Abemaciclib (methanesulfonate)

Abemaciclib (methanesulfonate)

• CAS Number: 1231930-82-7
• UNSPSC Description: Abemaciclib methanesulfonate (LY2835219 methanesulfonate) is a selective CDK4/6 inhibitor with IC50s of 2 nM and 10 nM for CDK4 and CDK6, respectively[1][2][3].
• Target Antigen: CDK
• Type: Reference compound
• Related Pathways: Cell Cycle/DNA Damage
• Applications: Cancer-Kinase/protease
• Field of Research: Cancer
• Assay Protocol: https://www.medchemexpress.com/LY2835219.html
• Solubility: DMSO : 10 mg/mL (ultrasonic;warming;heat to 80°C)|H2O : 125 mg/mL (ultrasonic)
• 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
• Molecular Weight: 602.70
• References & Citations: [1]Ku BM, et al. The CDK4/6 inhibitor LY2835219 has potent activity in combination with mTOR inhibitor in head and neck squamous cell carcinoma. Oncotarget. 2016 Mar 22;7(12):14803-13.|[2]Yadav V, et al. The CDK4/6 inhibitor LY2835219 overcomes PLX4032 resistance resulting from MAPK reactivation and cyclin D1 upregulation. Mol Cancer Ther. 2014 Oct;13(10):2253-63.|[3]Gelbert LM, et al. Preclinical characterization of the CDK4/6 inhibitor LY2835219: in-vivo cell cycle-dependent/independent anti-tumor activities alone/in combination with NSC 613327. Invest New Drugs. 2014 Oct;32(5):825-37.|[4]Wu T, et al. Effect of abemaciclib (LY2835219) on enhancement of chemotherapeutic agents in ABCB1 and ABCG2 overexpressing cells in vitro and in vivo. Biochem Pharmacol. 2017 Jan 15;124:29-42.Biochem Biophys Rep. 27, September 2021, 101099|Biochem Biophys Res Commun. 2018 Sep 26;504(1):231-237. |Biochem Pharmacol. 2017 Jan 15;124:29-42.|Biochim Biophys Acta. 2017 Nov 20;1865(2):354-363.|bioRxiv. 2020 Jun.|Cancer Res. 2016 Nov 15;76(22):6723-6734. |Cancer Res. 2023 Jun 29;CAN-23-0705.|Cell Death Dis. 2019 Mar 20;10(4):271.|Cell Rep. 2017 Oct 31;21(5):1386-1398.|Cell Rep. 2022 Sep 13;40(11):111331.|Cell. 2018 Nov 1;175(4):984-997.e24.|Clin Cancer Res. 2024 May 8.|EMBO J. 2022 Jan 5;e108946.|Harvard Medical School LINCS LIBRARY|J Exp Clin Cancer Res. 2022 Apr 21;41(1):149.|J Oncol. 2019 Jun 2;2019:5952836. |Mol Cell. 2017 Oct 19;68(2):336-349.e6.|Mol Oncol. 2017 Aug;11(8):1035-1049.|Nat Commun. 2017 Jun 27;8:15916.|Nat Commun. 2019 Jun 28;10(1):2860.|Nature. 2017 Aug 24;548(7668):471-475. |Nutrition. 2019 Apr;60:217-226. |Oncotarget. 2017 Jul 27;8(56):95116-95134. |Oncotarget. 2017 Jun 27;8(40):67422-67438. |Sci Transl Med. 2018 Jul 18;10(450):eaaq1093.|STAR Protocols. 2020 Jun 3;1(1):100024.|ACS Appl Mater Interfaces. 2022 May 11;14(18):20628-20640.|Adv Funct Mater. 2021 Apr 30.|Adv Sci (Weinh). 2020 Aug 4;7(18):2000906.|Adv Sci (Weinh). 2022 Aug 2;e2201834.|Bioact Mater. 8 September 2021.|Biochem Biophys Res Commun. 20 December 2021.|Biomed Chromatogr. 2020 Jun;34(6):e4825.|bioRxiv. 2023 Jan 25.|bioRxiv. 2023 Jul 17.|bioRxiv. 2023 Jul 19.|bioRxiv. 2024 Dec 10:2024.12.09.627542.|bioRxiv. 2024 Nov 15:2024.11.11.623139.|Blood Cancer J. 2022 Jan 11;12(1):5.|Br J Cancer. 2022 Jan 14.|Breast Cancer Res. 2019 Dec 26;21(1):150.|Cancer Cell. 2024 Aug 27:S1535-6108(24)00305-2.|Cancer Discov. 2023 Dec 4.|Cancer Res. 2017 May 1;77(9):2488-2499.|Cancer Res. 2019 Oct 15;79(20):5245-5259.|Cancer Res. 2022 May 16;82(10):1890-1908.|Cell Chem Biol. 2019 Aug 15;26(8):1067-1080.e8. |Cell Death Dis. 2020 Oct 28;11(10):925.|Cell Rep. 2022 Dec 20;41(12):111826.|Cell. 2023 Jun 8;186(12):2628-2643.e21.|Commun Biol. 2021 Mar 25;4(1):399.|Department of Biochemistry. 2020 Oct.|EMBO J. 2024 Aug 19.|EMBO J. 2024 Oct 24.|Eur J Drug Metab Pharmacokinet. 2021 Jul 18;1-11.|Front Oncol. 2021 Jul 13;11:704042.|Fundam Clin Pharmacol. 2021 Feb 1.|Heliyon. 2023 Sep 13.|Int J Biol Sci. 2019 Jan 1;15(3):522-532. |Int J Mol Sci. 2021 Jan 8;22(2):E575.|Int J Mol Sci. 2022 Feb 24;23(5):2493.|J Cell Biochem. 2023 Aug 11.|J Med Chem. 2023 Mar 6.|J Oncol. 2022 Jun 23;2022:8724933.|J Pharm Anal. 2024 Aug 22.|JCI Insight. 2021 Dec 21;e154402.|Leuk Res. September 2022, 106920.|Mol Cancer Ther. 2024 Jun 19.|Nat Commun. 2021 Aug 25;12(1):5112.|Nat Commun. 2021 Nov 16;12(1):6607.|Nat Commun. 2022 Aug 10;13(1):4689.|Nat Metab. 2020 Jan;2(1):41-49.|Nature Cancer. 2021 Apr;2(4):429-443.|Naunyn Schmiedebergs Arch Pharmacol. 2023 Feb 4.|NPJ Precis Oncol. 2021 Mar 19;5(1):20.|Patent. US20200108066A1|R Soc Open Sci. 2019 Jan 23;6(1):181714.|Sci Data. 2024 Sep 19.|Sci Rep. 2022 Jul 20;12(1):12420.|Sci Rep. 2024 May 8;14(1):10582.|Sci Rep. 2019 Oct 22;9(1):15099. |SSRN. 2022 Nov 21.|SSRN. 2023 Sep 29.|Texas Southern University. 2024 July 02.|Transl Lung Cancer Res. 2024 May 31;13(5):1032-1046.|University of Gothenburg. 2023 Jun 27.
• Shipping Conditions: Room Temperature
• Clinical Information: Launched