Glasdegib (PF-04449913)

Catalog No.S7160

Glasdegib (PF-04449913) Chemical Structure

Molecular Weight(MW): 374.44

Glasdegib (PF-04449913) is a potent, and orally bioavailable Smoothened (Smo) inhibitor with IC50 of 5 nM. Phase 2.

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Biological Activity

Description Glasdegib (PF-04449913) is a potent, and orally bioavailable Smoothened (Smo) inhibitor with IC50 of 5 nM. Phase 2.
Targets
Smoothened [1]
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. [1]

In vivo In rat and dog, PF-04449913 shows high clearance, and good oral bioavailability. [1]

Protocol

Animal Research:

[1]

+ Expand
  • Animal Models: Rat, dog
  • Formulation: 10% EtOH/20% PEG400/70% PBS (i.v.); 0.5% methylcellulose in water (p.o.)
  • Dosages: 1 mg/kg (Rat); 0.5 mg/kg (dog i.v.); 3 mg/kg (dog p.o.)
  • Administration: i.v. or p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 47 mg/mL (125.52 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 374.44
Formula

C21H22N6O

CAS No. 1095173-27-5
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03627754 Recruiting Hepatic Impairment Pfizer November 5 2018 Phase 1
NCT03596567 Completed Renal Impairment Pfizer May 17 2018 Phase 1
NCT03416179 Recruiting Leukemia Myeloid Acute Pfizer April 20 2018 Phase 3
NCT03466450 Recruiting Glioblastoma Grupo Español de Investigación en Neurooncología March 15 2018 Phase 1|Phase 2
NCT03390296 Recruiting Acute Myeloid Leukemia M.D. Anderson Cancer Center|Pfizer December 27 2017 Phase 2
NCT03270878 Completed Healthy Volunteer Study Pfizer September 7 2017 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Hedgehog/Smoothened Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID