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Ribociclib

Product Specifications

UNSPSC Description

RRibociclib (LEE011) is an ATP-competitive and orally active CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex[1][1].

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/LEE011.html

Solubility

DMSO : 6.25 mg/mL (ultrasonic)

Smiles

O=C(N(C)C)C(N1C2CCCC2)=CC(C1=N3)=CN=C3NC(N=C4)=CC=C4N5CCNCC5

Molecular Weight

434.54

References & Citations

[1]VanArsdale T, et al. Molecular Pathways: Targeting the Cyclin D-CDK4/6 Axis for Cancer Treatment. Clin Cancer Res. 2015 Jul 1;21(13):2905-10.|[2]Rader J, et al. Dual CDK4/CDK6 Inhibition Induces Cell-Cycle Arrest and Senescence in Neuroblastoma. Clin Cancer Res. 2013 Nov 15;19(22):6173-82.Artif Cells Nanomed Biotechnol. 2019 Dec;47(1):4001-4011.|Biomed Chromatogr. 2020 Mar;34(3):e4783.|Biomed Pharmacother. 2019 Feb 18;112:108602. |Biomed Res Int. 2020 Jun 11;2020:9525207.|bioRxiv. 2024 Nov 15:2024.11.11.623139.|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. 2019 Oct 15;79(20):5245-5259.|Cancers (Basel). 2022, 14(22), 5481|Cancers. 2020 Jun 16;12(6):1596.|Cell Chem Biol. 2019 Aug 15;26(8):1067-1080.e8. |Cell Death Dis. 2020 Sep 15;11(9):754.|Cell Rep Med. 2023 Sep 12;101200.|Cell Rep Methods. 2023 Oct 23;3(10):100599.|Cell Rep. 2017 Oct 31;21(5):1386-1398.|Cell Rep. 2020 Aug 4;32(5):107995.|Cell. 2023 Jun 8;186(12):2628-2643.e21.|Clin Cancer Res. 2015 Nov 1;21(21):4947-59.|Department of Biochemistry. 2020 Oct.|Eur J Cancer. 2018 Oct;102:10-22.|Eur J Drug Metab Pharmacokinet. 2021 Jul 18;1-11.|Front Oncol. 2022 Apr 8;12:819003.|Fundam Clin Pharmacol. 2021 Feb 1.|Harvard Medical School LINCS LIBRARY|Int J Biol Sci. 2019 Jan 1;15(3):522-532. |J Chromatogr B. 2020 Jun 15;1147:122142.|J Infect Dis. 2018 Nov 22;218(suppl_5):S365-S387.|J Pharmaceut Biomed. 2021, 113933.|J Transl Med. 2022 May 13;20(1):217.|J Virol. 2023 May 23;e0037023.|Leuk Res. September 2022, 106920.|Mil Med Res. 2022 Dec 19;9(1):71.|Mol Cancer Ther. 2018 May;17(5):897-907.|Mol Cell. 2017 Oct 19;68(2):336-349.e6.|Mol Oncol. 2017 Aug;11(8):1035-1049.|Nat Commun. 2021 Sep 10;12(1):5386.|Nat Commun. 2022 Aug 10;13(1):4689.|Nat Commun. 2019 Jun 28;10(1):2860.|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. US20220354911A1.|PLoS One. 2022 Dec 22;17(12):e0279522.|PLoS One. 2024 August 28.|Research Square Print. November 7th, 2022|RSC Adv. 2020, 10(38):22668-22683.|Sci Adv. 2022 Dec 23;8(51):eadc8911.|Sci Rep. 2021 Mar 8;11(1):5374.|Sci Rep. 2022 Jul 20;12(1):12420.|Sci Transl Med. 2018 Jul 18;10(450):eaaq1093.|Texas Southern University. 2024 July 02.|Transl Oncol. 2024 Aug 16:49:102092.|bioRxiv. 2023 Sep 16.|Clin Cancer Res. 2015 Nov 1;21(21):4947-59.|JCI Insight. 2021 Dec 21;e154402.|Cell Chem Biol. 2018 Feb 15;25(2):135-142.e5.|Nat Commun. 2021 Aug 25;12(1):5112.

Shipping Conditions

Room Temperature

Product Datasheet

http://file.medchemexpress.com/batch_PDF/HY-15777/Ribociclib-DataSheet-MedChemExpress.pdf

Product MSDS

http://file.medchemexpress.com/batch_PDF/HY-15777/Ribociclib-SDS-MedChemExpress.pdf

Clinical Information

Launched

CAS Number

1211441-98-3

Available Sizes

Curated Selection

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