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PF-5274857

  Cat. No.:  DC12373   Featured
Chemical Structure
1373615-35-0
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More than 5000 active chemicals with high quality for research!
Field of application
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.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1373615-35-0
Synonyms: PF-5274857,PF 5274857,PF5274857
SMILES: O=C(N1CCN(C2=NC=C(Cl)C(C3=NC=C(C)C=C3C)=C2)CC1)CCS(=O)(C)=O
Formula: C20H25ClN4O3S
M.Wt: 436.96
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: 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.
Target: IC50 value: 5.8 nM Target: Smoothened
In Vivo: PF-5274857 shows significant dose-dependent tumor growth inhibition (TGI) and induces tumor regression at high doses(>10 mg/kg)., PF-5274857 downregulates Gli1, Gli2, Ptch1, and Ptch2 gene expression levels to various degrees with maximal effects being achieved between 6 and 12 hours post-dose (Gli1 is the most sensitive gene), whereas PF-5274857 has little effect on Smo levels. In skin tissue, downregulation of Gli1 and Gli2 is also observed with a similar time course by PF-5274857. The model-derived drug concentration for half maximal inhibition of the tumor Gli1 mRNA production rate (IC50) by PF-5274857 is determined to be 8.9 nM in the Ptch+/?p53+/? medulloblastoma allograft mice, which mathematically corresponds to tumor regression of 119% TGI after 6 days of plasma exposure at this concentration. In the Ptch+/?p53?/? medulloblastoma allograft mice, the IC50 value is estimated to be 3.5 nM, consistent with the Ptch+/?p53+/? results. PF-5274857 is also able to cross the blood–brain barrier in rats within 4 hours post-dose [1].
In Vitro: PF-5274857 completely inhibits Shh-induced Hh pathway activity with IC50 of 2.7 nM measured by the transcriptional activity of Smo downstream gene Gli1 in MEF cells. The μ-opioid receptor is weakly inhibited by PF-5274857 with a dissociation constant of 36 μM subsequently determined in a functional assay [1].
References: [1]. Rohner A, 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. Mol Cancer Ther. 2012, 11(1), 57-65.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC4232 Vismodegib (GDC-0449) Vismodegib (formerly GDC-0449) is a hedgehog antagonist, is also an orally bioavailable small molecule with potential antineoplastic activity.
DC8391 Smoothened Agonist (SAG) HCl Smoothened Agonist (SAG) HCl is a cell-permeable Smoothened (Smo) agonist with EC50 of 3 nM in Shh-LIGHT2 cells.
DC12276 Saridegib (IPI-926; Patidegib) Saridegib is a potent and specific inhibitor of Smoothened (Smo), a key signaling transmembrane protein in the Hedgehog (Hh) pathway.
DC8327 SANT-1 SANT-1 is a membrane permeable antagonist of the Shh (Sonic Hedgehog) signaling pathway by direct binding to Smo.
DC7255 Purmorphamine Purmorphamine, which directly binds and activates Smoothened, blocks BODIPY-cyclopamine binding to Smo with IC50 of ~ 1.5 μM and also is an inducer of osteoblast differentiation with EC50 of 1 μM.
DC12373 PF-5274857 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.
DC9707 MK-4101 MK-4101 is a potent SMO Inhibitor of the Hedgehog Pathway, highly active against Medulloblastoma and Basal Cell Carcinoma.
DC7191 LY-2940680(Taladegib) LY2940680 binds to the Smoothened (Smo) receptor and potently inhibits Hedgehog (Hh) signaling.
DC7185 LDE225 Diphosphate LDE225 (NVP-LDE225) is a Smoothened (Smo) antagonist, inhibiting Hedgehog (Hh) signaling with IC50 of 1.3 nM (mouse) and 2.5 nM (human), respectively. Phase 3.
DC8493 NVP-LDE225(Erismodegib) LDE225 (NVP-LDE225) is a Smoothened (Smo) antagonist, inhibiting Hedgehog (Hh) signaling with IC50 of 1.3 nM (mouse) and 2.5 nM (human), respectively. Phase 3.
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