| Name | TAK-580 |
| Description | TAK-580 (MLN2480) is an oral, selective pan-Raf kinase inhibitor in Clinicalal trials. |
| Animal Research | [4]Animal Models: C57BL/6J miceFormulation: 100% PEG400Dosages: 12.5 mg/kgAdministration: oral gavage |
| In vitro | TAK-580 inhibits MAPK pathway signaling in BRAF mutant and some RAS mutant preClinicalal cancer models at concentrations that are tolerated in vivo. It is found to activate phosphorylated MEK at very low concentrations, but inhibits this same activity at higher concentrations. The inhibitory effects of MLN-2480 are found to vary across models and genetic contexts. In vitro analysis of this drug combination of TAK-580 and TAK-733(an investigational allosteric MEK kinase inhibitor) in cell proliferation assays demonstrates synergistic activity. In addition, western blot analysis demonstrates the effect of TAK-580 in reversing feedback activation of MEK in response to TAK-733, leading to more concerted MAPK pathway inhibition.MLN-2480 only modestly inhibits PRAK. |
| In vivo | In vivo, TAK-580 shows antitumor activity in melanoma, colon, lung, and pancreatic cancer xenograft models.MLN-2480 (37.5 mg/kg) is well tolerated in a tumor xenograft model. The combination of MLN-2480 (12.5 mg) and TAK-733 (1 mg/kg) is effective in an SK-MEL-30 xenograft model, but monotherapy with either compound produces negligible effects. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 93 mg/mL (183.7 mM)
Ethanol : 93 mg/mL (183.7 mM)
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| Keywords | MLN 2480 | BIIB 024 | Raf kinases | inhibit | MLN-2480 | TAK 580 | Raf | BIIB024 | Inhibitor | TAK580 | TAK-580 |
| Inhibitors Related | Regorafenib monohydrate | Exarafenib | Doramapimod | Vemurafenib | Sulindac sulfide | Sorafenib | Regorafenib | Dabrafenib | Sorafenib tosylate | PLX-4720 | LY3009120 | GW 441756 |
| Related Compound Libraries | Anti-Pancreatic Cancer Compound Library | Bioactive Compound Library | Pain-Related Compound Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Orally Active Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library |
United States
