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Chemical Structure : Glasdegib
CAS No.: 1095173-27-5
Catalog No.: PC-36044Not For Human Use, Lab Use Only.
Glasdegib (PF-04449913) is a potent, orally bioavailable smoothened (SMO) inhibitor with IC50 of 5 nM in the Gli-luciferase reporter assays, binds to human SMO (AA181-787) with IC50 of 4 nM.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $128 | In stock | |
| 10 mg | $198 | In stock | |
| 25 mg | Get quote | ||
| 100 mg | Get quote |
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Glasdegib (PF-04449913) is a potent, orally bioavailable smoothened (SMO) inhibitor with IC50 of 5 nM in the Gli-luciferase reporter assays, binds to human SMO (AA181-787) with IC50 of 4 nM.
Glasdegib (PF-04449913) inhibits sonic hedgehog (Shh) stimulated luciferase expression in mouse embryonic fibroblasts with an IC50 of 6.8 nM, significantly reduces medulloblastoma growth in a Ptch1+/-p53+/- allograft model at doses that decreased murine Shh target gene expression.
Glasdegib (PF-04449913) reduced downstream GLI2 protein and cell cycle regulatory gene expression in humanized stromal co-cultures and LSC (leukemia stem cells) xenografts.
| M.Wt | 374.448 | |
| Formula | C21H22N6O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
1-((2R,4R)-2-(1H-benzo[d]imidazol-2-yl)-1-methylpiperidin-4-yl)-3-(4-cyanophenyl)urea |
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1. Munchhof MJ, et al. ACS Med Chem Lett. 2011 Dec 21;3(2):106-11.
2. Wagner AJ, et al. Clin Cancer Res. 2015 Mar 1;21(5):1044-51.
3. Sadarangani A, et al. J Transl Med. 2015 Mar 21;13:98.
4. Martinelli G, et al. Lancet Haematol. 2015 Aug;2(8):e339-46.
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