An inhibitor of Cdk9/cyclin T1, Cdk1/cyclin B, and Cdk2/cyclin A complexes
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CDKI-73

Item No. 41099

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[[5-fluoro-4-[4-methyl-2-(methylamino)-5-thiazolyl]-2-pyrimidinyl]amino]-benzenesulfonamide
CAS Number
1421693-22-2
Synonyms
  • Asnuciclib
Molecular Formula
C15H15FN6O2S2
Formula Weight
394.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly Soluble: 1-10 mg/ml
SMILES
O=S(N)(C1=CC(NC2=NC=C(C(C3=C(C)N=C(NC)S3)=N2)F)=CC=C1)=O
InChi Code
InChI=1S/C15H15FN6O2S2/c1-8-13(25-15(18-2)20-8)12-11(16)7-19-14(22-12)21-9-4-3-5-10(6-9)26(17,23)24/h3-7H,1-2H3,(H,18,20)(H2,17,23,24)(H,19,21,22)
InChi Key
GAIOPWBQKZMUNO-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    5 mg

    $75

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    10 mg

    $142

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    25 mg

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    50 mg

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    Product Description

    CDKI-73 is an inhibitor of Cdk9/cyclin T1, Cdk1/cyclin B, and Cdk2/cyclin A complexes (Kis = 4, 4, and 3 nM, respectively).1 It is selective for these complexes over the Cdk7/cyclin H complex (Ki = 91 nM). CDKI-73 is cytotoxic to HCT116 colorectal cancer cells (GI50 = <10 nM). CDKI-73 (0.25 or 1 µM) induces apoptosis in COLO 205, HCT116, HT-29, and KM12 colorectal cancer cells.2 It reduces the levels of Bcl-2, cyclin D1, and myeloid cell leukemia-1 (Mcl-1), as well as decreases the mitochondrial membrane potential, in HCT116 cells when used at a concentration of 0.25 µM. In vivo, CDKI-73 (100 mg/kg every three days) decreases tumor volume in an HCT116 mouse xenograft model to a greater extent than the DNA-crosslinking agent cisplatin (Item No. 13119).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Shao, H., Shi, S., Huang, S., et al. Substituted 4-(thiazol-5-yl)-2-(phenylamino)pyrimidines are highly active CDK9 inhibitors: Synthesis, X-ray crystal structures, structure-activity relationship, and anticancer activities. J. Med. Chem. 56(3), 640-659 (2013).

    2. Rahaman, M.H., Lam, F., Zhong, L., et al. Targeting CDK9 for treatment of colorectal cancer. Mol. Oncol. 13(10), 2178-2193 (2019).