Amuvatinib (MP-470, HPK 56)

A multi-targeted RTK inhibitor

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库存: 现货

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2mg

￥787.00

630.00

- +
5mg

￥1087.00

870.00

- +
10mg

￥1925.00

1540.00

- +
50mg

￥4537.00

3630.00

- +

已选 0 种 0 瓶

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货号: ajci17024
CAS: 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
分子式: C23H21N5O3S
分子量: 447.51
纯度: >98%
溶解度: ≥ 22.4 mg/mL in DMSO
储存: Store at -20°C
库存: 现货

Background

Amuvatinib (also known as MP-470 or HPK 56), a synthetic carbothioamide, is a novel and potent tyrosine kinase inhibitor, which exerts in vitro and in vivo activities 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