产品
编 号：F754590
分子式：C26H24N10O2
分子量：508.53
分子式：C26H24N10O2
分子量：508.53
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 2681392-19-6
产品详情
生物活性：
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.
体内研究：
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.BI-1622 (0-100?mg/kg, orally, twice daily) inhibits tumor growth and inhibits oncogenic signaling in vivo.Animal Model:Female NMRI-Foxn1nu mice (6-8 weeks old, 8-10 mice per cage, engrafted subcutaneously with PC-9 HER2YVMA, NCI-H2170 HER2YVMA or NCI-N87 cells)
Dosage:10, 30 and 100?mg/kg
Administration:orally, twice daily
Result:In the NCI-H2170 HER2YVMA mechanistic model, 100?mg/kg twice daily BI-1622 resulted in a delay in tumor growth (73% TGI). In the ST3107 HER2 exon 20 mutant model, both BI-4142 (100?mg/kg twice daily) resulted in tumor regressions.
Animal Model:NMRI Foxn1nu mice (n=3 per group)
Dosage:1 mg/kg (IV); 10 and 100 mg/kg (Orally)
Administration:IV, Orally; once (Pharmacokinetic Analysis)
Result:Showed moderate in vivo clearance (50% hepatic blood flow), a moderate volume of distribution, and good to moderate bioavailability of up to 68%.
体外研究：
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.
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.
体内研究：
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.BI-1622 (0-100?mg/kg, orally, twice daily) inhibits tumor growth and inhibits oncogenic signaling in vivo.Animal Model:Female NMRI-Foxn1nu mice (6-8 weeks old, 8-10 mice per cage, engrafted subcutaneously with PC-9 HER2YVMA, NCI-H2170 HER2YVMA or NCI-N87 cells)
Dosage:10, 30 and 100?mg/kg
Administration:orally, twice daily
Result:In the NCI-H2170 HER2YVMA mechanistic model, 100?mg/kg twice daily BI-1622 resulted in a delay in tumor growth (73% TGI). In the ST3107 HER2 exon 20 mutant model, both BI-4142 (100?mg/kg twice daily) resulted in tumor regressions.
Animal Model:NMRI Foxn1nu mice (n=3 per group)
Dosage:1 mg/kg (IV); 10 and 100 mg/kg (Orally)
Administration:IV, Orally; once (Pharmacokinetic Analysis)
Result:Showed moderate in vivo clearance (50% hepatic blood flow), a moderate volume of distribution, and good to moderate bioavailability of up to 68%.
体外研究：
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.
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