For research use only. Not for therapeutic Use.
Abemaciclib (LY2835219)（Cat No.:I000698）is a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), which play a critical role in regulating cell cycle progression. By inhibiting CDK4/6, Abemaciclib blocks the transition from the G1 phase to the S phase, halting cell proliferation, particularly in cancer cells. It has demonstrated significant efficacy in the treatment of hormone receptor-positive (HR+) breast cancer and is under investigation for other cancers. Abemaciclib is widely used in cancer research to explore targeted therapies aimed at inhibiting tumor growth and improving patient outcomes.
| Catalog Number | I000698 |
| CAS Number | 1231929-97-7 (free base) |
| Synonyms | ;N-(5-((4-ethylpiperazin-1-yl)methyl)pyridin-2-yl)-5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazol-6-yl)pyrimidin-2-amine |
| Molecular Formula | C27H32F2N8 |
| Purity | ≥95% |
| Target | CDK inhibitor |
| Solubility | Soluble in DMSO, not in water |
| Storage | 0 - 4°Cfor short term (days to weeks), or -20 °C for long term (months). |
| IUPAC Name | N-[5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl]-5-fluoro-4-(7-fluoro-2-methyl-3-propan-2-ylbenzimidazol-5-yl)pyrimidin-2-amine |
| InChI | InChI=1S/C27H32F2N8/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/h6-7,12-15,17H,5,8-11,16H2,1-4H3,(H,30,31,33,34) |
| InChIKey | UZWDCWONPYILKI-UHFFFAOYSA-N |
| SMILES | CCN1CCN(CC1)CC2=CN=C(C=C2)NC3=NC=C(C(=N3)C4=CC5=C(C(=C4)F)N=C(N5C(C)C)C)F |
| Reference | </br>1: Yadav V, Burke TF, Huber L, Van Horn RD, Zhang Y, Buchanan SG, Chan EM, Starling JJ, Beckmann RP, Peng SB. The CDK4/6 Inhibitor LY2835219 Overcomes Vemurafenib Resistance Resulting from MAPK Reactivation and Cyclin D1 Upregulation. Mol Cancer Ther. 2014 Aug 13. pii: molcanther.0257.2014. [Epub ahead of print] PubMed PMID: 25122067.</br>2: Gelbert LM, Cai S, Lin X, Sanchez-Martinez C, Del Prado M, Lallena MJ, Torres R, Ajamie RT, Wishart GN, Flack RS, Neubauer BL, Young J, Chan EM, Iversen P, Cronier D, Kreklau E, de Dios A. 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. 2014 Jun 13. [Epub ahead of print] PubMed PMID: 24919854.</br>3: Tate SC, Cai S, Ajamie RT, Burke T, Beckmann RP, Chan EM, De Dios A, Wishart GN, Gelbert LM, Cronier DM. 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. 2014 Jul 15;20(14):3763-74. doi: 10.1158/1078-0432.CCR-13-2846. Epub 2014 May 21. PubMed PMID: 24850847.</br>4: Dickson MA. Molecular pathways: CDK4 inhibitors for cancer therapy. Clin Cancer Res. 2014 Jul 1;20(13):3379-83. doi: 10.1158/1078-0432.CCR-13-1551. Epub 2014 May 2. PubMed PMID: 24795392.</br> |
