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PF-04449913 (Synonyms: Glasdegib)

Catalog No.GC16230

PF-04449913 (PF-04449913) est un inhibiteur lissé puissant et biodisponible par voie orale. PF-04449913 (PF-04449913) se lie au SMO humain (acides aminés 181-787) avec une IC50 de 4 nM.

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PF-04449913 Chemical Structure

Cas No.: 1095173-27-5

Taille Prix Stock Qté
10mM (in 1mL DMSO)
183,00 $US
En stock
10mg
167,00 $US
En stock
50mg
585,00 $US
En stock
100mg
1 077,00 $US
En stock

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Sample solution is provided at 25 µL, 10mM.

Description Protocol Chemical Properties Product Documents Related Products

PF-04449913 is an orally bioavailable inhibitor of smoothened with IC50 value of 5nM [1].

In the Hedgehog (Hh) signaling pathway, the combination of Hh ligands and their receptor Patched leads to the activation of smoothened and subsequently activation of three transcription factors Gli1, Gli2 and Gli3. It then leads to the proliferation of cells. As an antagonist of smoothened, PF-04449913 is developed for treatment of cancer [1].

PF-04449913 is found not to inhibit cytochrome P450 and is negative in Ames and micronucleus assays suggesting it as a safe drug. In the preclinical studies, PF-04449913 shows a half-life of 30 h and an oral bioavailability of 55% in humans. It also has low plasma clearance of 1.03 mL/min/kg and moderate volume of distribution (2.7 L/kg) [1].

References:
[1] 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. Discovery of PF-04449913, a Potent and Orally Bioavailable Inhibitor of Smoothened. ACS Med Chem Lett. 2011 Dec 21;3(2):106-11.

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