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CAS No.: 194423-06-8

CL-387785 Catalog No. CSN16222

Synonyms: EKI-785;WAY-EKI 785;CL 387,785

CL-387785 irreversibly inhibits EGFR with IC50 of 370 pM and shows inhibition of the functional effects of mutations T790M.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 EGFR

IC50:370±120pM
描述Tumors with certain mutations in the epidermal growth factor receptor (EGFR) family genes dramatically respond to EGFR inhibitors. CL-387785 is a specific, irreversible and covalent anilinoquinazoline EGFR inhibitor. It also specifically inhibited kinase activity of the protein (IC50 = 370+/-120 pM), blocked EGF-stimulated autophosphorylation of the receptor in cells (ic50 approximately 5 nM), inhibited cell proliferation (IC50 = 31-125 nM) primarily in a cytostatic manner in cell lines that overexpress EGFR or cerbB-2, and profoundly blocked the growth of a tumor that overexpresses EGFR in nude mice (when given orally at 80 mg/kg/day for 10 days, daily)^[3]. CL-387785 is able to overcome resistance caused by the T790M mutation on a functional level, correlating with effective inhibition of downstream signaling pathways^[4]. CL-387,785 and blebbistatin interacted in a synergistic fashion to suppress cell proliferation and induce apoptosis in H1975 cells. The combination of CL-387,785 and blebbistatin enhanced the down-regulation of cyclooxygenase-2 (COX-2), a transcriptional target of nuclear EGFR^[5]. reatment with CL-387,785, low-dose WZ4002, and high-dose WZ4002 caused mean decreases in (18)F-FLT uptake of 21%, 26%, and 36%, respectively^[6].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6231 mL
- 13.1156 mL
- 26.2312 mL
- 5 mM
- 0.5246 mL
- 2.6231 mL
- 5.2462 mL
- 10 mM
- 0.2623 mL
- 1.3116 mL
- 2.6231 mL

技术信息

CAS号

194423-06-8

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H13BrN4O

运输

蓝冰

分子量

381.23

别名

EKI-785;WAY-EKI 785;CL 387,785;EKB-785

溶解度

DMSO	61.0 mg/mL (160.0 mM) warming
Water	Insoluble
Ethanol	Insoluble

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