化合物Rociletinib T2369

Product Introduction
Bioactivity


英文名: Rociletinib

描述: Rociletinib (CNX-419) 是一种可口服的EGFR 抑制剂，能够抑制 EGFRL858R/T790M 和 EGFRWT 的活性，IC50值分别为 21.5 nM 和 303.3 nM。

细胞实验: Cells are seeded at 3,000 cells per well in growth media supplemented with 5% FBS, 2 mmol/L, L-glutamine, and 1% penicillin–streptomycin, allowed to adhere overnight, and treated with a dilution series of test compounds for 72 hours. Cell viability is determined by CellTiter-Glo, and results are represented as background-subtracted relative light units normalized to a dimethyl sulfoxide (DMSO)–treated control. Growth inhibition (GI 50) values are determined by GraphPad Prism 5.04. MK-2206 and XL-880 compounds are obtained from Selleck Chemical. CI data are generated using CalcuSyn.(Only for Reference)

激酶实验: Inhibition Kinetics Studies: Recombinant human wild-type and T790M/L858R double mutant EGFR, both Nterminal GST-tagged, are used in the assay. The Omnia continuous read assay is performed as described by the vendor.

体外活性: CO-1686在所有EGFR突变体模型以及表达EGFRL858R-和EGFRL858R/T790M的转基因小鼠中引起显著的剂量依赖性肿瘤生长抑制.

体内活性: CO-1686选择性抑制NSCLC细胞表达的突变体EGFR的生长,GI50范围为7 到 32 nM,并诱导细胞凋亡。耐CO-1686的NSCLC细胞系表现出上皮 - 间充质转变的迹象并且对AKT抑制剂的敏感性增加。CO-1686在表达突变型EGFR的细胞中抑制p-EGFR,其IC50范围为62至187 nM,同时在三种WT EGFR表达细胞中抑制EGFR磷酸化,IC50> 2,000 nM。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 93 mg/mL (167.4 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)


关键字: CNX 419 | AVL 301 | HER1 | Inhibitor | inhibit | CO 1686 | EGFR | ErbB-1 | Rociletinib | AVL301 | CNX419 | Epidermal growth factor receptor | CO1686

相关产品: Methyl 2,5-dihydroxycinnamate | AG-1478 | EGFR/CSC-IN-1 | OK2 | EGFR-IN-11 | Brigatinib | Cisapride hydrate | EBE-A22 | Dacomitinib hydrate | Lidocaine Hydrochloride hydrate

相关库: Drug Repurposing Compound Library | FDA-Approved Kinase Inhibitor Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Inhibitor Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Highly Selective Inhibitor Library | Anti-Cancer Active Compound Library | Anti-Cancer Approved Drug Library

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