Abemaciclib methanesulfonate
Cat. No.：YN290387
CAS No. ：1231930-82-7
| 产品名称: | Abemaciclib methanesulfonate |
| CAS No.: | 1231930-82-7 |
| Chemical 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 |
| Synonyms: | LY2835219 methanesulfonate |
| 分子量: | 602.70 |
| 分子式: | C₂₈H₃₆F₂N₈O₃S |
| SMILES: | CC(N1C2=CC(C3=NC(NC4=NC=C(CN5CCN(CC)CC5)C=C4)=NC=C3F)=CC(F)=C2N=C1C)C.CS(=O)(O)=O |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | Abemaciclib methanesulfonate (LY2835219 methanesulfonate) 是选择性的CDK4/6抑制剂，抑制 CDK4/CDK6 的IC50分别为 2 nM 和 10 nM。 |
| IC50和靶点: | [{name:"Cdk4/cyclin D1:2 nM (IC50)"},{name: "CDK6/cyclinD1:10 nM (IC50)"},{name: "CDK9/cyclinT1:57 nM (IC50)"},{name: "CDK5/p35:287 nM (IC50)"},{name: "Cdk5/p25:355 nM (IC50)"},{name: "CDK2/cyclinE:504 nM (IC50)"},{name: "CDK1/cyclinB1:1627 nM (IC50)"},{name: "CDK7/Mat1/cyclinH1:3910 nM (IC50)"},{name: "PIM1:50 nM (IC50)"},{name: "PIM2:3400 nM (IC50)"},{name: "HIPK2:31 nM (IC50)"},{name: "DYRK2:61 nM (IC50)"},{name: "CK2:117 nM (IC50)"},{name: "GSK3b:192 nM (IC50)"},{name: "JNK3:389 nM (IC50)"},{name: "FLT3 (D835Y):403 nM (IC50)"},{name: "DRAK1:659 nM (IC50)"},{name: "FLT3:3960 nM (IC50)"}] |
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Dickson, M.A.Molecular pathways: CDK4 inhibitors for cancer therapyClin. Cancer Res.20(13),3379-3383(2014)
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 gemcitabineInvest. New. Drugs32(5),825-837(2014)
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 xenograftsClin. Cancer Res.20(14),3763-3774(2014)
