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PF-04880594

Catalog No. T21602   CAS 1111636-35-1

PF-04880594 is a potent and selective RAF inhibitor which inhibits both wild-type and mutant BRAF and CRAF. PF-04880594 exhibits antitumor activity [1].

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PF-04880594 Chemical Structure
PF-04880594, CAS 1111636-35-1
Pack Size Availability Price/USD Quantity
25 mg 6-8 weeks $ 1,520.00
50 mg 6-8 weeks $ 1,980.00
100 mg 6-8 weeks $ 2,500.00
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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
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Biological Description
Chemical Properties
Storage & Solubility Information
Description PF-04880594 is a potent and selective RAF inhibitor which inhibits both wild-type and mutant BRAF and CRAF. PF-04880594 exhibits antitumor activity [1].
In vitro PF-04880594 (100 nM, 48 h) causes ERK activation and stimulation of IL-8 release, both blocked by the treatment of PD-0325901 [1]. Western Blot Analysis [1] Cell Line: HL-60 Concentration: 100 nM alone or in combination with 100 nM PD-0325901 Incubation Time: 48 h Result: Induced ERK phosphorylation and induced IL-8 production. PD-0325901 treatment blocked the induction.
In vivo PF-04880594, administered at 10 mg/kg, was observed to induce ERK phosphorylation and BRAF-CRAF dimerization across multiple epithelial tissues in mice, with the effects being mitigable by co-treatment with PD0325901. Additionally, when administered at doses ranging from 0-40 mg/kg twice daily over three weeks, PF-04880594 led to epithelial hyperplasia in mice, a condition that was effectively prevented by PD0325901. In experiments involving nude mice, a single day’s administration of 10 mg/kg PF-04880594, followed by a dose 2 hours before necropsy on the next day, resulted in ERK phosphorylation within urinary bladder, tongue, skin, and esophagus tissues, which was attenuated by a concurrent administration of 0.5 mg/kg PD0325901. Continuous administration of PF-04880594, at dosages of 10, 20, and 40 mg/kg in combination with varying doses of PD-0325901 (0.1, 0.3, 0.5, 1.0, or 2.5 mg/kg) for three weeks, highlighted microscopic pathologies typical of unopposed BRAF inhibition and reported that hyperplasia in nonglandular stomach epithelium could be obstructed by PD0325901.
Molecular Weight 394.38
Formula C19H16F2N8
CAS No. 1111636-35-1

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Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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Keywords

PF-04880594 1111636-35-1 PF04880594 PF 04880594 inhibitor inhibit

 

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