Glasdegib (PF-04449913) is a potent, and orally bioavailable Smoothened (Smo) inhibitor with IC50 of 5 nM. Phase 2.
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
ANTAGONIST
Mechanism of action
Smoothened homolog antagonist
Product Description
Information
Glasdegib (PF-04449913) is a potent, and orally bioavailableSmoothened (Smo)inhibitor withIC50of 5 nM. Phase 2.
Targets
Smoothened 5 nM
In vitro
In vitro microsomal assays, PF-04449913 have high clearance in rat and low clearance in dog and human, without inhibiting any of the major cytochrome P450 isoforms.
In vivo
In rat and dog, PF-04449913 shows high clearance, and good oral bioavailability.
1.Munchhof MJ, Li Q, Shavnya A, Borzillo GV, Boyden TL, Jones CS, LaGreca SD, Martinez-Alsina L, Patel N, Pelletier K et al.. (2012) Discovery of PF-04449913, a Potent and Orally Bioavailable Inhibitor of Smoothened.. ACS Med Chem Lett, 3 (2):(106-11). [PMID:24900436][10.1021/op500134e]
2.Cortes JE, Douglas Smith B, Wang ES, Merchant A, Oehler VG, Arellano M, DeAngelo DJ, Pollyea DA, Sekeres MA, Robak T et al.. (2018) Glasdegib in combination with cytarabine and daunorubicin in patients with AML or high-risk MDS: Phase 2 study results.. Am J Hematol, 93 (11):(1301-1310). [PMID:30074259][10.1021/op500134e]
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C2328685