Amuvatinib (formerly known as MP470), is a novel receptor tyrosine kinase inhibitor, it has inhibitory effect on prostate cancer in combination with Erlotinib in vitro and in vivo. Amuvaninib (MP470) inhibited RAD51 protein expression and HR. Amuvatinib also inhibits activities of other receptor tyrosine kinases, such as c-Met, Ret oncoprotein, and mutant forms of Flt3, which are frequently dysregulated in variety of tumors. Amuvatinib (MP470) exhibits low microM IC50 in prostate cancer cell lines. When LNCaP were treated with MP470 in combination with Erlotinib, additive effects on both cytotoxicity and induction of apoptosis were observed. Furthermore, the MP470-Erlotinib combination produced 30-65% dose-dependent tumor growth inhibition (TGI) in a LNCaP mouse xenograft model. Amuvatinib (MP470) sensitized cells to IR and MMC, agents that are selectively toxic to HR-deficient cells. Mutant forms of c-Kit are often associated with tumor chemoresistance.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 30 mg/mL|
The receptor tyrosine kinase inhibitor amuvatinib (MP470) sensitizes tumor cells to radio- and chemo-therapies in part by inhibiting homologous recombination.
Zhao H, et al. Radiother Oncol. 2011 Oct;101(1):59-65. PMID: 21903282.
MP470, a novel receptor tyrosine kinase inhibitor, in combination with Erlotinib inhibits the HER family/PI3K/Akt pathway and tumor growth in prostate cancer.
Qi W, et al. BMC Cancer. 2009 May 11;9:142. PMID: 19432987.
|Related VEGFR/PDGFR Products|
Sunitinib is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit.
Avapritinib (BLU-285) is a small molecule kinase inhibitor that potently inhibits PDGFRα D842V mutant activity in vitro (IC50 = 0.5 nM) and PDGFRα D842V autophosphorylation in the cellular setting (IC50 = 30 nM); also a potent inhibitor of the analogous KIT mutation, D816V in KIT Exon 17 (IC50 = 0.5 nM).
|Nintedanib Ethanesulfonate Salt
BIBF 1120 esylate is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
Regorafenib (BAY 73-4506) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively.
|Pazopanib HCl (GW786034 )
Pazopanib HCl (GW786034 HCl) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively.
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