1. Stem Cell/Wnt
  2. Smo
  3. PF-5274857 hydrochloride

PF-5274857 hydrochloride 

Cat. No.: HY-13459A
Handling Instructions

PF-5274857 hydrochloride is a potent, selective, orally active and brain-penetrant antagonist of Smo, with an IC50 of 5.8 nM and Ki of 4.6 nM. PF-5274857 hydrochloride has potential for research of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway.

For research use only. We do not sell to patients.

PF-5274857 hydrochloride Chemical Structure

PF-5274857 hydrochloride Chemical Structure

CAS No. : 1613439-62-5

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Description

PF-5274857 hydrochloride is a potent, selective, orally active and brain-penetrant antagonist of Smo, with an IC50 of 5.8 nM and Ki of 4.6 nM. PF-5274857 hydrochloride has potential for research of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway[1].

IC50 & Target

IC50: 5.8 nM (Smo); Ki: 4.6 nM (Smo)[1]

In Vitro

PF-5274857 completely inhibits Shh-induced Hh pathway activity with an IC50 of 2.7±1.4 nM measured by the transcriptional activity of Smo downstream gene Gli1 in MEF cells[1].
PF-5274857 shows less than 20% inhibition against a broad panel of protein kinases at 1 μM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PF-5274857 (1-30 mg/kg; p.o. once daily for 6 days) shows robust antitumor efficacy and correlation between PK and PD in medulloblastoma allograft mice models[1].
PF-5274857 (10 mg/kg; i.h.) in the plasma is able to cross the blood-brain barrier in rats within 4 hours postdose[1].
PF-5274857 (10-100 mg/kg; p.o. once daily for 4 days) is able to target Smo in the brain leading to the downregulation of Hh pathway activity in the brain tumor[1].
PF-5274857 (30 mg/kg; p.o. once daily for 34 days) increases the survival rates of primary Ptch+/− p53−/− medulloblastoma mice[1].
PF-5274857 (5-30 mg/kg; p.o.) exhibits the apparent volume of distribution of 5.6±0.5 L/kg and the half-life (T1/2) of 1.7±0.1 hours[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Severe combined immunodeficient (SCID)-beige mice (6-8 weeks old) are genetically engineered[1]
Dosage: 0, 1, 5, 10, 30 mg/kg
Administration: P.o. once daily for 6 days
Result: Showed robust antitumor activity with an in vivo IC50 of 8.9±2.6 nM.
Animal Model: Severe combined immunodeficient (SCID)-beige mice (6-8 weeks old)[1]
Dosage: 0, 5, 10, 30 mg/kg (Pharmacokinetic Analysis)
Administration: A single p.o.
Result: The apparent volume of distribution of 5.6±0.5 L/kg; the half-life (T1/2) of 1.7±0.1 hours.
Molecular Weight

473.42

Formula

C₂₀H₂₆Cl₂N₄O₃S

CAS No.

1613439-62-5

SMILES

O=C(N1CCN(C2=NC=C(Cl)C(C3=NC=C(C)C=C3C)=C2)CC1)CCS(=O)(C)=O.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

PF-5274857PF5274857PF 5274857SmoSmoothenedtumorbrainmetastasisdrivenHhpathwayInhibitorinhibitorinhibit

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PF-5274857 hydrochloride
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HY-13459A
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