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Product Description
– Amuvatinib hydrochloride (MP470 hydrochloride) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret. Amuvatinib hydrochloride (MP470 hydrochloride) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair[1][2][3]. Antineoplastic activity[4].
Web ID
– HY-10206A
Shipping
– Room temperature
Applications
– Cancer-Kinase/protease
Molecular Formula
– C23H21N5O3S.xHCl
References
– [1]Tibes R, et al. 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 Feb;71(2):463-71.|[2]David J. Bearss, et al. Pharmaceutical formulations comprising salts of a protein kinase inhibitor and methods of using same. US20080226747A1.|[3]Qi W, et al. MP470, a novel receptor tyrosine kinase inhibitor, in combination with Erlotinib inhibits the HER family/PI3K/Akt pathway and tumor growth in prostate cancer. BMC Cancer. 2009 May 11;9:142.|[4]Choy G, et al. Safety, tolerability, and pharmacokinetics of amuvatinib from three phase 1 clinical studies in healthy volunteers. Cancer Chemother Pharmacol. 2012 Jul;70(1):183-90.|[5]Baxter PA, et al. Plasma and cerebrospinal fluid pharmacokinetics of MP470 in non-human primates. Cancer Chemother Pharmacol. 2011 Apr;67(4):809-12.
CAS Number
– 1055986-67-8
Molecular Weight
– N/A
SMILES
– S=C(N1CCN(C2=C3OC4=CC=CC=C4C3=NC=N2)CC1)NCC5=CC=C6OCOC6=C5.[x].Cl
Clinical Information
– Phase 2
Research Area
– Cancer
Solubility
– 10 mM in DMSO
Target
– c-Kit;c-Met/HGFR;FLT3;PDGFR;RAD51;RET
Isoform
– PDGFRα
Pathway
– Cell Cycle/DNA Damage;Protein Tyrosine Kinase/RTK
Product type
– Reference compound
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