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PF-5274857 (PF-5274857 free base) is an effective and selective hedgehog signaling pathway inhibitor (IC50: 5.8 nM and a Ki: 4.6 nM). PF-5274857 is a potentially attractive clinical candidate for the treatment of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway.PF-5274857 was found to effectively penetrate the blood-brain barrier and inhibit Smo activity in the brain of primary medulloblastoma mice, resulting in improved animal survival rates. PF-5274857 was orally available and metabolically stable in vivo.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 2 mg | $30 | In Stock | In Stock | |
| 5 mg | $42 | In Stock | In Stock | |
| 10 mg | $72 | In Stock | In Stock | |
| 25 mg | $133 | In Stock | In Stock | |
| 50 mg | $217 | In Stock | In Stock | |
| 100 mg | $323 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $47 | In Stock | In Stock |
| Description | PF-5274857 (PF-5274857 free base) is an effective and selective hedgehog signaling pathway inhibitor (IC50: 5.8 nM and a Ki: 4.6 nM). PF-5274857 is a potentially attractive clinical candidate for the treatment of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway.PF-5274857 was found to effectively penetrate the blood-brain barrier and inhibit Smo activity in the brain of primary medulloblastoma mice, resulting in improved animal survival rates. PF-5274857 was orally available and metabolically stable in vivo. |
| Targets&IC50 | Smo:5.8 nM (IC50), Smo:Ki: 4.6 nM |
| Synonyms | PF-5274857 free base |
| Molecular Weight | 436.96 |
| Formula | C20H25ClN4O3S |
| Cas No. | 1373615-35-0 |
| Smiles | Cc1cnc(c(C)c1)-c1cc(ncc1Cl)N1CCN(CC1)C(=O)CCS(C)(=O)=O |
| Relative Density. | no data available |
| Color | White |
| Appearance | Solid |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 125 mg/mL (286.07 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (9.15 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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