850879-09-3
Chemical Structure
Amuvatinib
Synonym(s): MP470; HPK 56
- CAS No.: 850879-09-3
- Formula:C23H21N5O3S
- Molecular Weight:447.51
IUPAC Name: N-(benzo[d][1,3]dioxol-5-ylmethyl)-4-(benzofuro[3,2-d]pyrimidin-4-yl)piperazine-1-carbothioamide
InChIKey: FOFDIMHVKGYHRU-UHFFFAOYSA-N
SMILES: S=C(N1CCN(C2=C3OC4=CC=CC=C4C3=NC=N2)CC1)NCC5=CC=C6OCOC6=C5
Biological Activity: 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].
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Amuvatinib | 99.40% | 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. Antineoplastic activity. | ||||||||||||||||||||
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Amuvatinib (Standard) | ≥98% | Amuvatinib (Standard) is the analytical standard of Amuvatinib. This product is intended for research and analytical applications. 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. Antineoplastic activity. | ||||||||||||||||||||
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References
- [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. [Content Brief]
- [2]. 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. [Content Brief]
- [3]. Baxter PA, et al. Plasma and cerebrospinal fluid pharmacokinetics of MP470 in non-human primates. Cancer Chemother Pharmacol. 2011 Apr;67(4):809-12. [Content Brief]
- [4]. David J. Bearss, et al. Pharmaceutical formulations comprising salts of a protein kinase inhibitor and methods of using same. US20080226747A1.
