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.
| Molecular Weight | 447.51 |
| Formula | C23H21N5O3S |
| CAS Number | 850879-09-3 |
| Solubility (25°C) | DMSO 40 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
| Related VEGFR/PDGFR Products |
|---|
| Isolinderalactone
Isolinderalactone suppresses human glioblastoma growth and angiogenic activity through the inhibition of VEGFR2 activation in endothelial cells. Isolinderalactone suppressed the expression of B-cell lymphoma 2 (BCL-2), as well as of survivin and X-linked inhibitor of apoptosis protein (XIAP). |
| Oglufanide
Oglufanide (H-Glu-Trp-OH) is a dipeptide immunomodulator isolated from calf thymus. |
| KLTWQELYQLKYKGI
KLTWQELYQLKYKGI (QK) is a VEGF mimicking peptide, binds to the VEGF receptors and competes with VEGF. |
| Protein LMWP
Protein LMWP is a cell-penetrating peptide with vascular endothelial growth factor (VEGF) inhibitory activity. |
| CBO-P11
CBO-P11 specifically binds to receptor of VEGFR-2 and is used as targeting ligand for tumor angiogenesis. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
