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 [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 . 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 .

Product information

CAS Number: 1111636-35-1

Molecular Weight: 394.38

Formula: C19H16F2N8

Chemical Name: 3-({4-[1-(2,2-difluoroethyl)-3-{1H-pyrrolo[2,3-b]pyridin-5-yl}-1H-pyrazol-4-yl]pyrimidin-2-yl}amino)propanenitrile

Smiles: N#CCCNC1N=C(C=CN=1)C1=CN(CC(F)F)N=C1C1C=C2C=CNC2=NC=1

InChiKey: HFYMVDKBZONUOJ-UHFFFAOYSA-N

InChi: InChI=1S/C19H16F2N8/c20-16(21)11-29-10-14(15-3-7-25-19(27-15)24-5-1-4-22)17(28-29)13-8-12-2-6-23-18(12)26-9-13/h2-3,6-10,16H,1,5,11H2,(H,23,26)(H,24,25,27)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.