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PF-04880594

Catalog No.GC15821

RAF inhibitor

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PF-04880594 Chemical Structure

Cas No.: 1111636-35-1

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5mg
$48.00
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25mg
$196.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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 [1].

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 [2]. 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 [3].

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 [3].

References:
[1].  Palmer C, Cui J, Deal J, Gu D, Guo C, Kephart S, et al. Discovery of potent, selective inhibitors of mutant B-Raf. (Abstract # MEDI-251). Abstracts of Papers, 242nd ACS National Meeting & Exposition 2011.
[2].  Lee, N. V. Lira, M. E. Pavlicek, A., et al. A novel SND1-BRAF fusion confers resistance to c-Met inhibitor PF-04217903 in GTL16 cells through [corrected] MAPK activation [J]. PLoS One, 2012, 7(6): e39653.
[3].  Vince R. Torti, Donald Wojciechowicz, Wenyue Hu, et al. Epithelial Tissue Hyperplasia Induced by the RAF Inhibitor PF-04880594 Is Attenuated by a Clinically Well-Tolerated Dose of the MEK Inhibitor PD-0325901 [J]. Mol Cancer Ther, 2012, 11(10):2274-2283.

Chemical Properties

Cas No. 1111636-35-1 SDF
Chemical Name 3-[[4-[1-(2,2-difluoroethyl)-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrazol-4-yl]pyrimidin-2-yl]amino]propanenitrile
Canonical SMILES C1=CNC2=NC=C(C=C21)C3=NN(C=C3C4=NC(=NC=C4)NCCC#N)CC(F)F
Formula C19H16F2N8 M.Wt 394.38
Solubility Soluble in DMSO Storage Store at -20° C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.5356 mL 12.6781 mL 25.3563 mL
5 mM 0.5071 mL 2.5356 mL 5.0713 mL
10 mM 0.2536 mL 1.2678 mL 2.5356 mL
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Reviews

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Average Rating: 5 ★★★★★ (Based on Reviews and 39 reference(s) in Google Scholar.)

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