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PF-04449913 CAS: 1095173-27-5

Category: Inhibitors
Product Name: PF-04449913
Cat No: I000401
CAS No: 1095173-27-5
Synonyms: 1-[(2R,4R)-2-(1H-benzimidazol-2-yl)-1-methylpiperidin-4-yl]-3-(4-cyanophenyl)urea
Molecular Formula: C21H22N6O
Molecular Weight: 374.4
SMILES: O=C(N[C@@H]1CCN(C)[C@@H](C2=NC(C=CC=C3)=C3N2)C1)NC4=CC=C(C#N)C=C4
InChI: None
Solubility: in DMSO > 10 mM
Target: Smoothened
IC50: 5 nM [1]
Storage: Store at -20°C
CAS 1095173-27-5,PF-04449913
  • Description

PF-04449913 is a potent and orally bioavailable inhibitor of smoothened with IC50 of 5 nM(Gli-luciferase reporter reporter in C3H10T1/2); the hedgehog pathway inhibitor.
IC50 value: 5 nM [1]
Target: smoothened
PF-04449913, a Smoothened inhibitor was identified possessing excellent potency and physical properties that translate to an attractive predicted human pharmacokinetic profile. PF-04449913 was advanced to in vivo tumor growth inhibition studies, preclinical safety studies, and ultimately to human clinical trials. These results will be reported in separate disclosures.

  • Spec

Appearance:white solid powder
Purity: > 98%

  • References

1:Metabolism, excretion and pharmacokinetics of [14C]glasdegib (PF-04449913) in healthy volunteers following oral administration. Lam JL, Vaz A, Hee B, Liang Y, Yang X, Shaik MN.Xenobiotica. 2017 Jan 3:1-13. doi: 10.1080/00498254.2016.1261307. [Epub ahead of print] PMID: 27866461
2:The human Smoothened inhibitor PF-04449913 induces exit from quiescence and loss of multipotent Drosophila hematopoietic progenitor cells. Giordani G, Barraco M, Giangrande A, Martinelli G, Guadagnuolo V, Simonetti G, Perini G, Bernardoni R.Oncotarget. 2016 Aug 23;7(34):55313-55327. doi: 10.18632/oncotarget.10879. PMID: 27486815 Free PMC Article
3:Treatment with PF-04449913, an oral smoothened antagonist, in patients with myeloid malignancies: a phase 1 safety and pharmacokinetics study. Martinelli G, Oehler VG, Papayannidis C, Courtney R, Shaik MN, Zhang X, O'Connell A, McLachlan KR, Zheng X, Radich J, Baccarani M, Kantarjian HM, Levin WJ, Cortes JE, Jamieson C.Lancet Haematol. 2015 Aug;2(8):e339-46. doi: 10.1016/S2352-3026(15)00096-4. Epub 2015 Jul 26. PMID: 26688487
4:A phase I study of PF-04449913, an oral hedgehog inhibitor, in patients with advanced solid tumors. Wagner AJ, Messersmith WA, Shaik MN, Li S, Zheng X, McLachlan KR, Cesari R, Courtney R, Levin WJ, El-Khoueiry AB.Clin Cancer Res. 2015 Mar 1;21(5):1044-51. doi: 10.1158/1078-0432.CCR-14-1116. Epub 2014 Nov 11. PMID: 25388167 Free Article
5:Evaluation of the effect of food and ketoconazole on the pharmacokinetics of the smoothened inhibitor PF-04449913 in healthy volunteers. Shaik MN, LaBadie RR, Rudin D, Levin WJ.Cancer Chemother Pharmacol. 2014 Aug;74(2):411-8. doi: 10.1007/s00280-014-2502-0. Epub 2014 Jun 19. PMID: 24944041
6:Discovery of PF-04449913, a Potent and Orally Bioavailable Inhibitor of Smoothened. Munchhof MJ, Li Q, Shavnya A, Borzillo GV, Boyden TL, Jones CS, LaGreca SD, Martinez-Alsina L, Patel N, Pelletier K, Reiter LA, Robbins MD, Tkalcevic GT.ACS Med Chem Lett. 2011 Dec 21;3(2):106-11. doi: 10.1021/ml2002423. eCollection 2012 Feb 9. PMID: 24900436 Free PMC Article

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