A dual inhibitor of CDKs and Aurora kinases
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JNJ-7706621

Item No. 18494

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[[5-amino-1-(2,6-difluorobenzoyl)-1H-1,2,4-triazol-3-yl]amino]-benzenesulfonamide
CAS Number
443797-96-4
Synonyms
  • Aurora A Inhibitor I
  • Aurora Kinase/CDK Inhibitor
Molecular Formula
C15H12F2N6O3S
Formula Weight
394.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 20 mg/mlEthanol: 20 mg/ml
λmax
202, 269, 307 nm
SMILES
NS(C1=CC=C(NC2=NN(C(C3=C(F)C=CC=C3F)=O)C(N)=N2)C=C1)(=O)=O
InChi Code
InChI=1S/C15H12F2N6O3S/c16-10-2-1-3-11(17)12(10)13(24)23-14(18)21-15(22-23)20-8-4-6-9(7-5-8)27(19,25)26/h1-7H,(H2,19,25,26)(H3,18,20,21,22)
InChi Key
KDKUVYLMPJIGKA-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    JNJ-7706621 is a dual inhibitor of cyclin-dependent kinases (CDKs) and Aurora kinases. It potently inhibits Cdk1/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, Cdk3/cyclin E, Cdk4/cyclin D1, Cdk6/cyclin D1, Aurora A, and Aurora B in vitro (IC50s = 9, 4, 3, 58, 253, 175, 11, and 15 nM, respectively).1 It shows selectivity for these enzymes over a panel of other receptors and kinases, although it exhibits submicromolar inhibition of VEGF and FGF receptors, as well as GSK3β.1 JNJ-7706621 blocks the growth of a large variety of cancer cell lines (IC50 values range from 112 to 514 nM), with lower potency against normal cells (IC50 values between 3.67 and 5.42 µM). It induces the regression of A375 melanoma human tumor xenografts in mice.1 JNJ-7706621 is a substrate for the ATP-binding cassette transporter G2, also known as breast cancer resistance protein.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Emanuel, S., Rugg, C.A., Gruninger, R.H., et al. The in vitro and in vivo effects of JNJ-7706621: a dual inhibitor of cyclin-dependent kinases and aurora kinases. Cancer Res. 65(19), 9038-9046 (2005).

    2. Seamon, J.A., Rugg, C.A., Emanuel, S., et al. Role of the ABCG2 drug transporter in the resistance and oral bioavailability of a potent cyclin-dependent kinase/Aurora kinase inhibitor. Mol. Cancer Ther. 5(10), 2459-2467 (2006).