A potent Aurora kinase inhibitor
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CYC-116

Item No. 21205

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-(2-amino-4-methyl-5-thiazolyl)-N-[4-(4-morpholinyl)phenyl]-2-pyrimidinamine
CAS Number
693228-63-6
Molecular Formula
C18H20N6OS
Formula Weight
368.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 1.25 mg/mlDMSO: 10 mg/mlDMSO:PBS(pH 7.2) (1:3): 0.25 mg/ml
λmax
295, 337 nm
SMILES
CC(N=C(N)S1)=C1C2=NC(NC3=CC=C(N4CCOCC4)C=C3)=NC=C2
InChi Code
InChI=1S/C18H20N6OS/c1-12-16(26-17(19)21-12)15-6-7-20-18(23-15)22-13-2-4-14(5-3-13)24-8-10-25-11-9-24/h2-7H,8-11H2,1H3,(H2,19,21)(H,20,22,23)
InChi Key
GPSZYOIFQZPWEJ-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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    5 mg

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    10 mg

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    25 mg

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    Product Description

    CYC-116 is a potent Aurora kinase inhibitor exhibiting Ki values of 8.0 and 9.2 nM for Aurora kinases A and B, respectively.1 It is significantly less potent against a panel of cyclin-dependent kinases and other related kinases, with the exception of Flt-3 (Ki = 44 nM). CYC-116 exhibits broad-spectrum antiproliferative activity against a panel of human cancer cell lines with a mean IC50 value of 0.54 µM (range = 0.09 – 1.6 µM). It is orally bioavailable and inhibits the growth of human tumor xenografts in mice.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wang, S., Midgley, C.A., Scaërou, F., et al. Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors. J. Med. Chem. 53(11), 4367-4378 (2010).