A dual inhibitor of CDK4 and CDK6
Related Products
Alternative(s)
21560LY2835219
Labeled Version(s)
43483LY2835219-d5
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LY2835219 (methanesulfonate)

Item No. 17740

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[5-[(4-ethyl-1-piperazinyl)methyl]-2-pyridinyl]-5-fluoro-4-[4-fluoro-2-methyl-1-(1-methylethyl)-1H-benzimidazol-6-yl]-2-pyrimidinamine, methanesulfonate
CAS Number
1231930-82-7
Synonyms
  • Abemaciclib
Molecular Formula
C27H32F2N8 • CH4O3S
Formula Weight
602.7
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMSO: 1 mg/mlEthanol: 5 mg/mlPBS (pH 7.2): 1 mg/ml
λmax
245, 272, 299 nm
SMILES
CCN1CCN(CC2=CC=C(NC3=NC=C(F)C(C4=CC(F)=C(N=C(C)N5C(C)C)C5=C4)=N3)N=C2)CC1.OS(C)(=O)=O
InChi Code
InChI=1S/C27H32F2N8.CH4O3S/c1-5-35-8-10-36(11-9-35)16-19-6-7-24(30-14-19)33-27-31-15-22(29)25(34-27)20-12-21(28)26-23(13-20)37(17(2)3)18(4)32-26;1-5(2,3)4/h6-7,12-15,17H,5,8-11,16H2,1-4H3,(H,30,31,33,34);1H3,(H,2,3,4)
InChi Key
NCJPFQPEVDHJAZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    LY2835219 is an orally-bioavailable dual inhibitor of cyclin-dependent kinase 4 (CDK4) and CDK6 (IC50s = 2 and 10 nM, respectively).1,2,3 Through this mechanism, it blocks phosphorylation of retinoblastoma protein, resulting in arrest of cell cycling in the G1 phase. LY2835219 has antitumor action against xenografts when used alone or in combination with other chemotherapeutic compounds.2,3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

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

    2. Gelbert, L.M., Cai, S., Lin, X., et al. Preclinical characterization of the CDK4/6 inhibitor LY2835219: In-vivo cell cycle-dependent/independent anti-tumor activities alone/in combination with gemcitabine. Invest. New. Drugs 32(5), 825-837 (2014).

    3. Tate, S.C., Cai, S., Ajamie, R.T., et al. Semi-mechanistic pharmacokinetic/pharmacodynamic modeling of the antitumor activity of LY2835219, a new cyclin-dependent kinase 4/6 inhibitor, in mice bearing human tumor xenografts. Clin. Cancer Res. 20(14), 3763-3774 (2014).