BI-1622 is an orally active, potent and highly selective HER2 (ERBB2) inhibitor, with an IC 50 of 7 nM. BI-1622 shows greater than 25-fold selectivity over EGFR. BI-1622 shows high antitumor efficacy in vivo in xenograft mouse tumor models with engineered H2170 and PC9 cells and had a favorable drug metabolism and pharmacokinetics profile.
性状
Solid
IC50 & Target[1][2]
HER2 7 nM (IC50) ErbB4
体外研究(In Vitro)
BI-1622 (0-5 μM, 72?h or 96?h) inhibits the proliferation of HER2-dependent cell lines.BI-1622 induces a dose-dependent decrease in pHER2 and pERK levels in NCI-H2170 HER2YVMA and PC-9 HER2YVMA cells with an accompanying decrease in DUSP6 messenger RNA levels.BI-1622 displays good permeability and no PgP-mediated efflux liability. BI-1622 shows good in vitro clearance in mouse liver microsomes and mouse hepatocytes. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
BI-1622 (1 mg/kg, IV; 10 and 100 mg/kg, Orally; once) shows moderate clearance, a moderate volume of distribution, and good to moderate bioavailability.
BI-1622 (0-100?mg/kg, orally, twice daily) inhibits tumor growth and inhibits oncogenic signaling in vivo. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
参考文献
[1]. Lamarre L, et al. Discovery of potent and selective HER2 inhibitors with efficacy against HER2 exon 20 insertion-driven tumors, which preserve wild-type EGFR signaling. Nat Cancer. 2022 Jul;3(7):821-836.
溶解度数据
In Vitro: DMSO : 100 mg/mL (196.65 mM; Need ultrasonic)配制储备液