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JNJ-7706621

Catalog No. T6126   CAS 443797-96-4
Synonyms: JNJ 7706621

JNJ-7706621 is a potent aurora kinase inhibitor, and also inhibits CDK1 and CDK2.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
JNJ-7706621 Chemical Structure
JNJ-7706621, CAS 443797-96-4
Pack Size Availability Price/USD Quantity
1 mg In stock $ 43.00
2 mg In stock $ 61.00
5 mg In stock $ 107.00
10 mg In stock $ 189.00
25 mg In stock $ 298.00
50 mg In stock $ 547.00
100 mg In stock $ 767.00
500 mg In stock $ 1,550.00
1 mL * 10 mM (in DMSO) In stock $ 90.00
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Purity: 99.66%
Purity: 99.1%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description JNJ-7706621 is a potent aurora kinase inhibitor, and also inhibits CDK1 and CDK2.
Targets&IC50 Aurora A:11 nM, Aurora B:15 nM, CDK2/CyclinE:3 nM, CDK2/CyclinA:4 nM, CDK1/CyclinB:9 nM
Kinase Assay In vitro kinase assay for CDK1 and Aurora kinases:CDK1 kinase activity is tested by the CDK1/cyclin B complex purified from baculovirus to phosphorylate a biotinylated peptide substrate containing the consensus phosphorylation site for histone H1, which is phosphorylated in vivo by CDK1. Inhibition of CDK1 activity is measured by observing a decreased amount of 33P-γ-ATP incorporation into the immobilized substrate in streptavidin-coated 96-well scintillating microplates. CDK1 enzyme is diluted in 50 mM Tris-HCl (pH 8), 10 mM MgCl2, 0.1 mM Na3VO4, 1 mM DTT, 1% DMSO, 0.25 μM peptide, 0.1 μCi per well 33P-γ-ATP, and 5 μM ATP in the presence or absence of various concentrations of JNJ-7706621 and incubated at 30 °C for 1 hour. The reaction is terminated by washing with PBS containing 100 mM EDTA and plates are counted in a scintillation counter. IC50 is determined by Linear regression analysis of the percent inhibition by JNJ-7706621.The Aurora kinase activity is measured with 10 μM ATP and a peptide containing a dual repeat of the kemptide phosphorylation motif.
Cell Research Cell lines: HeLa,HCT-116,A375,SK-OV-3,MDA-MB-231 and PC-3 cells. Concentrations: 1 nM - 10 μM,dissolved in DMSO. Method: Measuring incorporation of 14C-labelled thymidine into newly synthesized DNA within the cells to determine the ability of JNJ-7706621 to inhibit the proliferation of cell growth.Cells are trypsinized and counted and 3-8 ×103 cells are added to each well of a 96-well CytoStar tissue culture treated scintillating microplate in 100 μL complete medium in a volume.Cells are incubated for 24 hours at 37 °C in an atmosphere containing 5% CO2.Next,1 μL JNJ-7706621 is added to the wells of the plate.Cells are incubated for another 24 hours.Methyl 14C-thymidine 56 mCi/mmol is diluted in complete medium and 0.2 μCi/well is added to each well of the CytoStar plate in a volume of 20 μL.The plate is incubated for 24 hours at 37 °C in JNJ-7706621 with 14C-thymidine.The contents of the plate are discarded and the plate is washed twice with 200 μL PBS.200 μL of PBS is added to each well.The top of the plate is sealed with a transparent plate sealer and a white plate backing sealer is applied to the bottom of the plate.The degree of methyl 14C-thymidine incorporation is quantified on a Packard Top Count.
Animal Research Animal Models: Mouse xenograft model of A375 cellsFormulation & . Dosages: Dissolved in 0.5% methylcellulose containing 0.1% polysorbate 80 in sterile water.100 or 125 mg/kg. Administration: Orally or by intraperitoneal injection
Synonyms JNJ 7706621
Molecular Weight 394.36
Formula C15H12F2N6O3S
CAS No. 443797-96-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 73 mg/mL (185.1 mM)

H2O: <1 mg/mL

Ethanol: <1 mg/mL

TargetMolReferences and Literature

1. Emanuel S, et al. Cancer Res, 2005, 65(19), 9038-9046. 2. Seamon JA, et al. Mol Cancer Ther, 2006, 5(10), 2459-2467. 3. Lin R, et al. J Med Chem, 2005, 48(13), 4208-4211.

Related compound libraries

This product is contained In the following compound libraries:
Preclinical Compound Library Anti-Breast Cancer Compound Library Bioactive Compounds Library Max Autophagy Compound Library Anti-Cancer Active Compound Library Anti-Aging Compound Library Bioactive Compound Library Apoptosis Compound Library Anti-Cancer Compound Library Inhibitor Library

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Keywords

JNJ-7706621 443797-96-4 Apoptosis Cell Cycle/Checkpoint Chromatin/Epigenetic CDK Aurora Kinase Cyclin dependent kinase JNJ7706621 JNJ 7706621 inhibit Inhibitor inhibitor

 

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