| Identification | Back Directory | [Name]
Propanenitrile, 3-[[4-[1-(2,2-difluoroethyl)-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazol-4-yl]-2-pyriMidinyl]aMino]- | [CAS]
1111636-35-1 | [Synonyms]
CS-727
PF-04880594
PF-04880594/PF04880594
3-[[4-[1-(2,2-difluoroethyl)-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrazol-4-yl]pyrimidin-2-yl]amino]propanenitrile
3-[[4-[1-(2,2-Difluoroethyl)-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazol-4-yl]-2-pyrimidinyl]amino]propanenitrile
Propanenitrile, 3-[[4-[1-(2,2-difluoroethyl)-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazol-4-yl]-2-pyriMidinyl]aMino]-
3-[[4-[1-(2,2-Difluoroethyl)-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazol-4-yl]-2-pyrimidinyl]amino]propanenitrile
DISCONTINUED | [Molecular Formula]
C19H16F2N8 | [MOL File]
1111636-35-1.mol | [Molecular Weight]
394.38 |
| Chemical Properties | Back Directory | [density ]
1.48±0.1 g/cm3(Predicted) | [storage temp. ]
room temp | [solubility ]
Soluble in DMSO | [form ]
powder | [pka]
12.99±0.40(Predicted) | [color ]
white to beige |
| Hazard Information | Back Directory | [Uses]
3-[[4-[1-(2,2-Difluoroethyl)-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazol-4-yl]-2-pyrimidinyl]amino]propanenitrile is a pyrazole compound and a potential Raf inhibitors. | [Biochem/physiol Actions]
PF-04880594 is a potent and selective RAF inhibitor that inhibits both wild-type and mutant BRAF and CRAF. PF-04880594 potently inhibits tumor growth in BRAF-mutant melanoma xenograft models. | [in vivo]
PF-04880594 (10 mg/kg) induces ERK phosphorylation and BRAF-CRAF dimerization in multiple epithelial tissues in mice and the induction can be attenuated by PD0325901[1].
PF-04880594 (0-40 mg/kg, twice daily for 3 weeks) induces epithelial hyperplasia in mice and the induction is prevented by PD0325901[1]. | Animal Model: | Nude mice[1] | | Dosage: | 10 mg/kg alone or in combination with 0.5 mg/kg PD-0325901 | | Administration: | An am and pm dose on day 1 and then an am dose on day 2 approximately 2 hours before the animals were necropsied and the tissues harvested | | Result: | Induced ERK phosphorylation in urinary bladder, tongue, skin, and esophagus tissues.
The induction of ERK phosphorylation was attenuated by cotreatment with 0.5 mg/kg PD0325901.
|
| Animal Model: | Nude mice (6–8 weeks old)[1] | | Dosage: | 10, 20 and 40 mg/kg alone or in combination with 0.1, 0.3, 0.5, 1.0, or 2.5 mg/kg PD-0325901 | | Administration: | Twice daily for 3 weeks | | Result: | Tissues treated with the RAF inhibitor alone display the microscopic pathology typical of unopposed BRAF inhibition. Hyperplasia in nonglandular stomach epithelium was blocked by PD-0325901. |
| [target]
BRAFV599E | [IC 50]
Braf; CRAF | [storage]
Store at -20° C |
|
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