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Amuvatinib(MP-470,HPK 56)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Amuvatinib(MP-470,HPK 56)图片
CAS NO:850879-09-3
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
2mg电议
5mg电议
10mg电议
50mg电议

产品介绍
Amuvatinib (MP-470, HPK 56) (MP470) 是一种口服生物可利用的多靶点酪氨酸激酶抑制剂,对突变 c-Kit、PDGFRα、Flt3、c-Met 和 c-Ret 具有强效活性。 Amuvatinib (MP-470, HPK 56) (MP470) 也是一种 DNA 修复抑制剂,通过抑制 DNA 修复蛋白 RAD51,从而破坏 DNA 损伤修复。抗肿瘤活性。
Cas No.850879-09-3
别名N-(1,3-苯并二氧戊环-5-基甲基)-4-苯并呋喃并[3,2-D]嘧啶-4-基-1-哌嗪硫代甲酰胺,MP470,MP 470,HPK56
化学名N-(1,3-benzodioxol-5-ylmethyl)-4-([1]benzofuro[3,2-d]pyrimidin-4-yl)piperazine-1-carbothioamide
Canonical SMILESC1CN(CCN1C2=NC=NC3=C2OC4=CC=CC=C43)C(=S)NCC5=CC6=C(C=C5)OCO6
分子式C23H21N5O3S
分子量447.51
溶解度≥ 22.4 mg/mL in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Amuvatinib (also known as MP-470 or HPK 56), a synthetic carbothioamide, is a novel and potent tyrosine kinase inhibitor, which exertsin vitroandin vivoactivities against multiple targets including mutant KIT, platelet-derived growth factor receptor alpha (PDGFRα) and DNA repair. Μechanisticly, amuvatinib inhibits tyrosine kinase receptor KIT through occupying its ATP binding domain (IC50< 0.1 μM) and disrupts DNA repair through suppression of homologous recombination protein Rad51 as well as synergistic effects in combination with double stranded DNA damaging agents. Recent studies have shown that amuvatinib exhibits antitumor activity against human cancer cell lines, especially GIST-48 human cell line, in which it strongly inhibits proliferation (IC50= 0.20 μM).

Reference

[1].Raoul Tibes, Gil Fine, Gavin Choy, Sanjeev Redkar, Pietro Taverna, Aram Oganesian, Amarpao Sahai, Mohammad Azab and Anthony W. Tolcher. A phase I, first-in-human dose-escalation study of amuvatinib, a multi-targeted tyrosine kinase inhibitor, in patients with advanced solid tumors. Cancer Chemother Pharmacol (2013) 71: 463-471
[2].Gavin Choy, Rajashree Joshi-Hangal, Aram Oganesian, Gil Fine, Scott Rasmussen, Joanne Collier, James Kissling, Amarpal Sahai, Mohammad Azab and Sanjeev Redkar. Saftety, tolerability, and pharmacokinetics of amuvatinib from three phase 1 clinical studies in healthy volunteers. Cancer Chemother Pharmacol (2012) 70: 183-190