个强的，有选择性的，能够口服的Porcupine抑制剂能够阻止Wnt信号通路。

GNF-6231

GNF-6231 Chemical Structure

CAS No. : 1243245-18-2

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1381 In-stock
2 mg ￥1000 In-stock
5 mg ￥1400 In-stock
10 mg ￥2200 In-stock
50 mg ￥7500 In-stock
100 mg ￥12000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

GNF-6231 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Stem Cell Signaling Compound Library
  • Wnt/Hedgehog/Notch Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Orally Active Compound Library
  • Targeted Diversity Library

生物活性

GNF-6231 is a potent, selective, and orally bioavailable Porcupine inhibitor that blocks Wnt signaling. 1) GNF-6231 shows IC50s of greater than 10 μM on all CYP isoforms tested 2) GNF-6231 have favorable potency and a PK profile across preclinical species upon oral administration. 3) The reference for orally in MMTV-Wnt1 tumor bearing mice is dosed at 3 mg/kg. 4) GNF-6231 showed very robust dose-related antitumor efficacy.

分子量

448.49

Formula

C24H25FN6O2
CAS 号

1243245-18-2
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 : ≥ 36 mg/mL (80.27 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 2.2297 mL 11.1485 mL 22.2970 mL
5 mM 0.4459 mL 2.2297 mL 4.4594 mL
10 mM 0.2230 mL 1.1149 mL 2.2297 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: ≥ 3 mg/mL (6.69 mM); Clear solution

    此方案可获得 ≥ 3 mg/mL (6.69 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 30.0 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: ≥ 3 mg/mL (6.69 mM); Clear solution

    此方案可获得 ≥ 3 mg/mL (6.69 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 30.0 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: ≥ 3 mg/mL (6.69 mM); Clear solution

    此方案可获得 ≥ 3 mg/mL (6.69 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 30.0 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]. Cheng D et al. Discovery of Pyridinyl Acetamide Derivatives as Potent, Selective, and Orally Bioavailable Porcupine Inhibitors. ACS Med Chem Lett. 2016 May 10;7(7):676-80.

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

GNF-8625 monopyridin-N-piperazine hydrochloride

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。

GNF-8625 monopyridin-N-piperazine hydrochloride 

GNF-8625 monopyridin-N-piperazine hydrochloride (TRKi-2) 是TRK 的抑制剂，信息来自专利 WO 2020038415 A1。

GNF-8625 monopyridin-N-piperazine hydrochloride

GNF-8625 monopyridin-N-piperazine hydrochloride Chemical Structure

CAS No. : 2412055-62-8

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

GNF-8625 monopyridin-N-piperazine hydrochloride (TRKi-2), a TRK inhibitor, which is from the patent WO 2020038415 A1[1].

分子量

479.98

Formula

C25H27ClFN7
CAS 号

2412055-62-8
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]. By Liu, Jing, et al. Preparation of tropomyosin receptor kinase degradation compounds and methods of use. WO 2020038415 A1.

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

GNF-8625 monopyridin-N-piperazine hydrochloride

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。

GNF-8625 monopyridin-N-piperazine hydrochloride 

GNF-8625 monopyridin-N-piperazine hydrochloride (TRKi-2) 是TRK 的抑制剂，信息来自专利 WO 2020038415 A1。

GNF-8625 monopyridin-N-piperazine hydrochloride

GNF-8625 monopyridin-N-piperazine hydrochloride Chemical Structure

CAS No. : 2412055-62-8

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

GNF-8625 monopyridin-N-piperazine hydrochloride (TRKi-2), a TRK inhibitor, which is from the patent WO 2020038415 A1[1].

分子量

479.98

Formula

C25H27ClFN7
CAS 号

2412055-62-8
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]. By Liu, Jing, et al. Preparation of tropomyosin receptor kinase degradation compounds and methods of use. WO 2020038415 A1.

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

GNF-8625 monopyridin-N-piperazine hydrochloride

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。

GNF-8625 monopyridin-N-piperazine hydrochloride 

GNF-8625 monopyridin-N-piperazine hydrochloride (TRKi-2) 是TRK 的抑制剂，信息来自专利 WO 2020038415 A1。

GNF-8625 monopyridin-N-piperazine hydrochloride

GNF-8625 monopyridin-N-piperazine hydrochloride Chemical Structure

CAS No. : 2412055-62-8

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

GNF-8625 monopyridin-N-piperazine hydrochloride (TRKi-2), a TRK inhibitor, which is from the patent WO 2020038415 A1[1].

分子量

479.98

Formula

C25H27ClFN7
CAS 号

2412055-62-8
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]. By Liu, Jing, et al. Preparation of tropomyosin receptor kinase degradation compounds and methods of use. WO 2020038415 A1.

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