Catalog No.S1244 Synonyms: HPK 56
Molecular Weight(MW): 447.51
Amuvatinib (MP-470) is a potent and multi-targeted inhibitor of c-Kit, PDGFRα and Flt3 with IC50 of 10 nM, 40 nM and 81 nM, respectively. Phase 2.
Cited by 6 Publications
4 Customer Reviews
Effects of treatment for 48h with a vehicle or the indicated doses of MP-470 in parental or ER1 and ER2 cell lines in the absence and presence of erlotinib on the indicated biomarkers. Data represent 3 independent experiments.
Nat Genet 2012 44(8), 852-60. Amuvatinib (MP-470) purchased from Selleck.
Amuvatinib (3 umol/l, 72 h) leads to decreased pAXL, pAKT, and pERK expression by western blot.
Melanoma Res 2014 24(5), 448-53. Amuvatinib (MP-470) purchased from Selleck.
For MTT assays, cells (2,000 ~ 5,000 cells/well) were subcultured into 96-well plates according to their growth properties. Cell proliferation was assayed at 72 hr after treatment of MP-470 by adding 20 μl of 5 mg/ml 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution per 100 μl of growth medium. After incubating for 3-4 h at 37°C, the media were removed and 150 µl/well of MTT solvent (either absolute DMSO or isopropanol containing 4 mM HCl and 0.1% Nonidet-40) was added to dissolve the formazan.
Dr. Yong-Weon Yi from Georgetown University Medical Center. Amuvatinib (MP-470) purchased from Selleck.
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Choose Selective c-Kit Inhibitors
|Description||Amuvatinib (MP-470) is a potent and multi-targeted inhibitor of c-Kit, PDGFRα and Flt3 with IC50 of 10 nM, 40 nM and 81 nM, respectively. Phase 2.|
The hydrochloride salt of MP-470 also inhibits several mutants of c-Kit, including c-KitD816V, c-KitD816H, c-KitV560G, and c-KitV654A, as well as a Flt3 mutant (Flt3D835Y) and two PDGFRα mutants (PDGFRαV561D and PDGFRαD842V), with IC50 of 10 nM to 8.4 μM. MP-470 potently inhibits the proliferation of OVCAR-3, A549, NCI-H647, DMS-153, and DMS-114 cells, with IC50 of 0.9 μM–7.86 μM.  MP-470 also inhibits c-Kit and PDGFRα, with IC50 values of 31 μM and 27 μM, respectively. MP-470 demonstrates potent cytotoxicity against MiaPaCa-2, PANC-1, and GIST882 cells, with IC50 of 1.6 μM to 3.0 μM. MP-470 also binds to and inhibits several c-Kit mutants, including c-KitK642E, c-KitD816V, and c-KitK642E/D816V.  In MDA-MB-231 cells, MP-470 (1 μM) inhibits tyrosine phosphorylation of AXL.  In LNCaP and PC-3, but not DU145 cells, MP-470 exhibits cytotoxicity with IC50 of 4 μM and 8 μM, respectively, and induces apoptosis at 10 μM. In LNCaP cells, MP-470 (10 μM) elicits G1 arrest and decreases phosphorylation of Akt and ERK1/2.  In SF767 cells, MP-470 (10 μM) inhibits c-Met phosphorylation and sensitizes cells to radiation. In combination with radiation, MP-470 (10 μM) inhibits glycogen synthase kinase (GSK)3β activity, induces apoptosis, and disrupts the repair of dsDNA breaks probably through suppression of Rad51.  
|In vivo||In mice xenograft models of HT-29, A549, and SB-CL2 cells, MP-470 (10 mg/kg–75 mg/kg via i.p. or 50 mg/kg–200 mg/kg via p.o.) inhibits tumor growth.  In mice bearing LNCaP xenograft, MP-470 (20 mg/kg) combined with Erlotinib significantly induces tumor growth inhibition (TGI). |
Kinase inhibition assay of c-Kit and PDGFRα:For the testing of inhibitory activity against c-Kit and PDGFRα, enzymes are incubated with varying concentrations of MP-470 and radiolabeled γ-32P-ATP. After 30 min, the reaction mixtures are electrophoresed on an acrylamide gel and autophosphorylation, quantitated by the amount of radioactivity incorporated into the enzyme, is assayed.
-  Bearss DJ, et al. US Patent, US/2008/0226747.
-  Hurley LH, et al. World Patent, WO/2005/037825.
-  Mahadevan D, et al. Oncogene, 2007, 26(27), 3909-3919.
|In vitro||DMSO||32 mg/mL (71.5 mM)|
|In vivo||Add solvents individually and in order:
30% PEG400+0.5% Tween80+5% propylene glycol
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01357395||Unknown status||Small Cell Lung Carcinoma||Astex Pharmaceuticals||May 2011||Phase 2|
|NCT00881166||Completed||Malignant Disease||Astex Pharmaceuticals||November 2007||Phase 1|
|NCT00894894||Completed||Solid Tumors||Astex Pharmaceuticals||May 2007||Phase 1|
|NCT00504205||Terminated||Lymphoma|Unspecified Adult Solid Tumor, Protocol Specific||Astex Pharmaceuticals|National Cancer Institute (NCI)||May 2007||--|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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