PF-04880594
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 406212

CAS#: 1111636-35-1

Description: 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.

Chemical Structure

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PF-04880594
CAS# 1111636-35-1
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 406212
Name: PF-04880594
CAS#: 1111636-35-1
Chemical Formula: C19H16F2N8
Exact Mass: 394.15
Molecular Weight: 394.390
Elemental Analysis: C, 57.86; H, 4.09; F, 9.63; N, 28.41

Price and Availability

Size Price Availability Quantity
5mg USD 260 2 Weeks
25mg USD 750 2 Weeks
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Synonym: PF04880594; PF-04880594; PF 04880594.

IUPAC/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

InChi Key: HFYMVDKBZONUOJ-UHFFFAOYSA-N

InChi Code: 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)

SMILES Code: N#CCCNC1=NC=CC(C2=CN(CC(F)F)N=C2C3=CN=C(NC=C4)C4=C3)=N1

Appearance: Solid powder

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:         

Product Data:
Product Data
Instruction:
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Biological target: PF-04880594 is a RAF inhibitor.
In vitro activity: This study showed that the RAF inhibitor PF-04880594 induces ERK phosphorylation and RAF dimerization in those epithelial tissues that undergo hyperplasia. This study also showed that PF-04880594 stimulates production of the inflammatory cytokine interleukin 8 in HL-60 cells, suggesting a possible mechanism for the skin flushing observed in dogs.3 Reference: Mol Cancer Ther. 2012 Oct;11(10):2274-83. https://pubmed.ncbi.nlm.nih.gov/22752429/
In vivo activity: TBD

Preparing Stock Solutions

The following data is based on the product molecular weight 394.39 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: Torti VR, Wojciechowicz D, Hu W, John-Baptiste A, Evering W, Troche G, Marroquin LD, Smeal T, Yamazaki S, Palmer CL, Burns-Naas LA, Bagrodia S. Epithelial tissue hyperplasia induced by the RAF inhibitor PF-04880594 is attenuated by a clinically well-tolerated dose of the MEK inhibitor PD-0325901. Mol Cancer Ther. 2012 Oct;11(10):2274-83. doi: 10.1158/1535-7163.MCT-11-0984. Epub 2012 Jul 2. PMID: 22752429.
In vitro protocol: Torti VR, Wojciechowicz D, Hu W, John-Baptiste A, Evering W, Troche G, Marroquin LD, Smeal T, Yamazaki S, Palmer CL, Burns-Naas LA, Bagrodia S. Epithelial tissue hyperplasia induced by the RAF inhibitor PF-04880594 is attenuated by a clinically well-tolerated dose of the MEK inhibitor PD-0325901. Mol Cancer Ther. 2012 Oct;11(10):2274-83. doi: 10.1158/1535-7163.MCT-11-0984. Epub 2012 Jul 2. PMID: 22752429.
In vivo protocol: TBD

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1: Torti VR, Wojciechowicz D, Hu W, John-Baptiste A, Evering W, Troche G, Marroquin LD, Smeal T, Yamazaki S, Palmer CL, Burns-Naas LA, Bagrodia S. Epithelial tissue hyperplasia induced by the RAF inhibitor PF-04880594 is attenuated by a clinically well-tolerated dose of the mek inhibitor PD-0325901. Mol Cancer Ther. 2012 Oct;11(10):2274-83. doi: 10.1158/1535-7163.MCT-11-0984. Epub 2012 Jul 2. PubMed PMID: 22752429.

2: Lee NV, Lira ME, Pavlicek A, Ye J, Buckman D, Bagrodia S, Srinivasa SP, Zhao Y, Aparicio S, Rejto PA, Christensen JG, Ching KA. A novel SND1-BRAF fusion confers resistance to c-Met inhibitor PF-04217903 in GTL16 cells though MAPK activation. PLoS One. 2012;7(6):e39653. doi:  10.1371/journal.pone.0039653. Epub 2012 Jun 22. PubMed PMID: 22745804; PubMed Central PMCID: PMC3382171.