货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
V58066-1ml	10mM in DMSO	￥3380.00 V58066-1ml ￥3380.00 3-5天	0 货期：3-5天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

V58066-1ml

10mM in DMSO

￥3380.00

货期：3-5天

产品描述：

BI-1622 is an orally active, potent and highly selective HER2 (ERBB2) inhibitor, with an IC50 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 agent metabolism and pharmacokinetics profile[1].

靶点：

HER2:7 nM (IC50);ErbB4;EGFR;CDK11B;JAK3

体外研究：

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[1].
BI-1622 (0-100 mg/kg, orally, twice daily) inhibits tumor growth and inhibits oncogenic signaling in vivo[1].

体内研究：

BI-1622 (0-5 µM, 72 h or 96 h) inhibits the proliferation of HER2-dependent cell lines[1].
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[1].
BI-1622 displays good permeability and no PgP-mediated efflux liability[1].
BI-1622 shows good in vitro clearance in mouse liver microsomes and mouse hepatocytes[1].

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.

保存条件：

-80°C 6个月; -20°C 1个月,避光

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.966 ml	9.832 ml	19.665 ml
5 mM	0.393 ml	1.966 ml	3.933 ml
10 mM	0.197 ml	0.983 ml	1.966 ml
50 mM	0.039 ml	0.197 ml	0.393 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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