PF-04880594
(Synonyms: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]氨基]丙腈;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;4-丁基溴化苄)
目录号 : KG10725
CAS No. : 1111636-35-1
纯度 : 98%
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 .
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 .
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 . 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 .
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 .
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分子式 |
C19H16F2N8
|
分子量 |
394.38
|
CAS号 |
1111636-35-1
|
中文名称 |
4-丁基溴化苄
|
储存方式 |
Store at -20° C
|