EGFR-IN-1 hydrochloride

Research use only, not for human use.

EGFR-IN-1 hydrochloride is an irreversible and specific inhibitor of L858R/T790M mutant EGFR, with 100-fold selectivity over wild-type EGFR.

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.

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.Cell Proliferation Assay 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.

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.

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Angiogenesis

EGFR

EGFR

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2227455-78-7

551.04

C28H31ClN6O4

>98% (HPLC)

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Cl.O=C(C=C)NC1=CC=CC(=C1)N2C(=O)C=C(C=3C=NC(=NC32)NC4=CC=C(OCCN(C)C)C=C4OC)C

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(-20℃)

With Ice Pack

≥ 2 years