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Chemical Structure| 1373615-35-0 Chemical Structure| 1373615-35-0

Structure of PF-5274857
CAS No.: 1373615-35-0

Chemical Structure| 1373615-35-0

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PF-5274857 is a potent and selective Smoothened (Smo) antagonist, inhibits Hedgehog (Hh) signaling with IC50 and Ki of 5.8 nM and 4.6 nM, respectively, and can penetrate the blood–brain barrier.

Synonyms: PF-5274857

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Product Details of PF-5274857

CAS No. :1373615-35-0
Formula : C20H25ClN4O3S
M.W : 436.96
SMILES Code : O=C(N1CCN(C2=NC=C(Cl)C(C3=NC=C(C)C=C3C)=C2)CC1)CCS(=O)(C)=O
Synonyms :
PF-5274857
MDL No. :MFCD22420827
InChI Key :BBVNTTZIOTWDSV-UHFFFAOYSA-N
Pubchem ID :56956240

Safety of PF-5274857

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H317-H319
Precautionary Statements:P280-P305+P351+P338

Related Pathways of PF-5274857

Hedgehog

Isoform Comparison

Biological Activity

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL6/NCrl mice Depilated Mice model Topical application 0.5-2% (w/v) Single application, 8 hours duration To evaluate the inhibitory effect of PF-5274857 topical application on Gli1 and Ptch1 mRNA expression in depilated Mice skin. Results showed that PF-5274857 at 2% significantly inhibited Gli1 mRNA expression (approximately 70-80% inhibition), but had weaker inhibition on Ptch1 mRNA. PMC4804317

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.29mL

0.46mL

0.23mL

11.44mL

2.29mL

1.14mL

22.89mL

4.58mL

2.29mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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