Glasdegib (PF-04449913)

Catalog No.S7160

For research use only.

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

Glasdegib (PF-04449913) Chemical Structure

CAS No. 1095173-27-5

Selleck's Glasdegib (PF-04449913) has been cited by 2 Publications

Purity & Quality Control

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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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
C3H10T1/2 NUDk[pdbTnWwY4Tpc44h[XO|YYm= MoDGNlAhcHK| NIDqZ|ZKdmirYnn0bY9vKG:oIGPtc{BqdiCvb4Xz[UBEO0hzMGSxM|Ih[2WubIOgeZNqdmdiaIXtZY4hemWlb33ibY5idnRiU1jIJIF{e2W|c3XkJIF{KGWoZnXjeEBwdiCVTV:vV2hJKHS{YX7zbYVvfCC2cnHud4NzcXC2aX;uZYwh[WO2aY\heIlwdiCjZoTldkAzOCCqcoOgZpkhT2yrLXz1Z4ln\XKjc3WgdoVxd3K2ZYKgZZN{[XluIFnDOVA:OC5yMEZOwG0> MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyMESzOkc,OjR7MEC0N|Y9N2F-
In vivo In rat and dog, PF-04449913 shows high clearance, and good oral bioavailability. [1]

Protocol (from reference)

Animal Research:

[1]

  • 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.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 374.44
Formula

C21H22N6O

CAS No. 1095173-27-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN1CCC(CC1C2=NC3=CC=CC=C3N2)NC(=O)NC4=CC=C(C=C4)C#N

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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 Active not recruiting Drug: PF-04449913|Drug: Temozolomide Oral Capsule Glioblastoma Grupo Español de Investigación en Neurooncología March 15 2018 Phase 1|Phase 2
NCT02367456 Completed Drug: PF-04449913 (Glasdegib)|Drug: Azacitidine Myelodysplastic Syndrome|Acute Myeloid Leukemia|Chronic Myelomonocytic Leukemia Pfizer April 28 2015 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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