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| 品牌 | absin | CAS | 194423-06-8 |
|---|---|---|---|
| 分子式 | C18H13BrN4O | 纯度 | 98% |
| 分子量 | 381.23 | 货号 | abs47027963 |
| 规格 | 10mg | 供货周期 | 现货 |
| 主要用途 | able to overcome resistance | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
CL-387785 194423-06-8
| 产品描述 | |
| 描述 | CL-387785(EKI785; WAY-EKI 785) is an irreversible inhibitor of EGFR with IC50 of 370+/-120 pM; is able to overcome resistance caused by the T790M mutation on a functional level. |
| 纯度 | 98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | EKI-785； WAY-EKI 785 |
| 外观 | Off-white to yellow solid |
| 可溶性/溶解性 | DMSO : 13.67 mg/mL (35.86 mM) |
| 生物活性 | |
| 靶点 | EGFR |
| In vitro(体外研究) | CL-387785 blocks EGF-stimulated autoposphorylation of the receptor in cells (IC50, 5 nM), In cell lines that overexpress EGF-R or c-erbB-2, CL-387785 inhibits cell proliferation (IC50, 31 nM) primarily in a cytostatic manner. |
| In vivo(体内研究) | In nude mice overexpressed EGF-R, CL-387785 (80 mg/kg/day, p.o.) profoundly blocks the growth of tumor. In murine models of autosomal recessive polycystic kidney disease (ARPKD), treatment of Balb/c-bpk/bpk (BPK) mice with CL-387785 (90 mg/kg, i.p.) results in a marked reduction of collecting tubule cystic lesions, improved renal function, decreased biliary epithelial abnormalities, and prolonged life span. Doses of CL-387785 as low as 25 mg/kg reduces the growth of HCA-7-induced xenograft tumor, and a dose of 100 mg/kg prevents tumor growth entirely. Dose of 50 mg/kg CL-387785 is effective at reducing the growth of HCT-116-induced xenograft tumor. |
| 研究领域 | |
| 研究领域 | CancerGrowth factorsEGF CancerOncoproteins/suppressorsOncoproteinsGrowth factor receptors CancerSignal transductionProtein phosphorylationTyrosine kinasesReceptor tyrosine kinases CancerTumor biomarkersReceptors Cell CycleCell differentiation MicrobiologyOrganismVirusDNA VirusssRNA positive strand virusSARS Coronavirus NeuroscienceDevelopment NeuroscienceProcesses Signal TransductionGrowth Factors/HormonesEGF Signal TransductionProtein PhosphorylationTyrosine KinasesReceptor Tyrosine Kinases Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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