Home Stem Cells & Wnt Hedgehog/Smoothened inhibitor Glasdegib For research use only.

Glasdegib

Synonyms: PF-04449913

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

Glasdegib Chemical Structure

Glasdegib Chemical Structure

CAS No. 1095173-27-5

Purity & Quality Control

Glasdegib Related Products

Signaling Pathway

Hedgehog/Smoothened Signaling Pathways

Hedgehog/Smoothened Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
C3H10T1/2 Function assay 20 hrs Inhibition of Smo in mouse C3H10T1/2 cells using human recombinant SHH assessed as effect on SMO/SHH transient transcriptional activation after 20 hrs by Gli-luciferase reporter assay, IC50=0.005μM 24900436
Click to View More Cell Line Experimental Data

Biological Activity

Description Glasdegib 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 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 vivo In rat and dog, PF-04449913 shows high clearance, and good oral bioavailability. [1]
Animal Research 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.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04168502 Recruiting
Acute Myeloid Leukemia
Gruppo Italiano Malattie EMatologiche dell''Adulto
 September 24 2020 Phase 3
NCT04231851 Recruiting
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
Hepatic Impairment
Pfizer
 November 5 2018 Phase 1
NCT03466450 Completed
Glioblastoma
Grupo Español de Investigación en Neurooncología
 March 15 2018 Phase 1|Phase 2
NCT02367456 Completed
Myelodysplastic Syndrome|Acute Myeloid Leukemia|Chronic Myelomonocytic Leukemia
Pfizer
 April 28 2015 Phase 1

Chemical Information & Solubility

Molecular Weight 374.44 Formula

C21H22N6O
CAS No. 1095173-27-5 SDF Download Glasdegib SDF
Smiles CN1CCC(CC1C2=NC3=CC=CC=C3N2)NC(=O)NC4=CC=C(C=C4)C#N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 74 mg/mL ( (197.62 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

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.

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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