Glasdegib

Catalog No.S7160 Batch:S716002

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Technical Data

Formula

C21H22N6O
Molecular Weight 374.44 CAS No. 1095173-27-5
Solubility (25°C)* In vitro DMSO 74 mg/mL (197.62 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% Corn oil
3.7mg/ml 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. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
3.7mg/ml 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. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 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]

Protocol (from reference)

Animal Study:

[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.

Selleck's Glasdegib has been cited by 3 publications

Posttranslational splicing modifications as a key mechanism in cytarabine resistance in acute myeloid leukemia [ Leukemia, 2023, 37(8):1649-1659] PubMed: 37422594
Recreating the Bone Marrow Microenvironment to Model Leukemic Stem Cell Quiescence [ Front Cell Dev Biol, 2021, 9:662868] PubMed: 34589478
Comprehensive pharmacogenomic characterization of gastric cancer. [ Genome Med, 2020, 18;12(1):17] PubMed: 32070411

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.