CAS NO: | 2640352-86-7 |
包装 | 价格(元) |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
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] |
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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 (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].
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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. |