产品
编 号：F754593
分子式：C28H27N9O2
分子量：521.57
分子式：C28H27N9O2
分子量：521.57
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
结构图
CAS No: 2682003-36-5
产品详情
生物活性：
BI-4142 is a potent, highly selective and orally active HER2 inhibitor with an IC50 of 5 nM.
体内研究：
BI-4142 (0-100 mg/kg; p.o.; twice per day for 40 days) inhibits tumor growth and inhibits oncogenic signaling.Animal Model:NMRI-Foxn1nu mice, PC-9 HER2YVMA xenograft model
Dosage:3, 10, 30 and 100 mg/kg
Administration:Oral administration, twice per day for 40 days
Result:Resulted in tumor regressions in a dose-dependent manner (113%, 126%, 153% and 166% tumor growth inhibition at 3, 10, 30 and 100 mg/kg, respectively).
Animal Model:BomTac:NMRI Foxn1nu mice
Dosage:1 mg/kg or 10mg/kg and 100 mg/kg
Administration:IV for 1 mg/kg, PO for 10mg/kg and 100 mg/kg (Pharmacokinetic Analysis)
Result:In vivo mouse PK data for BI-4142CompoundDose iv/po(mg/kg) tmax(h) Cmax(nM) AUD(h?nM) Plasma CL(mL/min/kg) % F
i.v., 1mg/kgn/an/a3,2809.69n/a
BI-4142p.o., 10 mg/kg0.838,60023,200n/a71
p.o., 100 mg/kg0.6736,400196,000n/a60
体外研究：
BI-4142 shows inhibition with IC50 values of 10 nM, 18 nM, 270 nM and 2400 nM against HEK HER2YVMA, Ba/F3 HER2YVMA, HEK EGFRWT and Ba/F3 EGFRWT, 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.
BI-4142 is a potent, highly selective and orally active HER2 inhibitor with an IC50 of 5 nM.
体内研究：
BI-4142 (0-100 mg/kg; p.o.; twice per day for 40 days) inhibits tumor growth and inhibits oncogenic signaling.Animal Model:NMRI-Foxn1nu mice, PC-9 HER2YVMA xenograft model
Dosage:3, 10, 30 and 100 mg/kg
Administration:Oral administration, twice per day for 40 days
Result:Resulted in tumor regressions in a dose-dependent manner (113%, 126%, 153% and 166% tumor growth inhibition at 3, 10, 30 and 100 mg/kg, respectively).
Animal Model:BomTac:NMRI Foxn1nu mice
Dosage:1 mg/kg or 10mg/kg and 100 mg/kg
Administration:IV for 1 mg/kg, PO for 10mg/kg and 100 mg/kg (Pharmacokinetic Analysis)
Result:In vivo mouse PK data for BI-4142CompoundDose iv/po(mg/kg) tmax(h) Cmax(nM) AUD(h?nM) Plasma CL(mL/min/kg) % F
i.v., 1mg/kgn/an/a3,2809.69n/a
BI-4142p.o., 10 mg/kg0.838,60023,200n/a71
p.o., 100 mg/kg0.6736,400196,000n/a60
体外研究：
BI-4142 shows inhibition with IC50 values of 10 nM, 18 nM, 270 nM and 2400 nM against HEK HER2YVMA, Ba/F3 HER2YVMA, HEK EGFRWT and Ba/F3 EGFRWT, 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.
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备