Glasdegib | Hedgehog/Smoothened inhibitor | 5+ Citations | In Stock

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Quality Control

Batch: S716002 DMSO]74 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.49%

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS/MSDS
Datasheet

99.49

Related Targets	JAK TGF-beta/Smad Wnt/beta-catenin ERK GSK-3 ROCK PKA Secretase STAT Casein Kinase
Other Hedgehog/Smoothened Inhibitors	SAG (Smoothened Agonist) Hydrochloride Purmorphamine Cyclopamine (11-Deoxojervine) GANT 61 (NSC 136476) SAG (Smoothened Agonist) SANT-1 HPI-4 (Ciliobrevin A) BMS-833923 Taladegib (LY2940680) Ciliobrevin D

Cell Culture, Treatment & Working Concentration

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

Solubility

In vitro
Batch:

DMSO : 74 mg/mL (197.62 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.700mg/ml (9.88mM)	Taking the 1 mL working solution as an example, add 50 μL of 74 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.700mg/ml (9.88mM)	Taking the 1 mL working solution as an example, add 50 μL of 74 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

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

% DMSO

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%

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.

Chemical Information, Storage & Stability

Molecular Weight	374.44	Formula	C₂₁H₂₂N₆O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1095173-27-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	PF-04449913			SMILES	CN1CCC(CC1C2=NC3=CC=CC=C3N2)NC(=O)NC4=CC=C(C=C4)C#N

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC₅₀/Ki	Smoothened 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.
In vivo	In rat and dog, PF-04449913 shows high clearance, and good oral bioavailability.
References	[1] https://pubmed.ncbi.nlm.nih.gov/24900436/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-07-16)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04231851	ACTIVE_NOT_RECRUITING	Acute Myelogenous Leukemia (AML) Due to Therapy; Acute Myeloid Leukemia With Myelodysplasia-Related Changes	University of California, Irvine	2020-02-19	PHASE2
NCT03226418	COMPLETED	Adult Acute Myeloid Leukemia; Secondary Acute Myeloid Leukemia; Therapy-Related Acute Myeloid Leukemia	University of Nebraska	2017-07-07	PHASE2
NCT04655391	WITHDRAWN	Recurrent Acute Myeloid Leukemia	City of Hope Medical Center	2022-06-25	PHASE1
NCT03784014	COMPLETED	Soft Tissue Sarcoma	Institut National de la Santé Et de la Recherche Médicale, France	2019-10-19	PHASE3
NCT03466450	COMPLETED	Glioblastoma	Grupo Español de Investigación en Neurooncología	2018-03-15	PHASE1; PHASE2
NCT04111497	TERMINATED	Chronic Graft Versus Host Disease; Fasciitis	Fred Hutchinson Cancer Center	2019-12-03	PHASE1; PHASE2

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Glasdegib Hedgehog/Smoothened inhibitor

Chemical Structure

Molecular Weight: 374.44