An inhibitor of Cdk4/6
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LEE011 (succinate)

Item No. 36414

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
butanedioic acid, compd. with 7-cyclopentyl-N,N-dimethyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide
CAS Number
1374639-75-4
Synonyms
  • NVP-LEE011
  • Ribociclib
Molecular Formula
C23H30N8O • C4H6O4
Formula Weight
552.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 5 mg/mlDMSO: 5 mg/mlPBS (pH 7.2): 10 mg/ml
λmax
276, 345 nm
SMILES
O=C(N(C)C)C(N1C2CCCC2)=CC(C1=N3)=CN=C3NC(C=C4)=NC=C4N5CCNCC5.O=C(CCC(O)=O)O
InChi Code
InChI=1S/C23H30N8O.C4H6O4/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;5-3(6)1-2-4(7)8/h7-8,13-15,17,24H,3-6,9-12H2,1-2H3,(H,25,26,27,28);1-2H2,(H,5,6)(H,7,8)
InChi Key
NHANOMFABJQAAH-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    10 mg

    $44

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    25 mg

    $77

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    50 mg

    $110

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    100 mg

    $154

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    Product Description

    LEE011 is a cyclin-dependent kinase 4 (Cdk4) and Cdk6 inhibitor (IC50s = 0.53 and 2.3 nM, respectively).1 It is selective for Cdk4/6 over Cdk1, Cdk2, Cdk5, Cdk7, and Cdk9 (IC50s = >1,400, >2,500, >2,000, >2,000, and 190 nM, respectively). LEE011 reduces the proliferation of MCF-7 and T47D breast cancer cells (IC50s = 200 and 260 nM, respectively). It induces cell death in C666-1 and NPC/HK1 nasopharyngeal carcinoma cells (IC50s = 12.25 and 5.07 µM, respectively) and cell cycle arrest at the G0/G1 phase in the same cells when used at a concentration of 10 µM.2 LEE011 (200 mg/kg every two weeks), in combination with the PI3Kα inhibitor alpelisib (BYL719; Item No. 16986), reduces tumor growth in two patient-derived xenograft (PDX) mouse models of nasopharyngeal carcinoma.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Chen, P., Lee, N.V., Hu, W., et al. Spectrum and degree of CDK drug interactions predicts clinical performance. Mol. Cancer Ther. 15(10), 2273-2281 (2016).

    2. Wong, C.-H., Ma, B.B.Y., Hui, C.W.C., et al. Preclinical evaluation of ribociclib and its synergistic effect in combination with alpelisib in non-keratinizing nasopharyngeal carcinoma. Sci. Rep. 8(1), 8010 (2018).