BI-1622,2681392-19-6

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BI-1622

CAS No. : 2681392-19-6

MCE 国际站：BI-1622

产品活性：BI-1622 是一种口服有效的和高选择性 HER2 (ERBB2) 抑制剂，IC₅₀ 为 7 nM。BI-1622对 EGFR 的选择性大于 25 倍。BI-1622 在转染 H2170 和 PC9 细胞的移植瘤小鼠模型中表现出较高的体内的抗肿瘤效果，具有良好的活性分子代谢和药代动力学特性。

研究领域：JAK/STAT Signaling  |  Protein Tyrosine Kinase/RTK  |  PI3K/Akt/mTOR  |  Cell Cycle/DNA Damage  |  MAPK/ERK Pathway  |  Epigenetics  |  Stem Cell/Wnt

作用靶点：EGFR  |  Itk  |  PI4K  |  Btk  |  CDK  |  Raf  |  JAK

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.

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.

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