Glasdegib (PF-04449913)

For research use only.

Catalog No.S7160

1 publication

Glasdegib (PF-04449913) Chemical Structure

CAS No. 1095173-27-5

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

Selleck's Glasdegib (PF-04449913) has been cited by 1 publication

Purity & Quality Control

Choose Selective Hedgehog/Smoothened Inhibitors

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
C3H10T1/2 MUXGeY5kfGmxbjDhd5NigQ>? M1joOlIxKGi{cx?= M4X2eWlvcGmkaYTpc44hd2ZiU33vJIlvKG2xdYPlJGM{UDFyVEGvNkBk\WyuczD1d4lv\yCqdX3hckBz\WOxbXLpcoFvfCCVSFigZZN{\XO|ZXSgZZMh\W[oZXP0JI9vKFOPTz;TTGghfHKjboPp[Y51KHS{YX7zZ5JqeHSrb37hcEBi[3SrdnH0bY9vKGGodHXyJFIxKGi{czDifUBIdGlvbIXjbYZmemG|ZTDy[ZBwenSncjDhd5NigSxiSVO1NF0xNjByNd88US=> M1ftWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUCwOFM3Lz5{NEmwNFQ{PjxxYU6=

... Click to View More Cell Line Experimental Data

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

Protocol

Animal Research:

[1]

- Collapse
  • Animal Models: Rat, dog
  • 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
Smiles CN1CCC(CC1C2=NC3=CC=CC=C3N2)NC(=O)NC4=CC=C(C=C4)C#N

In vivo Formulation Calculator (Clear solution)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04168502 Recruiting Drug: Glasdegib|Drug: Gemtuzumab Ozogamicin Acute Myeloid Leukemia Gruppo Italiano Malattie EMatologiche dell''Adulto September 24 2020 Phase 3
NCT04231851 Recruiting Drug: Glasdegib|Drug: CPX-351 Acute Myelogenous Leukemia (AML) Due to Therapy|Acute Myeloid Leukemia With Myelodysplasia-Related Changes University of California Irvine|Jazz Pharmaceuticals|Pfizer February 19 2020 Phase 2
NCT03627754 Completed Drug: Glasdegib 100 mg single oral dose Hepatic Impairment Pfizer November 5 2018 Phase 1
NCT03466450 Recruiting Drug: PF-04449913|Drug: Temozolomide Oral Capsule Glioblastoma Grupo Español de Investigación en Neurooncología March 15 2018 Phase 1|Phase 2
NCT02367456 Active not recruiting Drug: PF-04449913 (Glasdegib)|Drug: Azacitidine Myelodysplastic Syndrome|Acute Myeloid Leukemia|Chronic Myelomonocytic Leukemia Pfizer April 28 2015 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

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Hedgehog/Smoothened Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID