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PF-5274857

🥰Excellent
Catalog No. T5465Cas No. 1373615-35-0
Alias PF-5274857 free base

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.

PF-5274857

PF-5274857

🥰Excellent
Purity: 98.53%
Catalog No. T5465Alias PF-5274857 free baseCas No. 1373615-35-0
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 SizePriceAvailabilityQuantity
2 mg$30In Stock
5 mg$42In Stock
10 mg$72In Stock
25 mg$133In Stock
50 mg$217In Stock
100 mg$323In Stock
1 mL x 10 mM (in DMSO)$47In Stock
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Purity:98.53%
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Product Introduction

Bioactivity
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
AliasPF-5274857 free base
Chemical Properties
Molecular Weight436.96
FormulaC20H25ClN4O3S
Cas No.1373615-35-0
SmilesCc1cnc(c(C)c1)-c1cc(ncc1Cl)N1CCN(CC1)C(=O)CCS(C)(=O)=O
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 125 mg/mL (286.07 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.2885 mL11.4427 mL22.8854 mL114.4269 mL
5 mM0.4577 mL2.2885 mL4.5771 mL22.8854 mL
10 mM0.2289 mL1.1443 mL2.2885 mL11.4427 mL
20 mM0.1144 mL0.5721 mL1.1443 mL5.7213 mL
50 mM0.0458 mL0.2289 mL0.4577 mL2.2885 mL
100 mM0.0229 mL0.1144 mL0.2289 mL1.1443 mL

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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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