Glasdegib | 99.49%(HPLC) | In Stock | Hedgehog/Smoothened inhibitor

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

Glasdegib Chemical Structure

CAS: 1095173-27-5

Selleck's Glasdegib has been cited by 3 publications

Purity & Quality Control

Batch: Purity: 99.49%

99.49

Glasdegib Related Products

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Related Compound Libraries	Kinase Inhibitor Library FDA-approved Drug Library Stem Cell Signaling Compound Library GPCR Compound Library Stem Cell Differentiation Compound Library	Click to Expand

Signaling Pathway

Hedgehog/Smoothened Signaling Pathway

Choose Selective Hedgehog/Smoothened Inhibitors

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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
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	Active not recruiting	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

References
[1] Munchhof MJ, et al. ACS Med Chem Lett. 2011, 3(2), 106-111.

References

[1] Munchhof MJ, et al. ACS Med Chem Lett. 2011, 3(2), 106-111.

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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

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

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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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

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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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