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

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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。

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

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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.

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