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TAK-580

Catalog No. T6895 CAS 1096708-71-2

Synonyms: MLN2480, BIIB-024

TAK-580 (MLN2480) is an oral, selective pan-Raf kinase inhibitor in Clinicalal trials.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

TAK-580, CAS 1096708-71-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 48.00
2 mg	In stock	$ 68.00
5 mg	In stock	$ 105.00
10 mg	In stock	$ 189.00
25 mg	In stock	$ 318.00
50 mg	In stock	$ 469.00
100 mg	In stock	$ 689.00
1 mL * 10 mM (in DMSO)	In stock	$ 118.00

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Purity: 99.77%

Purity: 98.42%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	TAK-580 (MLN2480) is an oral, selective pan-Raf kinase inhibitor in Clinicalal trials.
In vitro	MLN2480 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 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.
Animal Research	[4]Animal Models: C57BL/6J miceFormulation: 100% PEG400Dosages: 12.5 mg/kgAdministration: oral gavage

Synonyms	MLN2480, BIIB-024
Molecular Weight	506.29
Formula	C17H12Cl2F3N7O2S
CAS No.	1096708-71-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 93 mg/mL (183.7 mM)

Ethanol: 93 mg/mL (183.7 mM)

References and Literature

1. Elizabeth Grace Carideo Cunniff, et al. Journal of Clinical Oncology. 2013:e13529. 2. Macauley D, et al.Drugs Fut.2012,37(6):451. 3. Drew Warren Rasco, et al. J Clin Oncol 31, 2013 (suppl; abstr 2547)

Related compound libraries

This product is contained In the following compound libraries：

Tyrosine Kinase Inhibitor Library Anti-Cancer Drug Library Inhibitor Library Kinase Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Drug Repurposing Compound Library Anti-Liver Cancer Compound Library Anti-Colorectal Cancer Compound Library Immunology/Inflammation Compound Library

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Related compounds with same targets

Doramapimod K-Ras(G12C) inhibitor 9 ARS-853 B-Raf IN 13 KG5 AZ 628 MRTX0902 B-Raf IN 11

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

TAK-580 1096708-71-2 MAPK Raf MLN 2480 BIIB 024 Raf kinases inhibit MLN-2480 TAK 580 BIIB024 MLN2480 Inhibitor TAK580 BIIB-024 inhibitor

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