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Quisinostat (JNJ-26481585)

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Quisinostat (JNJ-26481585)
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Cat #: V0287 CAS #: 875320-29-9 Purity ≥ 98%

Description: Quisinostat (formerly JNJ26481585) is an orally bioavailable, 2nd generation, hydroxamate-based inhibitor of histone deacetylase (HDAC) with potential anticancer activity.

References: Arts J, et al. JNJ-26481585, a novel "second-generation" oral histone deacetylase inhibitor, shows broad-spectrum preclinical antitumoral activity. Clin Cancer Res. 2009 Nov 15;15(22):6841-51.

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Molecular Weight (MW)394.48
Molecular FormulaC21H26N6O2
CAS No.875320-29-9
Storage-20℃ for 3 years in powder formrr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: >19.2 mg/mLrr
Water: <1 mg/mLrr
Ethanol: <1 mg/mL
SynonymsJNJ 26481585; JNJ26481585; JNJ-26481585; Quisinostat Chemical Name: N-hydroxy-2-(4-((((1-methyl-1H-indol-3-yl)methyl)amino)methyl)piperidin-1-yl)pyrimidine-5-carboxamide InChi Key: PAWIYAYFNXQGAP-UHFFFAOYSA-N InChi Code: InChI=1S/C21H26N6O2/c1-26-14-17(18-4-2-3-5-19(18)26)11-22-10-15-6-8-27(9-7-15)21-23-12-16(13-24-21)20(28)25-29/h2-5,12-15,22,29H,6-11H2,1H3,(H,25,28) SMILES Code: O=C(C1=CN=C(N2CCC(CNCC3=CN(C)C4=C3C=CC=C4)CC2)N=C1)NO
ProtocolIn VitroQuisinostat (30-1000 nM; 24 hours) is a potent pan-HDAC inhibitor in tumor cells.Quisinostat inhibits HDAC isozymes in vitro.Quisinostat has a broad spectrum antiproliferative activity against solid and hematologic cancer cell lines and induces apoptosis.
In VivoQuisinostat induces continuous H3 acetylation in tumor tissue in vivo.Quisinostat (40 mg/kg; p.o.; once daily; for 3 days) acts as a potent HDAC1 inhibitor p21waf1,cip1 ZsGreen tumors in vivo.Quisinostat (10 mg/kg; once daily; i.p.; for 14 days) strongly inhibits the growth of large pre-established HCT116 colon xenografts
Animal modelNMRI nude mice, with HCT116 colon carcinoma cells xenografts
Dosages10 mg/kg
AdministrationIntraperitoneal injection, once daily, for 14 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
1mM2.5350 mL12.6749 mL25.3498 mL50.6997 mL
5mM0.5070 mL2.5350 mL5.0700 mL10.1399 mL
10mM0.2535 mL1.2675 mL2.5350 mL5.0700 mL
20mM0.1267 mL0.6337 mL1.2675 mL2.5350 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.