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EGFR-IN-1 hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
EGFR-IN-1 hydrochloride图片
CAS NO:2227455-78-7
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
EGFR-IN-1 hydrochloride 是一种口服活性不可逆的突变型选择性L858R/T790M EGFR抑制剂。与野生型 EGFR 相比,EGFR-IN-1 hydrochloride 对 Gefitinib 耐药的 EGFR L858R/T790M 有 100 倍的抑制作用。EGFR-IN-1 hydrochloride 对 H1975 细胞和 HCC827 细胞具有较强的抗增殖活性。具有抗肿瘤活性。
生物活性

EGFR-IN-1 hydrochloride is an orally active and irreversibleL858R/T790M mutant selectiveEGFRinhibitor. EGFR-IN-1 hydrochloride potently inhibits Gefitinib-resistantEGFRL858R, T790M with 100-fold selectivity over wild-typeEGFR. EGFR-IN-1 hydrochloride displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity[1].

IC50& Target[1]

EGFRL858R/T790M

 

体外研究
(In Vitro)

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[1].
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[1].

Cell Proliferation Assay[1]

Cell Line:NSCLC cell lines H1975 (T790M/L858R), HCC827 (?746-750)
Concentration:10 μM
Incubation Time:72 hours
Result:Inhibited H1975 nonsmall cell lung cancer cell line and the first line mutant HCC827 cell line with IC50s of 4 and 28 nM, respectively.
体内研究
(In Vivo)

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[1].
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[1].

Animal Model:Female athymic nude mice (H1975 Tumor Xenograft)[1]
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.
分子量

551.04

Formula

C28H31ClN6O4

CAS 号

2227455-78-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.