PF-04217903
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 202221

CAS#: 956905-27-4 (free base); 956906-93-7 (mesylate)

Description: PF-04217903 is a MET tyrosine kinase inhibitor, is also a n orally bioavailabe, small-molecule tyrosine kinase inhibitor of the proto-oncogene c-Met (hepatocyte growth factor receptor [HGFR]) with potential antineoplastic activity. c-Met inhibitor PF-04217903 selectively binds to and inhibits c-Met, disrupting the c-Met signaling pathway, which may result in the inhibition of tumor cell growth, migration and invasion of tumor cells, and the induction of death in tumor cells expressing c-Met.


Price and Availability

Size
Price

5mg
USD 110
50mg
USD 450
500mg
USD 1950
Size
Price

10mg
USD 150
100mg
USD 750
1g
USD 2850
Size
Price

25mg
USD 250
200mg
USD 1150
5g
Ask price

PF-04217903, purity > 98%, is in stock. The same day shipping out after order is received. Delivery time: overnight (USA/Canada); 3-5 days (worldwide). Shipping fee: $30.00 (USA); from $45.00 (Canada); from $70.00 (international).


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 202221
Name: PF-04217903
CAS#: 956905-27-4 (free base); 956906-93-7 (mesylate)
Chemical Formula: C19H16N8O
Exact Mass: 372.14471
Molecular Weight: 372.38
Elemental Analysis: C, 61.28; H, 4.33; N, 30.09; O, 4.30


Synonym: PF04217903; PF 04217903; PF-04217903; PF4217903; PF-4217903; PF 4217903.

IUPAC/Chemical Name: 2-(4-(1-(quinolin-6-ylmethyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl)-1H-pyrazol-1-yl)ethanol

SMILES Code: OCCN1N=CC(C2=CN=C3C(N(CC4=CC=C5N=CC=CC5=C4)N=N3)=N2)=C1


Technical Data

Appearance:
white solid powder

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

Certificate of Analysis:

Safety Data Sheet (MSDS):

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).

Harmonized System Code:
293490


Additional Information

 
 
 


References

1: Cui JJ, McTigue M, Nambu M, Tran-Dubé M, Pairish M, Shen H, Jia L, Cheng H, Hoffman J, Le P, Jalaie M, Goetz GH, Ryan K, Grodsky N, Deng YL, Parker M, Timofeevski S, Murray BW, Yamazaki S, Aguirre S, Li Q, Zou H, Christensen J. Discovery of a novel class of exquisitely selective mesenchymal-epithelial transition factor (c-MET) protein kinase inhibitors and identification of the clinical candidate 2-(4-(1-(quinolin-6-ylmethyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl)-1H-pyrazol-1 -yl)ethanol (PF-04217903) for the treatment of cancer. J Med Chem. 2012 Sep 27;55(18):8091-109. Epub 2012 Sep 10. Erratum in: J Med Chem. 2012 Nov 26;55(22):10314. PubMed PMID: 22924734.

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.

3: Sennino B, Ishiguro-Oonuma T, Wei Y, Naylor RM, Williamson CW, Bhagwandin V, Tabruyn SP, You WK, Chapman HA, Christensen JG, Aftab DT, McDonald DM. Suppression of tumor invasion and metastasis by concurrent inhibition of c-Met and VEGF signaling in pancreatic neuroendocrine tumors. Cancer Discov. 2012 Mar;2(3):270-87. doi: 10.1158/2159-8290.CD-11-0240. Epub 2012 Feb 24. PubMed PMID: 22585997; PubMed Central PMCID: PMC3354652.

4: Zou HY, Li Q, Lee JH, Arango ME, Burgess K, Qiu M, Engstrom LD, Yamazaki S, Parker M, Timofeevski S, Cui JJ, McTigue M, Los G, Bender SL, Smeal T, Christensen JG. Sensitivity of selected human tumor models to PF-04217903, a novel selective c-Met kinase inhibitor. Mol Cancer Ther. 2012 Apr;11(4):1036-47. doi: 10.1158/1535-7163.MCT-11-0839. Epub 2012 Mar 2. PubMed PMID: 22389468.

5: Dillon R, Nilsson CL, Shi SD, Lee NV, Krastins B, Greig MJ. Discovery of a novel B-Raf fusion protein related to c-Met drug resistance. J Proteome Res. 2011 Nov 4;10(11):5084-94. doi: 10.1021/pr200498v. Epub 2011 Oct 12. PubMed PMID: 21936566.

6: Yamazaki S, Skaptason J, Romero D, Vekich S, Jones HM, Tan W, Wilner KD, Koudriakova T. Prediction of oral pharmacokinetics of cMet kinase inhibitors in humans: physiologically based pharmacokinetic model versus traditional one-compartment model. Drug Metab Dispos. 2011 Mar;39(3):383-93. doi: 10.1124/dmd.110.035857. Epub 2010 Nov 23. PubMed PMID: 21098644.

7: Timofeevski SL, McTigue MA, Ryan K, Cui J, Zou HY, Zhu JX, Chau F, Alton G, Karlicek S, Christensen JG, Murray BW. Enzymatic characterization of c-Met receptor tyrosine kinase oncogenic mutants and kinetic studies with aminopyridine and triazolopyrazine inhibitors. Biochemistry. 2009 Jun 16;48(23):5339-49. doi: 10.1021/bi900438w. PubMed PMID: 19459657.