Amuvatinib

Amuvatinib (MP470) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret. Amuvatinib (MP470) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair[1][2][3]. Antineoplastic activity[4].

Product Specifications

CAS Number

[850879-09-3]

Product Name Alternative

MP470; HPK 56

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; c-Kit; c-Met/HGFR; FLT3; PDGFR; RAD51; RET

Type

Reference compound

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/amuvatinib.html

Purity

99.40

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

S=C(N1CCN(C2=C3OC4=CC=CC=C4C3=NC=N2)CC1)NCC5=CC=C6OCOC6=C5

Molecular Formula

C23H21N5O3S

Molecular Weight

447.51

Precautions

H302, H315, H319, H335

References & Citations

[1]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.|[2]Baxter PA, et al. Plasma and cerebrospinal fluid pharmacokinetics of MP470 in non-human primates. Cancer Chemother Pharmacol. 2011 Apr;67 (4) :809-12.|[3]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.|[4]David J. Bearss, et al. Pharmaceutical formulations comprising salts of a protein kinase inhibitor and methods of using same. US20080226747A1.|[5]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.