BI-4142 is a potent, highly selective and orally active HER2 inhibitor with an IC 50 of 5 nM.
性状
Solid
IC50 & Target[1][2]
HER2 5 nM (IC50)
体外研究(In Vitro)
BI-4142 shows inhibition with IC50 values of 10 nM, 18 nM, 270 nM and 2400 nM against HEK HER2, Ba/F3 HER2, HEK EGFR and Ba/F3 EGFR, respectively.BI-4142 (1 nM-5 μM, 72?h or 96?h) shows antiproliferative activity against tumor cells.BI-4142 displays good permeability and no PgP-mediated efflux liability in the CaCo-2 assay.BI-4142 inhibits HER2-dependent cell lines and inhibits downstream signaling. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
BI-4142 (0-100 mg/kg; p.o.; twice per day for 40 days) inhibits tumor growth and inhibits oncogenic signaling. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: NMRI-Foxn1nu mice, PC-9
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]. Wilding B, 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 (191.73 mM; Need ultrasonic)配制储备液
[1]. Wilding B, 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.