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GPCR/G Protein Hedgehog/Smoothened Glasdegib

Glasdegib

Catalog No. T6514   CAS 1095173-27-5
Synonyms: PF-04449913,

Glasdegib (PF-04449913) is a potent, and orally bioavailable Smoothened (Smo) inhibitor with IC50 of 5 nM. Phase 2.

Glasdegib, CAS 1095173-27-5
Pack Size Availability Price/USD Quantity
1 mg In stock 50.00
2 mg In stock 64.00
5 mg In stock 115.00
10 mg In stock 228.00
25 mg In stock 411.00
50 mg In stock 667.00
1 mL * 10 mM (in DMSO) In stock 260.00
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Purity 98.00%
Biological Description
Chemical Properties
Storage & Solubility Information
Description Glasdegib (PF-04449913) is a potent, and orally bioavailable Smoothened (Smo) inhibitor with IC50 of 5 nM. Phase 2.
Targets&IC50 Smoothened : ic50 5nM
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]
Cell Research
PF-04449913 is dissolved in DMSO and stored, and then diluted with appropriate medium before use[1]. Normal or BC CML CD34+ cells are plated on confluent mitomycin-C treated SL/M2 cells with vehicle, PF-04449913 (1 μM), Dasatinib (50 nM), or combination treatment. Mouse bone marrow stromal cell lines, M2-10B4 (M2) and SL/SL (SL) are treated with mitomycin-C (1 mg/mL) and plated in a 1:1 mixture at a total concentration of 100,000 cells/mL one day prior to co-culture with 10,000-20,000 CD34+ BC CML or normal progenitors. After 1 week of culture, progenitors are FACS sorted into hematopoietic progenitor assays and colonies are scored at 14 days. To assess survival of normal human hematopoietic stem and progenitor cells, irradiated (20 Gray) OP9 (M2 clone) stromal cells are co-cultured with 50,000 human CD34+ cord blood cells, vehicle or PF-04449913 in AlphaMEM with 20% Hyclone FBS, 1% pen strep glutamine and supplemented with 50 ng/mL SCF, 10 ng/mL thrombopoietin, and 10 ng/mL Flt3 and quantified by weekly FACS analysis[1].
Animal Research
Animal Model: Rat, dog
Synonyms PF-04449913 ,
Purity 98.00%
Molecular Weight 374.44
Formula C21H22N6O
CAS No. 1095173-27-5

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 44 mg/mL (117.5 mM)

Ethanol: <1 mg/mL

Water: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

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

Related Products

Related compounds with same targets
Glasdegib ALLO-2 GANT 58 SAG hydrochloride (912545-86-9(free base)) JK184 Taladegib BMS833923 NVP-LDE225

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Answers to questions you may have can be found in the Inhibitor Handling Instructions. Topics include how to prepare stock solutions, how to store Products, and issues that need special attention for cell-based assays and animal experiments.