2. Protein Tyrosine Kinase/RTK
  3. FGFR
  4. FGFR2/3-IN-1

FGFR2/3-IN-1 是一种有效的选择性 FGFR2 和 FGFR3 (FGFR) 抑制剂，IC50 分别为 1 nM 和 0.5 nM。FGFR2/3-IN-1 的选择性比 FGFR1/FGFR4 和其他激酶组高 40 倍以上。FGFR2/3-IN-1 也抑制 FGFR3 V555L 和 V555M 突变体，IC50 分别为 2.7 nM 和 6.1 nM。

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FGFR2/3-IN-1 Chemical Structure

FGFR2/3-IN-1 Chemical Structure

CAS No. : 2640352-86-7

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FGFR2/3-IN-1 相关抗体

Top Publications Citing Use of Products

查看 FGFR 亚型特异性产品:

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FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FGFR2/3-IN-1 is a potent and selective FGFR2 and FGFR3 (FGFR) inhibitor with IC50s of 1 nM and 0.5 nM, respectively. FGFR2/3-IN-1 displays >40-fold selectivity over FGFR1/FGFR4 and other kinome. FGFR2/3-IN-1 also inhibits FGFR3 V555L and V555M mutants with IC50s of 2.7 nM and 6.1 nM, respectively[1].

IC50 & Target[1]

FGFR2

1 nM (IC50)

FGFR3

0.5 nM (IC50)

FGFR3 V555L

2.7 nM (IC50)

FGFR3 V555M

6.1 nM (IC50)

FGFR1

21 nM (IC50)

FGFR4

145 nM (IC50)

体外研究
(In Vitro)

FGFR2/3-IN-1 (compound 29) has a clean CYP profile (CYP3A4 IC50 >25 μM). FGFR2/3-IN-1 displays excellent potency (whole blood, IC50 = 177 nM) in a whole blood (WB) assay[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

FGFR2/3-IN-1 相关抗体:
体内研究
(In Vivo)

FGFR2/3-IN-1 (compound 29) is advanced into rat pharmacokinetics studies. Clearance in the i.v. arm is low (hepatic blood flow (HBF) = 35%), with a moderate half-life (t1/2 = 1.7 h). In the p.o. dose, FGFR2/3-IN-1 demonstrates good exposure (AUC = 5108 nM·h) and high oral bioavailability (F% = 82)[2].

rat i.v. rat p.o.
dose (mg/kg) 1.0 dose (mg/kg) 3.0
HBF% 35 Cmax (nM) 2303
Vdss (L/kg) 1.6 AUC (nM·h) 5108
T1/2 (h) 1.7 F% 82

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

450.51

Formula

C23H22D3N7O3
CAS 号
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.
纯度 & 产品资料
参考文献

FGFR2/3-IN-1 相关分类

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  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

FGFR2/3-IN-12640352-86-7FGFRFibroblast growth factor receptorFGFR2FGFR3FGFR3 V555LFGFR3 V555Moral bioavailabilityInhibitorinhibitorinhibit

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