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账号

CO-1686(AVL-301),EGFR抑制剂, 表皮生长因子受体 erbB1 抑制剂

规格或纯度: ≥99%
有货

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货号 (SKU) 包装规格 是否现货 价格 数量
C124905-5mg
 5mg 现货 Stock Image
C124905-10mg
 10mg 现货 Stock Image
C124905-50mg
 50mg 现货 Stock Image
C124905-100mg
 100mg 现货 Stock Image
大包装询价 添加到收藏夹 比较  SDS中文版  DATASHEET
main product photo

基本描述

英文别名 Rociletinib|1374640-70-6|CO-1686|AVL-301|CNX-419|N-(3-((2-((4-(4-acetylpiperazin-1-yl)-2-methoxyphenyl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)phenyl)acrylamide|Rociletinib (CO-1686)|CO-1686 (AVL-301)|CS-1631|N-(3-((2-((4-(4-Acetylpiperazin-1-yl)-2
规格或纯度 ≥99%
英文名称 CO-1686 (AVL-301)
生化机理

Description:
IC50 Value: 21.5±1.7 nM (EGFRL858R/T790M); 303.3 ± 26.7 nM (EGFRWT) [1]
CO-1686 is a novel, irreversible and orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M while exhibiting minimal activity towards the wild-type (WT) receptor.
in vitro: CO-1686 is a potent inhibitor of EGFR L858R/T790M kinase (kinact/Ki = (2.41 ± 0.30) x 105 M-1s-1) and is approximately 22-fold selective over WT EGFR (kinactt/Ki = (1.12 ± 0.14) x 104 M-1s-1). CO-1686 potently inhibited proliferation in the mutant-EGFR NSCLC cellswith GI50 values ranging from 7 - 32 nM. In comparison, the GI50 value for A431 cells, an epidermoid cell line that is driven by amplified WT EGFR(19), was 547 nM. Two cell lines
expressing WT EGFR in the presence of an N- or KRAS mutation (NCI-H1299 and NCI-H358,
respectively) were inhibited by CO-1686 at a concentration of 4275 and 1806 nM, respectively [1].

储存温度 -20°C储存
运输条件 超低温冰袋运输
备注 50mg、10mg卖完停产，不再备货
产品介绍

CO-1686 (AVL-301)是一种不可逆的，突变选择性的EGFR抑制剂，作用于EGFRL858R/T790M和EGFRWT， Ki分别为21.5 nM和303.3 nM。Phase 2。

CO-1686 is an irreversible, mutant-selective EGFR inhibitor with Ki of 21.5 nM and 303.3 nM for EGFRL858R/T790M and EGFRWT, respectively. Phase 2.

产品属性

ALogP 4

名称和标识符

IUPAC Name N-[3-[[2-[4-(4-acetylpiperazin-1-yl)-2-methoxyanilino]-5-(trifluoromethyl)pyrimidin-4-yl]amino]phenyl]prop-2-enamide
INCHI InChI=1S/C27H28F3N7O3/c1-4-24(39)32-18-6-5-7-19(14-18)33-25-21(27(28,29)30)16-31-26(35-25)34-22-9-8-20(15-23(22)40-3)37-12-10-36(11-13-37)17(2)38/h4-9,14-16H,1,10-13H2,2-3H3,(H,32,39)(H2,31,33,34,35)
InChi Key HUFOZJXAKZVRNJ-UHFFFAOYSA-N
Canonical SMILES CC(=O)N1CCN(CC1)C2=CC(=C(C=C2)NC3=NC=C(C(=N3)NC4=CC(=CC=C4)NC(=O)C=C)C(F)(F)F)OC
Isomeric SMILES CC(=O)N1CCN(CC1)C2=CC(=C(C=C2)NC3=NC=C(C(=N3)NC4=CC(=CC=C4)NC(=O)C=C)C(F)(F)F)OC
PubChem CID 57335384
分子量 555.55

化学和物理性质

溶解性 DMSO 100 mg/mL Water <1 mg/mL Ethanol <1 mg/mL

质检证书(COA)

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参考文献

1. Yu HA, Riely GJ.  (2013)  Second-generation epidermal growth factor receptor tyrosine kinase inhibitors in lung cancers..  J Natl Compr Canc Netw,  11  (2):  (161-9).  [PMID:23411383]
2. Walter AO, Sjin RT, Haringsma HJ, Ohashi K, Sun J, Lee K, Dubrovskiy A, Labenski M, Zhu Z, Wang Z et al..  (2013)  Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC..  Cancer Discov,  3  (12):  (1404-15).  [PMID:24065731]
3. Ou SH, Soo RA.  (2015)  Dacomitinib in lung cancer: a "lost generation" EGFR tyrosine-kinase inhibitor from a bygone era?.  Drug Des Devel Ther,  9  (13):  (5641-53).  [PMID:26508839]
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