Catalog No.S7121 Synonyms: BIIB-024, TAK580
Molecular Weight(MW): 506.29
MLN2480 is an oral, selective pan-Raf kinase inhibitor in chinical trials.
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|Description||MLN2480 is an oral, selective pan-Raf kinase inhibitor in chinical trials.|
MLN2480 inhibits MAPK pathway signaling in BRAF mutant and some RAS mutant preclinical 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 MLN2480 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 MLN2480 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, MLN2480 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.|
|In vitro||DMSO||100 mg/mL (197.51 mM)|
|Ethanol||100 mg/mL (197.51 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02723006||Terminated||Melanoma||Millennium Pharmaceuticals Inc.|Takeda||July 5 2016||Phase 1|
|NCT03429803||Recruiting||Low-grade Glioma||Karen D. Wright MD|PLGA Foundation|Millennium Pharmaceuticals Inc.|National Cancer Institute (NCI)|Pacific Pediatric Neuro-Oncology Consortium|Team Jack Foundation|Dana-Farber Cancer Institute||February 27 2018||Phase 1|Phase 2|
|NCT01425008||Active not recruiting||Melanoma|Metastatic Melanoma|Solid Tumor||Millennium Pharmaceuticals Inc.|Takeda||September 15 2011||Phase 1|
|NCT02327169||Completed||Advanced Nonhematologic Malignancies||Millennium Pharmaceuticals Inc.|Takeda||January 14 2015||Phase 1|
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