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Glasdegib Hedgehog/Smoothened inhibitor

Cat.No.S7160

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

Chemical Structure

Molecular Weight: 374.44

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.49%

99.49

Related Targets	JAK STAT TGF-beta/Smad Wnt/beta-catenin ERK GSK-3 Casein Kinase Notch ROCK PKA Secretase PORCN OCT KLF Stemness kinase SFRP Fascin
Related Products	Cyclopamine (11-Deoxojervine) GANT61 SAG Hydrochloride Purmorphamine SANT-1 SAG BMS-833923 HPI-4 (Ciliobrevin A) Taladegib (LY2940680) PF-5274857 Jervine Ciliobrevin D MK-4101 JK184 ARL 13B Antibody [F4B9] Shh Antibody [L19M13] MNX1/HB9 Antibody [M23L14] ALLO-2 Sonic Hedgehog Antibody [N3D2] GLI1 Antibody [A19H14] GANT58(NSC75503) MRT-81 MRT 10 PTCH1 Antibody [K3H23]

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

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

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.
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.

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

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.

Mechanism of Action

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

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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