产品
编 号：F619107
分子式：C28H31ClN6O4
分子量：551.04
分子式：C28H31ClN6O4
分子量：551.04
产品类型
规格
价格
是否有货
结构图
CAS No: 2227455-78-7
产品详情
生物活性：
EGFR-IN-1 hydrochloride is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 hydrochloride potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 hydrochloride displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity.
体内研究：
EGFR-IN-1 hydrochloride (30 mg/kg; p.o.; daily for 2 weeks) displays significant tumor growth inhibition with no observed loss in body weight.EGFR-IN-1 hydrochloride evaluates in a time course PD experiment upon oral dosing at 30 mg/kg.EGFR-IN-1 shows a >50% inhibition of phosphorylation of EGFR for >12 h. EGFR-IN-1 reaches maximal concentration of 0.10 μM at 2 h and systemic exposure (AUC0-inf.) is 0.33 μM. h.Animal Model:Female athymic nude mice (H1975 Tumor Xenograft)
Dosage:30 mg/kg
Administration:p.o.; daily for 2 weeks
Result:Led to significant tumor growth inhibition with no observed loss in body weight.
体外研究：
EGFR-IN-1 hydrochloride (compound 24) (10 μM; 72 hours) displays strong antiproliferative activity against the H1975 and HCC827 cells with IC50s of 4 and 28 nM, respectively.EGFR-IN-1 hydrochloride inhibits p-EGFR in H1975 and HCC827 cells with IC50s of 4 and 9 nM, respectively. EGFR-IN-1 highly selective against a panel of 100 kinases.
EGFR-IN-1 hydrochloride is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 hydrochloride potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 hydrochloride displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity.
体内研究：
EGFR-IN-1 hydrochloride (30 mg/kg; p.o.; daily for 2 weeks) displays significant tumor growth inhibition with no observed loss in body weight.EGFR-IN-1 hydrochloride evaluates in a time course PD experiment upon oral dosing at 30 mg/kg.EGFR-IN-1 shows a >50% inhibition of phosphorylation of EGFR for >12 h. EGFR-IN-1 reaches maximal concentration of 0.10 μM at 2 h and systemic exposure (AUC0-inf.) is 0.33 μM. h.Animal Model:Female athymic nude mice (H1975 Tumor Xenograft)
Dosage:30 mg/kg
Administration:p.o.; daily for 2 weeks
Result:Led to significant tumor growth inhibition with no observed loss in body weight.
体外研究：
EGFR-IN-1 hydrochloride (compound 24) (10 μM; 72 hours) displays strong antiproliferative activity against the H1975 and HCC827 cells with IC50s of 4 and 28 nM, respectively.EGFR-IN-1 hydrochloride inhibits p-EGFR in H1975 and HCC827 cells with IC50s of 4 and 9 nM, respectively. EGFR-IN-1 highly selective against a panel of 100 kinases.
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备