PF-04880594 is a RAF inhibitor, which induces ERK phosphorylation and RAF dimerization in those epithelial tissues that undergo hyperplasia. PF-04880594 stimulates production of the inflammatory cytokine interleukin 8 in HL-60 cells. Epithelial tissue hyperplasia induced by the RAF inhibitor PF-04880594 is attenuated by a clinically well-tolerated dose of the MEK inhibitor PD-0325901. The combination treatment with PF-04880594 and MEK inhibitors might greatly increase the safety and therapeutic index of RAF inhibitors for the treatment of melanoma and other cancers.
CAS 1111636-35-1 MFCD211636351
化学结构图
SMILES: N#CCCNc1nccc(-c2cn(CC(F)F)nc2-c2cnc3[nH]ccc3c2)n1
化学属性
| Mol. Weight | 394.38 |
|---|---|
| Appearance | Solid powder |
| Solubility | Soluble in DMSO, not in water |
别名和识别编码
| Chemical Name Translation | |
|---|---|
| Chemical Name | PF-04880594 is a RAF inhibitor, which induces ERK phosphorylation and RAF dimerization in those epithelial tissues that undergo hyperplasia. PF-04880594 stimulates production of the inflammatory cytokine interleukin 8 in HL-60 cells. Epithelial tissue hyperplasia induced by the RAF inhibitor PF-04880594 is attenuated by a clinically well-tolerated dose of the MEK inhibitor PD-0325901. The combination treatment with PF-04880594 and MEK inhibitors might greatly increase the safety and therapeutic index of RAF inhibitors for the treatment of melanoma and other cancers. |
| Formula | C19H16F2N8 |
| Synonym | PF04880594; PF-04880594; PF 04880594. |
| IUPAC 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 |
| 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) |
| Canonical SMILES | N#CCCNC1=NC=CC(C2=CN(CC(F)F)N=C2C3=CN=C(NC=C4)C4=C3)=N1 |
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- PF-04880594 is a RAF inhibitor, which induces ERK phosphorylation and RAF dimerization in those epithelial tissues that undergo hyperplasia. PF-04880594 stimulates production of the inflammatory cytokine interleukin 8 in HL-60 cells. Epithelial tissue hyperplasia induced by the RAF inhibitor PF-04880594 is attenuated by a clinically well-tolerated dose of the MEK inhibitor PD-0325901. The combination treatment with PF-04880594 and MEK inhibitors might greatly increase the safety and therapeutic index of RAF inhibitors for the treatment of melanoma and other cancers.
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