MLN2480

For research use only.

Catalog No.S7121 Synonyms: BIIB-024, TAK580

3 publications

MLN2480 Chemical Structure

CAS No. 1096708-71-2

MLN2480 (BIIB-024, TAK580) is an oral, selective pan-Raf kinase inhibitor in chinical trials.

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Biological Activity

Description MLN2480 (BIIB-024, TAK580) 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].

Assay
Methods Test Index PMID
Western blot
p-ERK / ERK ; 

PubMed: 28082416     


Wild-type BRAF cells were treated with MLN2480 for 1 hour and phospho-ERK assayed by immunoblot.

28082416
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
  • Dosages: 12.5 mg/kg
  • Administration: oral gavage
    (Only for Reference)

Solubility (25°C)

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

* 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
Smiles CC(C1=NC=C(S1)C(=O)NC2=NC=C(C(=C2)C(F)(F)F)Cl)NC(=O)C3=C(C(=NC=N3)N)Cl

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03429803 Recruiting Drug: TAK-580 Low-grade Glioma Karen D. Wright MD|PLGA Fund at Pediatric Brain Tumor 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
NCT01425008 Completed Drug: MLN2480 Melanoma|Metastatic Melanoma|Solid Tumor|Neoplasm Millennium Pharmaceuticals Inc.|Takeda September 15 2011 Phase 1

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

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Raf Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID