A cell-permeable inhibitor of Cdk4/6
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Cdk4/6 Inhibitor IV

Item No. 17974

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
trans-4-[[6-(ethylamino)-2-[[1-(phenylmethyl)-1H-indol-5-yl]amino]-4-pyrimidinyl]amino]-cyclohexanol
CAS Number
359886-84-3
Synonyms
  • CINK4
  • Cyclin-dependent kinase 4/6 Inhibitor IV
Molecular Formula
C27H32N6O
Formula Weight
456.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS(pH 7.2) (1:4): 0.2 mg/mlEthanol: 1 mg/ml
λmax
212, 285 nm
SMILES
CCNC1=NC(NC2=CC=C(N(CC3=CC=CC=C3)C=C4)C4=C2)=NC(N[C@H]5CC[C@H](O)CC5)=C1
InChi Code
InChI=1S/C27H32N6O/c1-2-28-25-17-26(29-21-8-11-23(34)12-9-21)32-27(31-25)30-22-10-13-24-20(16-22)14-15-33(24)18-19-6-4-3-5-7-19/h3-7,10,13-17,21,23,34H,2,8-9,11-12,18H2,1H3,(H3,28,29,30,31,32)/t21-,23-
InChi Key
YVXCDLCJCIDFHE-AFARHQOCSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $48

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    Product Description

    Cdk4/6 inhibitor IV is a cell-permeable triaminopyrimidine that reversibly blocks Cdk4/cyclin D1 and Cdk6/cyclin D1 activity with IC50 values of 1.5 and 5.6 μM, respectively.1 It demonstrates potent selectivity for Cdk4/6 over Cdk5/p35, v-abl, c-met, IGF-1R, insulin receptor, Cdk2/cyclin A, Cdk2/cyclin E, Cdk4/cyclin D2, Cdk6/cyclin D2, and Cdk1/cyclin B (IC50s = > 10-100 µM).1 At 5-10 µM, this compound blocks retinoblastoma protein phosphorylation at Ser780 and Ser795, inducing cell cycle arrest in the G1 phase and apoptosis in asynchronous cell lines.1 In mice bearing human HCT116 colon carcinoma xenografts, 30 mg/kg, i.p. Cdk/6 inhibitor IV suppressed tumor growth after 29 days of treatment.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Soni, R., O'Reilly, T., Furet, P., et al. Selective in vivo and in vitro effects of a small molecule inhibitor of cyclin-dependent kinase 4. J. Natl. Cancer Inst. 93(6), 436-446 (2001).

    Product Citations

    Yan, K.N., Nie, Y.Q., Wang, J.Y., et al. Accelerating PROTACs discovery through a direct-to-biology platform enabled by modular photoclick chemistry. Adv. Sci. (Weinh) 11(26), e2400594 (2024).