A selective cyclin D1/CDK4 and cyclin D3/CDK6 inhibitor
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LEE011

Item No. 17666

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
7-cyclopentyl-N,N-dimethyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide
CAS Number
1211441-98-3
Synonyms
  • Ribociclib
Molecular Formula
C23H30N8O
Formula Weight
434.5
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 5 mg/mlDMSO: 10 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/mlEthanol: 0.5 mg/ml
λmax
284, 346 nm
SMILES
O=C(N(C)C)C(N1C2CCCC2)=CC(C1=N3)=CN=C3NC(C=C4)=NC=C4N5CCNCC5
InChi Code
InChI=1S/C23H30N8O/c1-29(2)22(32)19-13-16-14-26-23(28-21(16)31(19)17-5-3-4-6-17)27-20-8-7-18(15-25-20)30-11-9-24-10-12-30/h7-8,13-15,17,24H,3-6,9-12H2,1-2H3,(H,25,26,27,28)
InChi Key
RHXHGRAEPCAFML-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    Product Description

    LEE011 is a cyclin-dependent kinase (CDK) inhibitor that targets cyclin D1/CDK4 and cyclin D3/CDK6 at nanomolar concentrations.1,2,3 It inhibits retinoblastoma protein phosphorylation, which prevents CDK-mediated G1-S phase transition, arresting the cell cycle in the G1 phase, suppressing DNA synthesis, and inhibiting cancer cell growth.3 LEE011 has been shown to reduce proliferation in 12 of 17 human neuroblastoma-derived cell lines by inducing cytostasis (mean IC50 = 306 nM in sensitive lines).3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kim, S., Loo, A., Chopra, R., et al. LEE011: An orally bioavailable, selective small molecule inhibitor of CDK4/6 - Reactivating Rb in cancer. Mol. Cancer Ther. 12, (2013).

    2. Dickson, M.A. Molecular pathways: CDK4 inhibitors for cancer therapy. Clin. Cancer Res. 20(13), 3379-3383 (2014).

    3. Rader, J., Russell, M.R., Hart, L.S., et al. Dual CDK4/CDK6 inhibition induces cell-cycle arrest and senescence in neuroblastoma. Clin. Cancer Res. 19(22), 6173-6182 (2013).