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Amuvatinib (MP-470, HPK 56)

Multi-kinase inhibitor, inhibits PDGFR, c-Kit, and Flt3

Amuvatinib (MP-470, HPK 56)

Catalog No. A4237
Size Price Stock Qty
Evaluation Sample $28.00 In stock
2mg $75.00 In stock
5mg $130.00 In stock
10mg $230.00 In stock
50mg $520.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

Amuvatinib (MP-470, HPK 56)

Related Biological Data

Amuvatinib (MP-470, HPK 56)

Related Biological Data

Amuvatinib (MP-470, HPK 56)

Biological Activity

Description Amuvatinib (MP-470) is a potent and multi-targeted inhibitor of c-Kit, PDGFRα and Flt3 with IC50 of 10 nM, 40 nM and 81 nM, respectively.
Targets c-KitD816H PDGFRαV561D Flt3D835Y      
IC50 10 nM 40 nM 81 nM      

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Chemical Properties

Cas No. 850879-09-3 SDF Download SDF
Synonyms MP470,MP 470,HPK56
Chemical Name N-(1,3-benzodioxol-5-ylmethyl)-4-([1]benzofuro[3,2-d]pyrimidin-4-yl)piperazine-1-carbothioamide
Canonical SMILES C1CN(CCN1C2=NC=NC3=C2OC4=CC=CC=C43)C(=S)NCC5=CC6=C(C=C5)OCO6
Formula C23H21N5O3S M.Wt 447.51
Solubility Soluble in DMSO Storage Store at -20°C
Shipping Condition: Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

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

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

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