标签归档：fiin

FIIN-1(Synonyms: FGFR irreversible inhibitor-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。

FIIN-1 (Synonyms: FGFR irreversible inhibitor-1)

FIIN-1 是一种有效的，不可逆的选择性 FGFR 抑制剂。FIIN-1 与 FGFR1/2/3/4 和 Flt1/4 结合，Kd 分别为 2.8/6.9/5.4/120 nM 和 32/120 nM。FIIN-1 抑制 FGFR1/2/3/4 的 IC50 分别是 9.2，6.2，11.9 和 189 nM。

FIIN-1(Synonyms: FGFR irreversible inhibitor-1)

FIIN-1 Chemical Structure

CAS No. : 1256152-35-8

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

FIIN-1 is a potent, irreversible, selective FGFR inhibitor. FIIN-1 binds to FGFR1/2/3/4 and Flt1/4 with Kds of 2.8/6.9/5.4/120 nM and 32/120 nM respectively. The biochemical IC50s of FIIN-1 are 9.2, 6.2, 11.9, and 189 nM against FGFR1/2/3/4, respectively[1].

IC50 & Target[1]

FGFR1

2.8 nM (Kd)

FGFR2

6.9 nM (Kd)

FGFR3

5.4 nM (Kd)

FGFR4

120 nM (Kd)

FGFR1

9.2 nM (IC50)

FGFR2

6.2 nM (IC50)

FGFR3

11.9 nM (IC50)

FGFR4

189 nM (IC50)

体外研究
(In Vitro)

FIIN-1 binds to BLK, ERK5, KIT, MET, PDGFRB and VEGFR2 with Kds of 65 nM, 160, 420, 1000, 480 and 210 nM, respectively. The IC50s for Blk and Flt1 are 381 nM and 661 nM respectively[1].
FIIN-1 (14 nM-46 μM; 72 hours) inhibits proliferation of FGF signaling-sensitive cancer cell lines[1].
FIIN-1 (20 nM) inhibits iFGFR1 autophosphorylation and its downstream Erk1/2 almost completely.

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: Stomach KATO III, SNU-16 and FU97 cells; Bladder RT4 cells; Kidney G-401 and G-402 cells; Lung SBC-3 and H520 cells; Pancreas A2.1 cells; Ovary A2780 and PA-1 cells; Bone RD-ES cells
Concentration:
Incubation Time: 72 hours
Result: The EC50 of 70 nM for Bladder RT4 cell.
The EC50 of 230 nM for Pancreas A2.1 cell.
The EC50 of 2.3 μM for Bone RD-ES cell.
EC50s of 0.22 and 4.6 μM for Ovary A2780 and PA-1 cells, respectively.
EC50s of 0.08 and 4.5 μM for Lung SBC-3 and H520 cells, respectively.
EC50s of 0.14 and 1.65 μM for Kidney G-401 and G-402 cells, respectively.
EC50s of 0.014, 0.03 and 0.65 μM for Stomach KATO III, SNU-16, FU97 cells, respectively.

Western Blot Analysis[1]

Cell Line: Serum-starved MCF10A cells that stably express iFGFR1
Concentration: 20 nM
Incubation Time: 30 minutes
Result: Blocked activation of iFGFR1 and phosphorylation of downstream effectors Erk1/2.

分子量

656.60

Formula

C32H39Cl2N7O4
CAS 号

1256152-35-8
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]. Wenjun Zhou, et al. A structure-guided approach to creating covalent FGFR inhibitors. Chem Biol. 2010 Mar 26;17(3):285-95.

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

FIIN-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。

FIIN-2  纯度: 99.63%

FIIN-2 是 FGFR 的不可逆抑制剂，对FGFR1，FGFR2，FGFR3和FGFR4的IC50 值分别为3.1，4.3，27和45 nM。

FIIN-2

FIIN-2 Chemical Structure

CAS No. : 1633044-56-0

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1424 In-stock
5 mg ￥1020 In-stock
10 mg ￥1600 In-stock
25 mg ￥3200 In-stock
50 mg ￥5500 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

FIIN-2 相关产品

•相关化合物库:

  • Covalent Screening Library Plus
  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Covalent Screening Library
  • Reprogramming Compound Library
  • Anti-Lung Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Targeted Diversity Library
  • Anti-Liver Cancer Compound Library

生物活性

FIIN-2 is an irreversible inhibitor of FGFR with an IC50 of 3.1, 4.3, 27, and 45 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively.

