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MLN 2480

Names

[ CAS No. ]:
1096708-71-2

[ Name ]:
MLN 2480

[Synonym ]:
(R)-2-(1-(6-amino-5-chloropyrimidine-4-carboxamido)ethyl)-N-(5-chloro-4-(trifluoromethyl)pyridin-2-yl)thiazole-5-carboxamide
2-[(1R)-1-[(6-amino-5-chloropyrimidine-4-carbonyl)amino]ethyl]-N-[5-chloro-4-(trifluoromethyl)pyridin-2-yl]-1,3-thiazole-5-carboxamide
BIIB024
CS-0751
MLN 2480

Biological Activity

[Description]:

MLN 2480 is an orally active and selective inhibitor of pan-Raf kinase.

[Related Catalog]:

Research Areas >> Cancer

[Target]

RAF


[In Vitro]

MLN2480 has effect on reversing feedback activation of MEK in response to TAK-733, leading to more concerted MAPK pathway inhibition[1].

[In Vivo]

MLN2480 inhibits MAPK pathway signaling in BRAF mutant and some RAS mutant preclinical cancer models at concentrations that are tolerated in vivo. MLN2480 is most potent in BRAF mutant melanoma models but also has single agent activity in some RAS mutant models. The combination of MLN2480 with TAK-733 inhibits the growth of a broader range of RAS mutant tumor models than single agent MLN2480, including primary human tumor xenograft models of melanoma and CRC[1].

[References]

[1]. Elizabeth Grace Carideo Cunniff, et al. Abstract C146: 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


[Related Small Molecules]

PLX8394 | Doramapimod (BIRB 796) | PLX-4720 | LGX 818 | LY 3009120 | GW5074 | RAF265 (CHIR-265) | AZ 628 | RAF709 | CEP-32496 | GDC-0879 | LXH254 | TAK-632 | PLX7904 | HG6-64-1

Chemical & Physical Properties

[ Density]:
1.64

[ Molecular Formula ]:
C17H12Cl2F3N7O2S

[ Molecular Weight ]:
506.28900

[ Exact Mass ]:
505.01000

[ PSA ]:
164.02000

[ LogP ]:
5.02430

[ Storage condition ]:
-20℃


Related Compounds