PF-03814735

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

PF-03814735
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100mg$900Check With Us
250mg$1650Check With Us
500mg$2475Check With Us

Cat #: V0366 CAS #: 942487-16-3 Purity ≥ 98%

Description: PF-03814735 (PF03814735) is a reversible, orally bioavailable, and ATP-competitive inhibitor of Aurora A/B kinases with potential antitumor activity.

References: Jani JP, et al. PF-03814735, an orally bioavailable small molecule aurora kinase inhibitor for cancer therapy. Mol Cancer Ther. 2010 Apr;9(4):883-94.

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Molecular Weight (MW)474.48
Molecular FormulaC23H25F3N6O2
CAS No.942487-16-3
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 0.4 mg/mL (0.84 mM)r
Water: <1 mg/mLr
Ethanol: <1 mg/mL
Solubility In Vivo2% Cremophor EL, 2% N,N-dimethylacetamide, pH 5.0: ~30 mg/mL
SMILES CodeCC(NCC(N1[C@@]2([H])CC[C@]1([H])C3=C2C=CC(NC4=NC=C(C(F)(F)F)C(NC5CCC5)=N4)=C3)=O)=O
SynonymsPF-03814735; PF 03814735; PF03814735
ProtocolIn VitroIn intact cells, the inhibitory activity of PF-03814735 on the Aurora1 and Aurora2 kinases reduces levels of phospho-Aurora1, phosphohistone H3, and phospho-Aurora2. PF-03814735 produces a block in cytokinesis, resulting in inhibition of cell proliferation and the formation of polyploid multinucleated cells.
In VivoOnce-daily oral administration of PF-03814735 to mice bearing human xenograft tumors produces a reduction in phosphohistone H3 in tumors at doses that are tolerable and that result in significant inhibition of tumor growth. The combination of PF-03814735 and docetaxel in xenograft mouse tumor models shows additive tumor growth inhibition.
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
1mM2.1076 mL10.5379 mL21.0757 mL42.1514 mL
5mM0.4215 mL2.1076 mL4.2151 mL8.4303 mL
10mM0.2108 mL1.0538 mL2.1076 mL4.2151 mL
20mM0.1054 mL0.5269 mL1.0538 mL2.1076 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.