IC50 & Target[1]

FGFR1

3.1 nM (IC50)

FGFR2

4.3 nM (IC50)

FGFR3

27 nM (IC50)

FGFR4

45 nM (IC50)

体外研究
(In Vitro)

FIIN-2 potently inhibits WT FGFRs (EC50s in the 1- to 93-nM range) and the gatekeeper mutant of FGFR2 (EC50 of 58 nM). FIIN-2 also moderately inhibits EGFR, with an IC50 of 204 nM. FIIN-2 inhibits proliferation of FGFR1-4 Ba/F3 cells with EC50s in the single- to double-digit nanomolar range and are especially potent against FGFR2, with EC50s in the 1-nM range. FIIN-2 shows good potency against gatekeeper mutant V564F[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)

Treatment of fish in the embryonic state with either FIIN-2 causes defects to the posterior mesoderm similar to the phenotypes reported following genetic knockdown of FGFR or treatment with other reported FGFR inhibitors. FIIN-2 causes mild or severe phenotypes to the tail morphogenesis in all treated embryonic zebrafish[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

634.73

Formula

C35H38N8O4
CAS 号

1633044-56-0
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 : ≥ 30 mg/mL (47.26 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 1.5755 mL 7.8774 mL 15.7547 mL
5 mM 0.3151 mL 1.5755 mL 3.1509 mL
10 mM 0.1575 mL 0.7877 mL 1.5755 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 (3.94 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.94 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 (3.94 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.94 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 (3.94 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.94 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]. Tan L, et al. Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors. Proc Natl Acad Sci U S A. 2014 Nov 11;111(45):E4869-4877.
Cell Assay
[1]

TEL-FGFR2–transformed Ba/F3 cells are seeded in a 96-well plate and are treated with each concentration of the compounds. After 72 h the cells are assessed by MTS tetrazolium assay[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]. Tan L, et al. Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors. Proc Natl Acad Sci U S A. 2014 Nov 11;111(45):E4869-4877.

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

FIIN-3

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。

FIIN-3  纯度: 98.13%

FIIN-3 是 FGFR 的不可逆抑制剂，对FGFR1，FGFR2，FGFR3和FGFR4的IC50 值分别为13.1，21，31.4和35.3 nM。

FIIN-3

FIIN-3 Chemical Structure

CAS No. : 1637735-84-2

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3347 In-stock
1 mg ￥900 In-stock
5 mg ￥2200 In-stock
10 mg ￥3500 In-stock
50 mg ￥12000 In-stock
100 mg 询价

* Please select Quantity before adding items.

FIIN-3 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
  • Reprogramming 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

FIIN-3 is an irreversible inhibitor of FGFR with an IC50 of 13.1, 21, 31.4, and 35.3 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively.

IC50 & Target

FGFR1

13.1 nM (IC50)

FGFR2

21 nM (IC50)

FGFR3

31.4 nM (IC50)

FGFR4

35.3 nM (IC50)

体外研究
(In Vitro)

FIIN-3 potently inhibits both WT FGFRs (EC50 in the 1- to 41-nM range) and the gatekeeper mutant of FGFR2 (EC50 of 64 nM). FIIN-3 also strongly inhibits EGFR, with an EC50 of 43 nM. FIIN-3 shows good potency against gatekeeper mutant V564F; FIIN-3 also is potent against the gatekeeper-plus-1 mutant E565K; FIIN-3 also displays antiproliferative activity (with an EC50 of 135 nM) against Ba/F3 cells transformed by the EGFR vIII fusion protein, which has a WT EGFR kinase domain. FIIN-3 shows even better activity against EGFR mutant L858R (EC50 of 17 nM) and moderate activity, displaying an EC50 of 231 nM, against the EGFR mutant L858R/T790M mutant. In WT FGFR2 Ba/F3 cells, FIIN-3 completely inhibits the FGFR2 autophosphorylation on Tyr656/657 at concentrations as low as 3 nM. In FGFR2 V564M Ba/F3 cells, FIIN-3 is capable of inhibiting the FGFR2 mutant V564M autophosphorylation with partial inhibition at 100 nM and complete inhibition observed at 300 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.
分子量

691.61

Formula

C34H36Cl2N8O4
CAS 号

1637735-84-2
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 : 10 mg/mL (14.46 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.4459 mL 7.2295 mL 14.4590 mL
5 mM 0.2892 mL 1.4459 mL 2.8918 mL
10 mM 0.1446 mL 0.7230 mL 1.4459 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 (3.61 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.61 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 (3.61 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (3.61 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 (3.61 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.61 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]. Tan L et al. Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors. Proc Natl Acad Sci U S A, 2014 Nov 11, 111(45):E4869-77
Cell Assay
[1]

TEL-FGFR2–transformed Ba/F3 cells are seeded in a 96-well plate and are treated with each concentration of FIIN-3. After 72 h the cells are assessed by MTS tetrazolium assay[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]. Tan L et al. Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors. Proc Natl Acad Sci U S A, 2014 Nov 11, 111(45):E4869-77

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