FGFR2/3-IN-1

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FGFR2/3-IN-1

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CAS NO:

2640352-86-7

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。

生物活性

FGFR2/3-IN-1 is a potent and selectiveFGFR2andFGFR3(FGFR) inhibitor withIC₅₀s 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 inhibitsFGFR3V555L and V555M mutants withIC₅₀s 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].

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 (t_1/2= 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	C_max(nM)	2303
V_dss(L/kg)	1.6	AUC (nM·h)	5108
T_1/2(h)	1.7	F%	82

分子量

450.51

Formula

C₂₃H₂₂D₃N₇O₃

CAS 号

2640352-86-7

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.