EGFR-IN-1 hydrochloride

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EGFR-IN-1 hydrochloride 

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。

EGFR-IN-1 hydrochloride

EGFR-IN-1 hydrochloride Chemical Structure

CAS No. : 2227455-78-7

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EGFR-IN-1 hydrochloride 的其他形式现货产品:

EGFR-IN-1 TFA

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[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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

参考文献
  • [1]. Wurz RP, et al. Oxopyrido[2,3-d]pyrimidines as Covalent L858R/T790M Mutant Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors. ACS Med Chem Lett. 2015 Jul 27;6(9):987-92.

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