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Glasdegib

Cat. No. M9205
Glasdegib Structure
Synonym:

PF-04449913

Size Price Availability Quantity
10mM*1mL In DMSO USD 320 In stock
5mg USD 157 In stock
10mg USD 290 In stock
50mg USD 875 In stock
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Quality Control
Biological Activity

Glasdegib (PF-04449913) inhibits sonic hedgehog (Shh) stimulated luciferase expression in mouse embryonic fibroblasts with an IC50 of 6.8 nM. 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, CD34+ cord blood engrafted NSG mice are treated with Glasdegib (PF-04449913), the frequency of human CD45+ cells, progenitors and both myeloid and lymphoid cell fate commitment remained comparable to vehicle treated controls indicating that unlike LSC, normal human HSC cell fate decisions are Hh pathway independent.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 374.44
Formula C21H22N6O
CAS Number 1095173-27-5
Purity 99.28%
Solubility DMSO: ≥ 65 mg/mL
Storage at -20°C
References

GLI2 inhibition abrogates human leukemia stem cell dormancy.
Sadarangani A, et al. J Transl Med. 2015 Mar 21;13:98. PMID: 25889765.

Discovery of PF-04449913, a Potent and Orally Bioavailable Inhibitor of Smoothened.
Munchhof MJ, et al. ACS Med Chem Lett. 2011 Dec 21;3(2):106-11. PMID: 24900436.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Glasdegib, PF-04449913 supplier, Smo, inhibitors

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