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Olmutinib(HM61713,BI 1482694)
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。
Olmutinib(HM61713,BI 1482694)图片
CAS NO:1353550-13-6
包装与价格:
包装价格(元)
5mg电议
25mg电议
100mg电议

产品介绍
Olmutinib (HM61713, BI 1482694) (HM61713; BI-1482694) 是一种具有口服活性且不可逆的第三种 EGFR 酪氨酸激酶抑制剂,可与激酶结构域附近的半胱氨酸残基结合。 Olmutinib (HM61713, BI 1482694) 用于非小细胞肺癌。
Cas No.1353550-13-6
别名奥莫替尼
化学名N-(3-((2-((4-(4-methylpiperazin-1-yl)phenyl)amino)thieno[3,2-d]pyrimidin-4-yl)oxy)phenyl)acrylamide
Canonical SMILESC=CC(NC1=CC=CC(OC2=C3C(C=CS3)=NC(NC4=CC=C(N5CCN(C)CC5)C=C4)=N2)=C1)=O
分子式C26H26N6O2S
分子量486.59
溶解度DMSO: 44 mg/mL
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

GI50: 9.2 and 10 nM for H1975 (L858-T790M) and HCC827 (exon 19 del.), respectively.

Olmutinib (HM61713, BI 1482694) is an EGFR mutant-specific inhibitor.

The tyrosine kinase inhibitors (TKI) against epidermal growth factor receptor (EGFR) are widely used in patients with non-small cell lung cancer (NSCLC). However, EGFR T790M mutation leads to resistance to most clinically available EGFR TKIs. Third-generation EGFR TKIs against the T790M mutation have been in active clinical development.

In vitro: Olmutinib has been identified as an irreversible kinase inhibitor and could covalently bind to a cysteine residue near the kinase domain of mutant EGFR. Olmutinib had a half-life of over 24h for EGFR inhibition. Olmutinib was able to cause potent inhibition in cell lines H1975 (L858R and T790M) and HCC827 (exon 19 deletion). Olmutinib showed a low potency for NSCLC cell line H358 with wild-type EGFR [1].

In vivo: The previous in vivo studies of xenograft models with grafts of H1975 and HCC827 showed that olmutinib was active against the tumors without dasplaying any side effects [1].

Clinical trial: In the ongoing phase I/II study of olmutinib in patients with advanced NSCLC who had failed previous EGFR TKIs, EGFR mutated patients received olmutinib doses ranging from 75 to 1200 mg/day. In the phase II expansion part of the study, 800 mg QD was the dose given to patients. The ORR was 58.8% in the 34 patients who received olmutinib with a dose more than 650 mg. Moreover, 10 patients had unconfirmed partial responses, and 13 showed disease stabilization. DLTs included GI symptoms and elevation of alanine aminotransferase, aspartate aminotransferase, amylase, and lipase. Thus, olmutinib could represent another promising drug for patients with T790M-positive NSCLC [1].

Reference:
[1] Wang S, Cang S, Liu D.  Third-generation inhibitors targeting EGFR T790M mutation in advanced non-small cell lung cancer. J Hematol Oncol. 2016 Apr 12;9:34.