| Identification | Back Directory | [Name]
BenzaMide, N-[3-[3-[4-[(diMethylaMino)Methyl]phenyl]pyrazolo[1,5-a]pyriMidin-7-yl]phenyl]-3-(trifluoroMethyl)- | [CAS]
950736-05-7 | [Synonyms]
CS-1184
MDK36057
RAF-IN-10n
B-Raf IN 1
B-Raf inhibit 1
B-Raf IN 1, >=98%
N-(3-(3-(4-((diMethylaMino)Methyl)phenyl)pyrazolo[1,5-a]pyriMidin-7-yl)phenyl)-3-(trifluoroMethyl)benzaMide
BenzaMide, N-[3-[3-[4-[(diMethylaMino)Methyl]phenyl]pyrazolo[1,5-a]pyriMidin-7-yl]phenyl]-3-(trifluoroMethyl)- | [Molecular Formula]
C29H24F3N5O | [MDL Number]
MFCD25977055 | [MOL File]
950736-05-7.mol | [Molecular Weight]
515.53 |
| Chemical Properties | Back Directory | [density ]
1.28±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 14 mg/ml; DMSO: 33 mg/ml; Ethanol: 1 mg/ml | [form ]
Powder | [pka]
12.75±0.70(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Description]
B-RAF IN 1 is an inhibitor of B-RAF (IC50 = 24 nM) that also inhibits C-RAF (IC50 = 25 nM). It is selective over 13 other kinases, including PKCα, IKKβ, and PI3Kα, at concentrations greater than 2 μM, but does inhibit p38α and CAMKII (IC50s = 216 and 822 nM, respectively). B-RAF IN 1 binds to B-RAF in the inactive conformation based on co-crystallization with the wild-type enzyme. It inhibits proliferation of WM 266-4 and HT29 cells with IC50 values of 920 and 780 nM, respectively. | [Uses]
N-[3-[3-[4-[(Dimethylamino)methyl]phenyl]pyrazolo[1,5-a]pyrimidin-7-yl]phenyl]-3-(trifluoromethyl)benzamide is a potent and selective B-Raf inhibitor. | [IC 50]
B-Raf: 24 nM (IC50) | [References]
[1] DAN M. BERGER . Non-hinge-binding pyrazolo[1,5-a]pyrimidines as potent B-Raf kinase inhibitors[J]. Bioorganic & Medicinal Chemistry Letters, 2009, 19 23: Pages 6519-6523. DOI: 10.1016/j.bmcl.2009.10.049 |
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