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CAS No.: 366017-09-6

Mubritinib/木利替尼 Catalog No. CSN11482

Synonyms: TAK-165;木利替尼

Mubritinib is a potent and selective inhibitor of HER2/ErbB2 with IC50 of 6 nM with no inhibition on EGFR, FGFR, PDGFR, and etc.

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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 HER2

IC50:6nM
描述Human epidermal growth factor receptor (EGFR; HER1,erbB1), human epidermal growth factor r eceptor 2 (HER2; erbB2), HER3 (erbB3) and HER4 (erbB4) are members of the ErbB family of transmembrane receptor tyrosine kinases. Among them, HER2 is a validated and high-value target. Overexpression of HER2 occurs in gastric, colorectal, NSCLC, breast and ovarian cancers. Mubritinib is a highly selective Her2 inhibitor with IC50 value of 6nM (measured by tyrosine-kinase activity), with almost no inhibition of other related target including EGFR, FGFR, PDGFR, Jak1, Src and Blk (all IC50 values>25000nM). Treatment with mubritinib at concentration>0.1μM for 2h caused significant decrease of autophosphorylation of Her2, as well as phosphorylation level of the key signal transduction mediator AKT and MAPK, in BT474 cells overexpressing HER2. The sensitivity of cell to Mubritinib depended on HER2 levels, as BT474 cells over-expressing HER2 strongly with highly sensitivity to Mubritinib (IC50=0.005µM), PC-3 cells expressing HER2 very weakly with less sensitive to Mubritinib (IC50=4.62µM), and HT1376 and ACHN cells over-expressed EGFR with much higher IC50 values (>25μM). Oral administration of 20mg/kg Mubritinib twice daily for 2 weeks significantly inhibited tumor growth in UMUC-3 bladder cancer model, as well as LN-REC4 prostate cancer model at dose of 10 or 20mg/kg^[1].
动物研究
剂量
Mice^[1] (p.o.): 10 m/kg, 20 mg/kg

给药途径
p.o.
临床研究

动物研究
剂量	Mice^[1] (p.o.): 10 m/kg, 20 mg/kg
给药途径	p.o.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00034281	Breast Neoplasm ... more >> Pancreatic Neoplasm Lung Neoplasm Ovarian Neoplasm Renal Neoplasm Collapse <<	Phase 1	Completed	-	United States, Arizona ... more >> Arizona Cancer Center Scottsdale, Arizona, United States, 85258 United States, Texas The Institute for Drug Development San Antonio, Texas, United States, 78229 Brooke Army Medical Center/Drug Development Unit San Antonio, Texas, United States, 78234 South Texas VA, Audie Murphy Division San Antonio, Texas, United States, 78284 Collapse <<

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
- 2.1346 mL
- 10.6730 mL
- 21.3460 mL
- 5 mM
- 0.4269 mL
- 2.1346 mL
- 4.2692 mL
- 10 mM
- 0.2135 mL
- 1.0673 mL
- 2.1346 mL

技术信息

CAS号

366017-09-6

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H23F3N4O2

运输

蓝冰

分子量

468.47

别名

TAK-165;木利替尼

溶解度

DMSO	100.0 mg/mL (213.5 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+40% PEG300+water	2 mg/mL	clear
PO	0.5% CMC-Na	18 mg/mL	suspension

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