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Product name : PF5274857
Item : CRR805
CAS : 1373615-35-0
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Details:
Description of:PF5274857
PF-5274857 is a novel Smo antagonist that specifically binds to Smo with a K(i) of 4.6 ± 1.1 nmol/L and completely blocks the transcriptional activity of the downstream gene Gli1 with an IC(50) of 2.7 ± 1.4 nmol/L in cells. This Smo antagonist showed robust antitumor activity in a mouse model of medulloblastoma with an in vivo IC(50) of 8.9 ± 2.6 nmol/L. The downregulation of Gli1 is closely linked to the tumor growth inhibition in patched(+/-) medulloblastoma mice. Mathematical analysis of the relationship between the drug's pharmacokinetics and Gli1 pharmacodynamics in patched(+/-) medulloblastoma tumor models yielded similar tumor and skin Gli1 IC(50) values, suggesting that skin can be used as a surrogate tissue for the measurement of tumor Gli1 levels. In addition, 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. The brain permeability of PF-5274857 was also confirmed and quantified in nontumor-bearing preclinical species with an intact blood-brain barrier. PF-5274857 was orally available and metabolically stable in vivo. 

Theoretical analysis:PF5274857
CAS No.:1373615-35-0
Formula:C20H25ClN4O3S
M.Wt:436.96
Purity:>98%
Storage:RT

Availability and price:PF5274857
Pakage:25mg/50mg/100mg/250mg/500mg/1g/5g
Stock : in stock
We offer significant discount for larger quantity order.
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sales@chemrenpharm.com

Quality control data:
Quality Control by H-NMR,C-NMR,LC-MS,HPLC.
Product will be shipped with supporting analytical data.
Fast delivery about 4-5 working days


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