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B-Raf inhibitor

Names

[ CAS No. ]:
1315330-11-0

[ Name ]:
B-Raf inhibitor

[Synonym ]:
N-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-4-methyl-3-((6-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)benzamide
B-Raf inhibitor|
CS-1099
N-[4-[(4-Ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-4-methyl-3-[(6-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy]benzamide
B-Raf inhibitor

Biological Activity

[Description]:

TAK1/MAP4K2 inhibitor 1 is a potent dual TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2) inhibitor, with IC50s of 41.1 nM and 18.2 nM, respectively.

[Related Catalog]:

Signaling Pathways >> MAPK/ERK Pathway >> MAP3K
Signaling Pathways >> MAPK/ERK Pathway >> MAP4K
Research Areas >> Cancer

[Target]

TAK1:41.1 nM (IC50)

MAP4K2:18.2 nM (IC50)


[In Vivo]

TAK1/MAP4K2 inhibitor 1 has moderate terminal elimination half-life (t1/2=2.94 h for mice (1 mg/kg, iv))[1].

[References]

[1]. Tan L, et al. Discovery of type II inhibitors of TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2). J Med Chem. 2015 Jan 8;58(1):183-96.


[Related Small Molecules]

Takinib | Selonsertib(GS-4997) | NG25 | GNE-495 | NCB-0846 | GNE-3511 | 5Z-7-Oxozeaenol | NQDI 1 | PF-06260933 | GS-444217 | GNE 220

Chemical & Physical Properties

[ Molecular Formula ]:
C29H31F3N6O2

[ Molecular Weight ]:
552.59100

[ Exact Mass ]:
552.24600

[ PSA ]:
89.87000

[ LogP ]:
6.03540

[ Storage condition ]:
2-8℃


Related Compounds