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MP-470 (Amuvatinib) Chemical Structure
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Biological Activity
MP-470 (Amuvatinib) is a multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Met, c-Kit, PDGFRalpha, Flt3, and c-Ret and with an IC50 of median 5 μM. MP-470 (Amuvatinib) reduced c-Met phosphorylation and enhanced radiation-induced cell kill by 0.4 logs in SF767 cells. Cells pretreated with MP-470 (Amuvatinib) had more ds DNA damage than cells treated with radiation alone. Mechanistically, MP-470 was shown to inhibit dsDNA break repair and increase apoptosis. [1][2] In a study, the cytotoxicity ofMP-470 (Amuvatinib) was evaluated on prostate cancer cell lines (LNCaP, PC-3 and DU-145). MP-470 (Amuvatinib) was effective on LNCaP and PC-3 cells with IC50 of ~4 μM and 8 μM, respectively. [3]
References on MP-470 (Amuvatinib)
- [1] Radiation Oncology 2009;4:69
- [2] BMC Cancer 2009; 9:142
Chemical Information
| Molecular Weight (WM): | 447.51 |
|---|---|
| Formula: | C23H21N5O3S |
| CAS No.: | 850879-09-3 |
| Synonyms: |
N/A
|
| Dissolve in (25°C): | DMSO ≥32mg/mL |
| Water <1mg/mL | |
| Ethanol <1mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
Quality Control & MSDS
Research Area
Receptor Tyrosine Kinase >> c-Met >> c-Met Inhibitors
Receptor Tyrosine Kinase >> c-Kit >> c-Kit Inhibitors
Receptor Tyrosine Kinase >> PDGFR >> PDGFR Inhibitors
Angiogenesis >> PDGFR >> PDGFR Inhibitors
Receptor Tyrosine Kinase >> c-RET >> c-RET Inhibitors
Apoptosis >> c-RET >> c-RET Inhibitors
Angiogenesis >> Flt >> Flt Inhibitors
Receptor Tyrosine Kinase >> c-Kit >> c-Kit Inhibitors
Receptor Tyrosine Kinase >> PDGFR >> PDGFR Inhibitors
Angiogenesis >> PDGFR >> PDGFR Inhibitors
Receptor Tyrosine Kinase >> c-RET >> c-RET Inhibitors
Apoptosis >> c-RET >> c-RET Inhibitors
Angiogenesis >> Flt >> Flt Inhibitors
Notes:
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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.
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.
Data independently produced by Dr. Yong-Weon Yi from Georgetown University Medical Center.MP-470 purchased from Selleck. MP-470 (Amuvatinib) purchased from Selleck
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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. |
Data independently produced by Dr. Yong-Weon Yi from Georgetown University Medical Center.MP-470 purchased from Selleck.
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