PLX-647

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

PLX-647
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1g$1725Check With Us

Cat #: V5141 CAS #: 873786-09-5 Purity ≥ 98%

Description: PLX-647 (PLX647) is a novel, potent and highly specific dual FMS/KIT kinase inhibitor with anticancer activity.

References: Zhang C, et al. Design and pharmacology of a highly specific dual FMS and KIT kinase inhibitor. Proc Natl Acad Sci U S A. 2013 Apr 2;110(14):5689-94.

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Molecular Weight (MW)382.38
Molecular FormulaC21H17F3N4
CAS No.873786-09-5
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
SMILES CodeFC(C1=CC=C(C=C1)CNC2=NC=C(CC3=CNC4=NC=CC=C43)C=C2)(F)F
SynonymsPLX647; PLX 647; PLX-647
ProtocolIn VitroPLX647 potently inhibits the growth of FLT3–ITD-expressing MV4-11 cells (IC50=110 nM). PLX647 displayed minimal inhibition of the proliferation of Ba/F3 cells expressing BCR–KDR (IC50=5 μM). PLX647 inhibits osteoclast differentiation with an IC50 of 0.17 μM. In vitro, PLX647 potently inhibits proliferation of BCR-FMS cells, with an IC50 of 92 nM. A corresponding Ba/F3 cell line expressing BCR-KIT is also quite sensitive to PLX647, with an IC50 of 180 nM. PLX647 also inhibits endogenous FMS and KIT, as demonstrated by inhibition of the ligand-dependent cell lines M-NFS-60 (IC50=380 nM) and M-07e (IC50=230 nM), which express FMS and KIT, respectively.
In VivoPLX647 (30 mg/kg) results in significant inhibition of TRAP5b immunostaining and bone osteolysis. PLX647 (30 mg/kg BID) is able to prevent bone damage by the tumor cells. PLX647 (20-80 mg/kg; p.o.; daily or twice daily from 27-41 days) shows effects on collagen-induced arthritis. PLX647 (40 mg/kg; p.o.; male Swiss Webster mice) reduces LPS-induced TNF-α and IL-6 release. PLX647 (40 mg/kg; p.o.; twice daily for 7 days) reduces macrophage accumulation in UUO kidney and blood monocytes.
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
1mM2.6152 mL13.0760 mL26.1520 mL52.3040 mL
5mM0.5230 mL2.6152 mL5.2304 mL10.4608 mL
10mM0.2615 mL1.3076 mL2.6152 mL5.2304 mL
20mM0.1308 mL0.6538 mL1.3076 mL2.6152 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
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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.