MLN 2480Pan-Raf kinase inhibitor,investigational CAS# 1096708-71-2 |
2D Structure
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Quality Control & MSDS
3D structure
Package In Stock
Number of papers citing our products
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. |
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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. |
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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. |
Description | MLN 2480 is an oral, selective inhibitor of Raf kinases. | |||||
Targets | Raf kinases |
MLN 2480 Dilution Calculator
MLN 2480 Molarity Calculator
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. |
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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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