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MedKoo Cat#: 100948 | Name: Ribociclib succinate
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Ribociclib, also known as LEE011, is an orally available cyclin-dependent kinase (CDK) inhibitor targeting cyclin D1/CDK4 and cyclin D3/CDK6 cell cycle pathway, with potential antineoplastic activity. LEE011 specifically inhibits CDK4 and 6, thereby inhibiting retinoblastoma (Rb) protein phosphorylation.

Chemical Structure

Ribociclib succinate
Ribociclib succinate
CAS#1374639-75-4 (succinate)

Theoretical Analysis

MedKoo Cat#: 100948

Name: Ribociclib succinate

CAS#: 1374639-75-4 (succinate)

Chemical Formula: C27H36N8O5

Exact Mass: 0.0000

Molecular Weight: 552.64

Elemental Analysis: C, 58.68; H, 6.57; N, 20.28; O, 14.48

Price and Availability

Size Price Availability Quantity
25mg USD 150.00 Ready to ship
50mg USD 225.00 Ready to ship
100mg USD 385.00 Ready to ship
200mg USD 685.00 Ready to ship
500mg USD 1,450.00 Ready to ship
1g USD 2,450.00 Ready to ship
2g USD 4,250.00 Ready to ship
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Related CAS #
1211441-98-3 (free base) 1211443-80-9 (HCl) 1374639-75-4 (succinate)
Synonym
Ribociclib succinate; LEE011-BBA; LEE011 succinate; LEE011; LEE-011; LEE 011; LEE011A; LEE-011A; LEE 011A; Kisqali;
IUPAC/Chemical Name
7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide succinate
InChi Key
NHANOMFABJQAAH-UHFFFAOYSA-N
InChi Code
InChI=1S/C23H30N8O.C4H6O4/c1-29(2)22(32)19-13-16-14-26-23(28-21(16)31(19)17-5-3-4-6-17)27-20-8-7-18(15-25-20)30-11-9-24-10-12-30;5-3(6)1-2-4(7)8/h7-8,13-15,17,24H,3-6,9-12H2,1-2H3,(H,25,26,27,28);1-2H2,(H,5,6)(H,7,8)
SMILES Code
CN(C(C1=CC2=CN=C(NC3=NC=C(N4CCNCC4)C=C3)N=C2N1C5CCCC5)=O)C.O=C(O)CCC(O)=O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Biological target:
Ribociclib is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively. It inhibits Rb phosphorylation, which prevents CDK-mediated G1-S phase transition, thereby arresting the cell cycle in the G1 phase, suppressing DNA synthesis and inhibiting cancer cell growth.
In vitro activity:
Ribociclib induces apoptosis of renal cell carcinoma (RCC) cell. The combination of ribociclib with chemotherapeutic or immunotherapeutic agents is synergistic in RCC cell lines. Ribociclib demonstrates selective anti-RCC activity by sparing normal kidney cells and fibroblast cells. Ribociclib remarkably inhibits phosphorylation of Rb at various sites, leading to the suppression of transcription of E2F target genes in RCC cells. Reference: Biomed Res Int. 2020; 2020: 9525207. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7306082/
In vivo activity:
Treatment of mice tumos with the combination of ribociclib and gemcitabine was well tolerated, slowed tumor progression and metastatic spread, and increased survival. The findings in both mouse and human patient-derived orthotopic xenograft models suggest that ribociclib and gemcitabine combination therapy warrants further investigation as a treatment strategy for children with group3 medulloblastoma. Reference: Mol Cancer Ther. 2022 Aug 2;21(8):1306-1317. https://pubmed.ncbi.nlm.nih.gov/35709750/
Solvent mg/mL mM
Solubility
DMSO 70.8 121.19
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 552.64 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Chen D, Sun X, Zhang X, Cao J. Inhibition of the CDK4/6-Cyclin D-Rb Pathway by Ribociclib Augments Chemotherapy and Immunotherapy in Renal Cell Carcinoma. Biomed Res Int. 2020 Jun 11;2020:9525207. doi: 10.1155/2020/9525207. PMID: 32626773; PMCID: PMC7306082. 2. Kim S, Tiedt R, Loo A, Horn T, Delach S, Kovats S, Haas K, Engstler BS, Cao A, Pinzon-Ortiz M, Mulford I, Acker MG, Chopra R, Brain C, di Tomaso E, Sellers WR, Caponigro G. The potent and selective cyclin-dependent kinases 4 and 6 inhibitor ribociclib (LEE011) is a versatile combination partner in preclinical cancer models. Oncotarget. 2018 Oct 16;9(81):35226-35240. doi: 10.18632/oncotarget.26215. Erratum in: Oncotarget. 2020 Apr 07;11(14):1289. PMID: 30443290; PMCID: PMC6219668. 3. Malorni L, Bianchini G, Caputo R, Zambelli A, Puglisi F, Bianchi GV, Del Mastro L, Paris I, Montemurro F, Allegrini G, Colleoni M, Tamberi S, Zamagni C, Cazzaniga ME, Orditura M, Guarneri V, Castelletti D, Benelli M, Di Marino M, Arpino G, De Laurentiis M. Serum thymidine kinase activity in patients with HR-positive/HER2-negative advanced breast cancer treated with ribociclib plus letrozole: Results from the prospective BioItaLEE trial. Eur J Cancer. 2023 Jun;186:1-11. doi: 10.1016/j.ejca.2023.03.001. Epub 2023 Mar 8. PMID: 37003098. 4. Pribnow A, Jonchere B, Liu J, Smith KS, Campagne O, Xu K, Robinson S, Patel Y, Onar-Thomas A, Wu G, Stewart CF, Northcott PA, Yu J, Robinson GW, Roussel MF. Combination of Ribociclib and Gemcitabine for the Treatment of Medulloblastoma. Mol Cancer Ther. 2022 Aug 2;21(8):1306-1317. doi: 10.1158/1535-7163.MCT-21-0598. PMID: 35709750; PMCID: PMC9578677.
In vitro protocol:
1. Chen D, Sun X, Zhang X, Cao J. Inhibition of the CDK4/6-Cyclin D-Rb Pathway by Ribociclib Augments Chemotherapy and Immunotherapy in Renal Cell Carcinoma. Biomed Res Int. 2020 Jun 11;2020:9525207. doi: 10.1155/2020/9525207. PMID: 32626773; PMCID: PMC7306082. 2. Kim S, Tiedt R, Loo A, Horn T, Delach S, Kovats S, Haas K, Engstler BS, Cao A, Pinzon-Ortiz M, Mulford I, Acker MG, Chopra R, Brain C, di Tomaso E, Sellers WR, Caponigro G. The potent and selective cyclin-dependent kinases 4 and 6 inhibitor ribociclib (LEE011) is a versatile combination partner in preclinical cancer models. Oncotarget. 2018 Oct 16;9(81):35226-35240. doi: 10.18632/oncotarget.26215. Erratum in: Oncotarget. 2020 Apr 07;11(14):1289. PMID: 30443290; PMCID: PMC6219668.
In vivo protocol:
1. Malorni L, Bianchini G, Caputo R, Zambelli A, Puglisi F, Bianchi GV, Del Mastro L, Paris I, Montemurro F, Allegrini G, Colleoni M, Tamberi S, Zamagni C, Cazzaniga ME, Orditura M, Guarneri V, Castelletti D, Benelli M, Di Marino M, Arpino G, De Laurentiis M. Serum thymidine kinase activity in patients with HR-positive/HER2-negative advanced breast cancer treated with ribociclib plus letrozole: Results from the prospective BioItaLEE trial. Eur J Cancer. 2023 Jun;186:1-11. doi: 10.1016/j.ejca.2023.03.001. Epub 2023 Mar 8. PMID: 37003098. 2. Pribnow A, Jonchere B, Liu J, Smith KS, Campagne O, Xu K, Robinson S, Patel Y, Onar-Thomas A, Wu G, Stewart CF, Northcott PA, Yu J, Robinson GW, Roussel MF. Combination of Ribociclib and Gemcitabine for the Treatment of Medulloblastoma. Mol Cancer Ther. 2022 Aug 2;21(8):1306-1317. doi: 10.1158/1535-7163.MCT-21-0598. PMID: 35709750; PMCID: PMC9578677.
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Eur J Med Chem. 2019 Jun 15;172:143-153. doi: 10.1016/j.ejmech.2019.03.064. Epub 2019 Apr 4. Review. PubMed PMID: 30978559. 4: Eggersmann TK, Degenhardt T, Gluz O, Wuerstlein R, Harbeck N. CDK4/6 Inhibitors Expand the Therapeutic Options in Breast Cancer: Palbociclib, Ribociclib and Abemaciclib. BioDrugs. 2019 Apr;33(2):125-135. doi: 10.1007/s40259-019-00337-6. Review. PubMed PMID: 30847853. 5: Petrelli F, Ghidini A, Pedersini R, Cabiddu M, Borgonovo K, Parati MC, Ghilardi M, Amoroso V, Berruti A, Barni S. Comparative efficacy of palbociclib, ribociclib and abemaciclib for ER+ metastatic breast cancer: an adjusted indirect analysis of randomized controlled trials. Breast Cancer Res Treat. 2019 Apr;174(3):597-604. doi: 10.1007/s10549-019-05133-y. Epub 2019 Jan 18. Review. PubMed PMID: 30659432. 6: Ribociclib for breast cancer. Aust Prescr. 2018 Oct;41(5):172. doi: 10.18773/austprescr.2018.058. Epub 2018 Oct 2. Review. PubMed PMID: 30410218; PubMed Central PMCID: PMC6202289. 7: Büyükkaramikli NC, de Groot S, Riemsma R, Fayter D, Armstrong N, Portegijs P, Duffy S, Kleijnen J, Al MJ. Ribociclib with an Aromatase Inhibitor for Previously Untreated, HR-Positive, HER2-Negative, Locally Advanced or Metastatic Breast Cancer: An Evidence Review Group Perspective of a NICE Single Technology Appraisal. Pharmacoeconomics. 2019 Feb;37(2):141-153. doi: 10.1007/s40273-018-0708-4. Review. PubMed PMID: 30194622; PubMed Central PMCID: PMC6386053. 8: Drugs and Lactation Database (LactMed) [Internet]. Bethesda (MD): National Library of Medicine (US); 2006-. Available from http://www.ncbi.nlm.nih.gov/books/NBK500944/ PubMed PMID: 30000003. 9: Laderian B, Fojo T. CDK4/6 Inhibition as a therapeutic strategy in breast cancer: palbociclib, ribociclib, and abemaciclib. Semin Oncol. 2017 Dec;44(6):395-403. doi: 10.1053/j.seminoncol.2018.03.006. Epub 2018 Mar 26. Review. PubMed PMID: 29935901. 10: Burris HA 3rd. Ribociclib for the treatment of hormone receptor-positive, human epidermal growth factor receptor 2-negative advanced breast cancer. Expert Rev Anticancer Ther. 2018 Mar;18(3):201-213. doi: 10.1080/14737140.2018.1435275. Epub 2018 Feb 19. Review. PubMed PMID: 29457921. 11: Edessa D, Sisay M. Recent advances of cyclin-dependent kinases as potential therapeutic targets in HR+/HER2- metastatic breast cancer: a focus on ribociclib. Breast Cancer (Dove Med Press). 2017 Dec 6;9:567-579. doi: 10.2147/BCTT.S150540. eCollection 2017. Review. PubMed PMID: 29263697; PubMed Central PMCID: PMC5726365. 12: Zangardi ML, Spring LM, Blouin GC, Bardia A. Ribociclib for post-menopausal women with HR+/HER2- advanced or metastatic breast cancer. Expert Rev Clin Pharmacol. 2017 Nov;10(11):1169-1176. doi: 10.1080/17512433.2017.1376653. Epub 2017 Sep 18. Review. PubMed PMID: 28875723. 13: López-Tarruella S, Jerez Y, Márquez-Rodas I, Echavarria I, Martin M. Ribociclib for the treatment of advanced hormone receptor-positive, HER2-negative breast cancer. Future Oncol. 2017 Oct;13(24):2137-2149. doi: 10.2217/fon-2017-0183. Epub 2017 Jul 31. Review. PubMed PMID: 28758424. 14: Kwapisz D. Cyclin-dependent kinase 4/6 inhibitors in breast cancer: palbociclib, ribociclib, and abemaciclib. Breast Cancer Res Treat. 2017 Nov;166(1):41-54. doi: 10.1007/s10549-017-4385-3. Epub 2017 Jul 24. Review. PubMed PMID: 28741274. 15: Costa R, Costa RB, Talamantes SM, Helenowski I, Peterson J, Kaplan J, Carneiro BA, Giles FJ, Gradishar WJ. Meta-analysis of selected toxicity endpoints of CDK4/6 inhibitors: Palbociclib and ribociclib. Breast. 2017 Oct;35:1-7. doi: 10.1016/j.breast.2017.05.016. Epub 2017 Jun 12. Review. PubMed PMID: 28618307. 16: Curigliano G, Criscitiello C, Esposito A, Intra M, Minucci S. Pharmacokinetic drug evaluation of ribociclib for the treatment of metastatic, hormone-positive breast cancer. 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