PF-5274857

This product is for research use only, not for human use. We do not sell to patients.

PF-5274857
For small sizes, please check our retail website as below: www.invivochem.com
Size Price Stock
250mg$1350Check With Us
500mg$1920Check With Us
1g$2880Check With Us

Cat #: V1336 CAS #: 1373615-35-0 Purity ≥ 98%

Description: PF-5274857 (PF5274857; PF 5274857) is a novel, potent, orally bioavailable and selective Smoothened (Smo) antagonist with potential antineoplastic activity.

References: 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.

Top Publications Citing Invivochem Products
Publications Citing InvivoChem Products

Product Promise

Promise
Molecular Weight (MW)436.96
Molecular FormulaC20H25ClN4O3S
CAS No.1373615-35-0
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 93 mg/mL (212.8 mM)r
Water:<1 mg/mLr
Ethanol: 93 mg/mL (212.8 mM)
Solubility In VivoSaline: 30 mg/mL
SynonymsPF-5274857; PF 5274857; PF5274857
ProtocolIn VitroPF-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
In VivoPF-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
Animal modelSevere combined immunodeficient (SCID)-beige mice (6-8 weeks old) are genetically engineered
Dosages0, 1, 5, 10, 30 mg/kg
AdministrationP.o. once daily for 6 days
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM2.2885 mL11.4427 mL22.8854 mL45.7708 mL
5mM0.4577 mL2.2885 mL4.5771 mL9.1542 mL
10mM0.2289 mL1.1443 mL2.2885 mL4.5771 mL
20mM0.1144 mL0.5721 mL1.1443 mL2.2885 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
×
Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

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 add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.