PF-5274857 |
| Catalog No.GC13280 |
Smo antagonist,potent and selective
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1373615-35-0
Sample solution is provided at 25 µL, 10mM.
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PF-5274857 is an inhibitor of hedgehog (Hh) signaling pathway and is identified as a potent and selective antagonist of Smoothened (Smo) with an IC50 of 5.8 nM.
Smoothened, a G protein-coupled receptor, is a component of the hedgehog signaling pathway and is conserved from flies to humans. This protein is the molecular target of the teratogen cyclopamine. SMO can act as an oncogene and the activation of SMO mutations leads to unregulated activation of the hedgehog pathway and cancer.
In MEF cells, treatment of PF-5274857 completely blocked Shh-induced Hh pathway activity, which was measured by the transcriptional activity of Smo downstream gene Gli1.
In vivo, PF-5274857 showed anti-tumor activity in a mouse medulloblastoma model with IC50 of 8.9 nM. PF-5274857 also shows significant dose-dependent tumor growth inhibition (TGI) and induces tumor regression. In skin tissue, downregulation of Gli1 and Gli2 is also observed with a similar time course by PF-52748571.
Reference:
1. Rohner A, Spilker ME, Lam JL, et al. Effective targeting of Hedgehog signaling in a medulloblastoma model with PF-5274857, a potent and selective Smoothened antagonist that penetrates the blood-brain barrier. Molecular cancer therapeutics.2012;11(1):57-65.
| Cas No. | 1373615-35-0 | SDF | |
| Chemical Name | 1-[4-[5-chloro-4-(3,5-dimethylpyridin-2-yl)pyridin-2-yl]piperazin-1-yl]-3-methylsulfonylpropan-1-one | ||
| Canonical SMILES | CC1=CC(=C(N=C1)C2=CC(=NC=C2Cl)N3CCN(CC3)C(=O)CCS(=O)(=O)C)C | ||
| Formula | C20H25ClN4O3S | M.Wt | 436.96 |
| Solubility | ≥ 19.65mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.2885 mL | 11.4427 mL | 22.8854 mL |
| 5 mM | 457.7 μL | 2.2885 mL | 4.5771 mL |
| 10 mM | 228.9 μL | 1.1443 mL | 2.2885 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 37 reference(s) in Google Scholar.)
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