A Cdk2 inhibitor
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K03861

Item No. 19921

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-[(2-amino-4-pyrimidinyl)oxy]phenyl]-N'-[4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-urea
CAS Number
853299-07-7
Synonyms
  • AUZ454
Molecular Formula
C24H26F3N7O2
Formula Weight
501.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/mlEthanol: Soluble: ≥10 mg/ml
SMILES
CN1CCN(CC2=C(C(F)(F)F)C=C(NC(NC3=CC=C(OC4=NC(N)=NC=C4)C=C3)=O)C=C2)CC1
InChi Code
InChI=1S/C24H26F3N7O2/c1-33-10-12-34(13-11-33)15-16-2-3-18(14-20(16)24(25,26)27)31-23(35)30-17-4-6-19(7-5-17)36-21-8-9-29-22(28)32-21/h2-9,14H,10-13,15H2,1H3,(H2,28,29,32)(H2,30,31,35)
InChi Key
PWDLXPJQFNVTNL-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $76

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    10 mg

    $137

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    50 mg

    $494

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    100 mg

    $684

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    Product Description

    K03861 is an inhibitor of cyclin-dependent kinase 2 (Cdk2).1 It binds to wild-type Cdk2, Cdk2C118L, Cdk2A144C, and Cdk2C118L/A144C (Kds = 50, 18.6, 15.4, and 9.7 nM, respectively). K03861 selectively inhibits the proliferation of IL-3-stimulated Ba/F3 cells expressing an FMS-related tyrosine kinase 3 bearing internal-tandem duplication (FLT3-ITD) over wild-type Ba/F3 cells (IC50s = ~0.001 and > 0.1 µM, respectively).2 It inhibits human cytomegalovirus replication in primary human monocyte-derived macrophages (IC50 = 1.028 µM).3 K03861 (10 µM) inhibits spindle organization and chromosome alignment in meiosis I and prevents egg activation in isolated mouse oocytes.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Alexander, L.T., Möbitz, H., Drueckes, P., et al. Type II inhibitors targeting CDK2. ACS Chem. Biol. 10(9), 2116-2125 (2015).

    2. Weisberg, E., Roesel, J., Furet, P., et al. Antileukemic effects of novel first- and second-generation FLT3 inhibitors: Structure-affinity comparison. Genes Cancer 1(10), 1021-1032 (2010).

    3. Syrigos, G.V., Feige, M., Dirlam, A., et al. Abemaciclib restricts HCMV replication by suppressing pUL97-mediated phosphorylation of SAMHD1. Antiviral Res. 217, 105689 (2023).

    4. Li, J., Chang, H.-Y., Yi, Z.-Y., et al. Transient inhibition of CDK2 activity prevents oocyte meiosis I completion and egg activation in mouse. J. Cell. Physiol. 237(11), 4317-4325 (2022).