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CO-1686(AVL-301),EGFR抑制剂

规格或纯度: ≥99%
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C124905-5mg
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epidermal growth factor receptor Inhibitor
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基本描述

规格或纯度 ≥99%
英文名称 CO-1686 (AVL-301)
别名 AVL-301;CNX-419;N-[3-[[2-[[4-(4-Acetyl-1-piperazinyl)-2-methoxyphenyl]amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]phenyl]-2-propenamide
英文别名 AVL-301;CNX-419;N-[3-[[2-[[4-(4-Acetyl-1-piperazinyl)-2-methoxyphenyl]amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]phenyl]-2-propenamide
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.

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
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

关联配体

Ligand ID 7966
名称 rociletinib
别名 CO-1686
类别 Synthetic organic
学名 N-[3-[[2-[4-(4-acetylpiperazin-1-yl)-2-methoxyanilino]-5-(trifluoromethyl)pyrimidin-4-yl]amino]phenyl]prop-2-enamide
生物活性评价 The Ki value for activated EGFR carrying the L858R and T790M mutations is 21.5nM, which is >10 times the potency at the wild type receptor . In tumour xenograft and transgenic models rociletinib treatment induces tumour regression in EGFR-mutated NSCLC, with little effect against the wild type receptor expressing cells .
评价 Rociletinib is an orally bioavailable small molecule, irreversible inhibitor of epidermal growth factor receptor (EGFR) with potential antineoplastic activity . This compound was designed to selectively target both the initial activating EGFR mutations and the T790M resistance mutation which confers acquired tumour resistance to first-generation inhibitors such as and .

Third-generation mutant EGFR inhibitors like rociletinib are being developed to circumvent dose-limiting WT EGFR-driven toxicities such as gastrointestinal toxicity and rash. The progress being made in developing advanced generation EGFR inhibitors is discussed by Yu and Riely (2013) and Ou and Soo (2015) .

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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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