| CAS NO: | 1111636-35-1 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 25mg | 电议 |
| Cas No. | 1111636-35-1 |
| 别名 | 3-[[4-[1-(2,2-二氟乙基)-3-(1H-吡咯并[2,3-B]吡啶-5-基)-1H-吡唑-4-基]-2-嘧啶基]氨基]-丙腈 |
| 化学名 | 3-[[4-[1-(2,2-difluoroethyl)-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrazol-4-yl]pyrimidin-2-yl]amino]propanenitrile |
| Canonical SMILES | C1=CNC2=NC=C(C=C21)C3=NN(C=C3C4=NC(=NC=C4)NCCC#N)CC(F)F |
| 分子式 | C19H16F2N8 |
| 分子量 | 394.38 |
| 溶解度 | Soluble in DMSO |
| 储存条件 | Store at -20° C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | PF-04880594 is a selective inhibitor of B-Raf, B-RafV599E and c-Raf with IC50 value of 0.19 nM, 0.13 nM and 0.39 nM, respectively [1]. Raf is a serine/threonine protein kinase and plays an important role in the MAPK/ERK signaling pathway. It has been revealed that Raf involves in cancers and developmental syndromes and its inhibitors are regarded as a promising target for cancer treatment [2, 3]. PF-04880594 is a potent Raf inhibitor. When tested with GTL16 and GTL16 resistant cell clones, PF-04880594 treatment significantly decreased cell viability and ERK activity [2]. In 3D culture model of RHE cells (histologic similar to human epidermal lasers), PF-04880594 treatment (62.5 nmol/L, 2 d) significantly induced necrosis with ghost cells accounting for nearly 50% to 60% of the culture thickness via inducing p-ERK expression level [3]. Treated nude mice model with PF-04880594 (10-40 mg/kg, twice daily for 3 weeks) and then mice were sacrificed for further study. The results revealed that PF-04880594 treatment induced ERK phosphorylation and B-Raf-c-Raf dimerization in multiple epithelial tissues which phenomenon could be attenuated by PD-0325901 [3]. References: |
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