MLN 2480

Pan-Raf kinase inhibitor,investigational CAS# 1096708-71-2

MLN 2480

Catalog No. BCC1771----Order now to get a substantial discount!

Product Name & Size Price Stock
MLN 2480: 5mg $138 In Stock
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Chemical structure

MLN 2480

3D structure

Chemical Properties of MLN 2480

Cas No. 1096708-71-2 SDF Download SDF
PubChem ID 25161177 Appearance Powder
Formula C17H12Cl2F3N7O2S M.Wt 506.29
Type of Compound N/A Storage Desiccate at -20°C
Synonyms BIIB-024
Solubility DMSO : 50 mg/mL (98.76 mM; Need ultrasonic)
Chemical Name 2-[(1R)-1-[(6-amino-5-chloropyrimidine-4-carbonyl)amino]ethyl]-N-[5-chloro-4-(trifluoromethyl)pyridin-2-yl]-1,3-thiazole-5-carboxamide
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
Standard InChIKey VWMJHAFYPMOMGF-ZCFIWIBFSA-N
Standard InChI InChI=1S/C17H12Cl2F3N7O2S/c1-6(28-15(31)12-11(19)13(23)27-5-26-12)16-25-4-9(32-16)14(30)29-10-2-7(17(20,21)22)8(18)3-24-10/h2-6H,1H3,(H,28,31)(H2,23,26,27)(H,24,29,30)/t6-/m1/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of MLN 2480

DescriptionMLN 2480 is an oral, selective inhibitor of Raf kinases.
TargetsRaf kinases    

MLN 2480 Dilution Calculator

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MLN 2480 Molarity Calculator

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Preparing Stock Solutions of MLN 2480

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.9752 mL 9.8758 mL 19.7515 mL 39.5031 mL 49.3788 mL
5 mM 0.395 mL 1.9752 mL 3.9503 mL 7.9006 mL 9.8758 mL
10 mM 0.1975 mL 0.9876 mL 1.9752 mL 3.9503 mL 4.9379 mL
50 mM 0.0395 mL 0.1975 mL 0.395 mL 0.7901 mL 0.9876 mL
100 mM 0.0198 mL 0.0988 mL 0.1975 mL 0.395 mL 0.4938 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

Organizitions Citing Our Products recently

 
 
 

Calcutta University

University of Minnesota

University of Maryland School of Medicine

University of Illinois at Chicago

The Ohio State University

University of Zurich

Harvard University

Colorado State University

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Yale University

Worcester Polytechnic Institute

Washington State University

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University of Leipzig

Universidade da Beira Interior

The Institute of Cancer Research

Heidelberg University

University of Amsterdam

University of Auckland
TsingHua University
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The University of Michigan
The University of Michigan
Miami University
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DRURY University
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Jilin University
Jilin University
Fudan University
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Wuhan University
Wuhan University
Sun Yat-sen University
Sun Yat-sen University
Universite de Paris
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Deemed University
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Auckland University
Auckland University
The University of Tokyo
The University of Tokyo
Korea University
Korea University

Background on MLN 2480

MLN2480 is an potent pan-RAF kinase inhibitor.

In vitro: MLN2480 inhibits MAPK pathway signaling in BRAF mutant and some RAS mutant preclinical cancer models at concentrations that are tolerated in vivo. In vitro analysis of this drug combination of MLN2480 and TAK-733 in cell proliferation assays demonstrates synergistic activity [1].

In vivo: MLN2480 is most potent in BRAF mutant melanoma models but also has single agent activity in some RAS mutant models. The MLN2480 and TAK-733 combination inhibits the growth of a broader range of RAS mutant tumor models than MLN2480 single agent, including primary human tumor xenograft models of melanoma and CRC [2].

Clinical trial: In the first-in-human study (n=24), the safety profile of MLN2480 up to 200 mg Q2D was acceptable. Accrual continues at 200 mg to confirm the MTD [2].

References:
[1] Elizabeth Grace Carideo Cunniff, Julie Zhang, Jouhara Chouitar, et al.  Combination treatment with the investigational RAF kinase inhibitor MLN2480 and the investigational MEK kinase inhibitor TAK-733 inhibits the growth of BRAF mutant and RAS mutant preclinical models of melanoma and CRC. Mol Cancer Ther November 2013 12; C146
[2] Drew Warren Rasco, Anthony J.   Olszanski, Amita Patnaik, et al. MLN2480, an investigational oral pan-RAF kinase inhibitor, in patients (pts) with relapsed or refractory solid tumors: Phase I study. J Clin Oncol 31, 2013 (suppl; abstr 2547)

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Description

TAK-580 (MLN 2480) is an orally active and selective inhibitor of pan-Raf kinase.

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