MLN2480

Catalog No.S7121 Synonyms: BIIB-024, TAK580

MLN2480 Chemical Structure

Molecular Weight(MW): 506.29

MLN2480 is an oral, selective pan-Raf kinase inhibitor in chinical trials.

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Biological Activity

Description MLN2480 is an oral, selective pan-Raf kinase inhibitor in chinical trials.
Targets
Raf [1]
In vitro

MLN2480 inhibits MAPK pathway signaling in BRAF mutant and some RAS mutant preclinical cancer models at concentrations that are tolerated in vivo[1]. 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[2]. 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[1][2].

In vivo In vivo, MLN2480 shows antitumor activity in melanoma, colon, lung, and pancreatic cancer xenograft models[3].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[2].

Protocol

Animal Research:

[4]

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  • Animal Models: C57BL/6J mice
  • Formulation: 100% PEG400
  • Dosages: 12.5 mg/kg
  • Administration: oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (197.51 mM)
Ethanol 100 mg/mL (197.51 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 506.29
Formula

C17H12Cl2F3N7O2S

CAS No. 1096708-71-2
Storage powder
in solvent
Synonyms BIIB-024, TAK580

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Tech Support

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Raf Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID