Ribociclib HCl
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MedKoo CAT#: 206739

CAS#: 1211443-80-9 (HCl)

Description: Ribociclib hydrochloride is an potent and orally available cyclin-dependent kinase (CDK) inhibitor targeting cyclin D1/CDK4 and cyclin D3/CDK6 cell cycle pathway, with potential antineoplastic activity. Ribociclib specifically inhibits CDK4 and 6, thereby inhibiting retinoblastoma (Rb) protein phosphorylation. Inhibition of Rb phosphorylation prevents CDK-mediated G1-S phase transition, thereby arresting the cell cycle in the G1 phase, suppressing DNA synthesis and inhibiting cancer cell growth.


Price and Availability

Size Price Shipping out time Quantity
50mg USD 150 Same day
500mg USD 350 Same day
1g USD 450 Same day
5g USD 1650 Same day
10g USD 2250 Same day
20g USD 3650 Same day
50g USD 4950 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2020-10-31. Prices are subject to change without notice.

Ribociclib HCl, purity > 99%, is in stock. The same day shipping out after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 206739
Name: Ribociclib HCl
CAS#: 1211443-80-9 (HCl)
Chemical Formula: C23H31ClN8O
Exact Mass:
Molecular Weight: 471.006
Elemental Analysis: C, 58.65; H, 6.63; Cl, 7.53; N, 23.79; O, 3.40


Related CAS #: 1211441-98-3 (free base)   1211443-80-9 (HCl)   1374639-75-4 (succinate)    

Synonym: Ribociclib hydrochloride; LEE011; LEE-011. LEE 011; 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 hydrochloride

InChi Key: JZRSIQPIKASMEV-UHFFFAOYSA-N

InChi Code: InChI=1S/C23H30N8O.ClH/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;/h7-8,13-15,17,24H,3-6,9-12H2,1-2H3,(H,25,26,27,28);1H

SMILES Code: O=C(C1=CC2=CN=C(NC3=NC=C(N4CCNCC4)C=C3)N=C2N1C5CCCC5)N(C)C.[H]Cl


Technical Data

Appearance:
Yellow solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

Safety Data Sheet (SDS):

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


Additional Information

Related CAS#
1211441-98-3 (Ribociclib free base)
1211443-80-9 (Ribociclib hydrochloride)
1374639-75-4 (Ribociclib succinate)


References

1: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012-. Available from http://www.ncbi.nlm.nih.gov/books/NBK548818/ PubMed PMID: 31644125.

2: Bellet M, Ahmad F, Villanueva R, Valdivia C, Palomino-Doza J, Ruiz A, Gonzàlez X, Adrover E, Azaro A, Valls-Margarit M, Parra JL, Aguilar J, Vidal M, Martín A, Gavilá J, Escrivá-de-Romaní S, Perelló A, Hernando C, Lahuerta A, Zamora P, Reyes V, Alcalde M, Masanas H, Céliz P, Ruíz I, Gil M, Seguí MÀ, de la Peña L. Palbociclib and ribociclib in breast cancer: consensus workshop on the management of concomitant medication. Ther Adv Med Oncol. 2019 May 10;11:1758835919833867. doi: 10.1177/1758835919833867. eCollection 2019. Review. PubMed PMID: 31205497; PubMed Central PMCID: PMC6535716.

3: Poratti M, Marzaro G. Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib. 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. Expert Opin Drug Metab Toxicol. 2017 May;13(5):575-581. doi: 10.1080/17425255.2017.1318848. Epub 2017 Apr 21. Review. PubMed PMID: 28395543.

17: Tripathy D, Bardia A, Sellers WR. Ribociclib (LEE011): Mechanism of Action and Clinical Impact of This Selective Cyclin-Dependent Kinase 4/6 Inhibitor in Various Solid Tumors. Clin Cancer Res. 2017 Jul 1;23(13):3251-3262. doi: 10.1158/1078-0432.CCR-16-3157. Epub 2017 Mar 28. Review. PubMed PMID: 28351928; PubMed Central PMCID: PMC5727901.

18: Barroso-Sousa R, Shapiro GI, Tolaney SM. Clinical Development of the CDK4/6 Inhibitors Ribociclib and Abemaciclib in Breast Cancer. Breast Care (Basel). 2016 Jun;11(3):167-73. doi: 10.1159/000447284. Epub 2016 Jun 22. Review. PubMed PMID: 27493615; PubMed Central PMCID: PMC4960359.