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

50mg
USD 150
5g
USD 1650
Size
Price

500mg
USD 350
20g
USD 2650
Size
Price

1g
USD 450
50g
USD 4650

Ribociclib HCl, purity > 99%, is in stock. The same day shipping out after order is received. Note: the estimated shipping out time for order > 20g may be 2 weeks..


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.

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 (MSDS):

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).

Harmonized System Code:
293490


Additional Information

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


References

1: Hortobagyi GN, Stemmer SM, Burris HA, Yap YS, Sonke GS, Paluch-Shimon S, Campone M, Blackwell KL, André F, Winer EP, Janni W, Verma S, Conte P, Arteaga CL, Cameron DA, Petrakova K, Hart LL, Villanueva C, Chan A, Jakobsen E, Nusch A, Burdaeva O, Grischke EM, Alba E, Wist E, Marschner N, Favret AM, Yardley D, Bachelot T, Tseng LM, Blau S, Xuan F, Souami F, Miller M, Germa C, Hirawat S, O'Shaughnessy J. Ribociclib as First-Line Therapy for HR-Positive, Advanced Breast Cancer. N Engl J Med. 2016 Nov 3;375(18):1738-1748. PubMed PMID: 27717303.

2: Curigliano G, Gómez Pardo P, Meric-Bernstam F, Conte P, Lolkema MP, Beck JT, Bardia A, Martínez García M, Penault-Llorca F, Dhuria S, Tang Z, Solovieff N, Miller M, Di Tomaso E, Hurvitz SA. Ribociclib plus letrozole in early breast cancer: A presurgical, window-of-opportunity study. Breast. 2016 Aug;28:191-8. doi: 10.1016/j.breast.2016.06.008. PubMed PMID: 27336726.

3: Infante JR, Cassier PA, Gerecitano JF, Witteveen PO, Chugh R, Ribrag V, Chakraborty A, Matano A, Dobson JR, Crystal AS, Parasuraman S, Shapiro GI. A Phase I Study of the Cyclin-Dependent Kinase 4/6 Inhibitor Ribociclib (LEE011) in Patients with Advanced Solid Tumors and Lymphomas. Clin Cancer Res. 2016 Dec 1;22(23):5696-5705. PubMed PMID: 27542767.

4: 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. Review. PubMed PMID: 27493615; PubMed Central PMCID: PMC4960359.

5: Ribociclib Lengthens Breast Cancer Survival. Cancer Discov. 2016 Dec;6(12):1299. PubMed PMID: 27810861.

6: Aristizabal Prada ET, Noelting S, Spoettl G, Maurer J, Auernhammer CJ. The Novel Cyclin-Dependent Kinase 4/6 Inhibitor Ribociclib (LEE011) Alone and in Dual-Targeting Approaches Demonstrates Antitumoral Efficacy in Neuroendocrine Tumors in vitro. Neuroendocrinology. 2017 Feb 23. doi: 10.1159/000463386. [Epub ahead of print] PubMed PMID: 28226315.

7: de Gramont A, Herrera A, de Gramont A. Ribociclib for HR-Positive, Advanced Breast Cancer. N Engl J Med. 2017 Jan 19;376(3):288-289. PubMed PMID: 28102649.

8: Araki K, Miyoshi Y. Ribociclib for HR-Positive, Advanced Breast Cancer. N Engl J Med. 2017 Jan 19;376(3):288. PubMed PMID: 28102647.

9: Hortobagyi GN. Ribociclib for HR-Positive, Advanced Breast Cancer. N Engl J Med. 2017 Jan 19;376(3):289. doi: 10.1056/NEJMc1615255. PubMed PMID: 28099830.

10: Burki TK. Ribociclib in HR-positive, HER2-negative breast cancer. Lancet Oncol. 2016 Nov;17(11):e482. doi: 10.1016/S1470-2045(16)30502-2. PubMed PMID: 27746106.

11: Jansen VM, Bhola NE, Bauer JA, Formisano L, Lee KM, Hutchinson KE, Witkiewicz AK, Moore PD, Estrada MV, Sanchez V, Ericsson PG, Sanders M, Pohlmann PR, Pishvaian MJ, Riddle DA, Wei W, Dugger TC, Knudsen E, Arteaga CL. Kinome-wide RNA interference screen reveals a role for PDK1 in acquired resistance to CDK4/6 inhibition in ER-positive breast cancer. Cancer Res. 2017 Mar 1. pii: canres.2653.2016. doi: 10.1158/0008-5472.CAN-16-2653. [Epub ahead of print] PubMed PMID: 28249908.

12: Sablin MP, Ricci F, Loirat D, Jobard A, Basse C, Romano E, Le Tourneau C, Dieras V. [Cell cycle inhibitors in endocrine receptor positive breast cancer]. Bull Cancer. 2017 Feb;104(2):114-122. doi: 10.1016/j.bulcan.2016.12.005. French. PubMed PMID: 28126188.

13: Wood A, Krytska K, Ryles HT, Infarinato NR, Sano R, Hansel TD, Hart LS, King F, Smith TR, Ainscow E, Grandinetti KB, Tuntland T, Kim S, Caponigro G, He YQ, Krupa S, Li N, Harris J, Mosse YP. Dual ALK and CDK4/6 inhibition demonstrates on-target synergy against neuroblastoma. Clin Cancer Res. 2016 Dec 16. pii: clincanres.1114.2016. [Epub ahead of print] PubMed PMID: 27986745.

14: Hart LS, Rader J, Raman P, Batra V, Russell MR, Tsang M, Gagliardi M, Chen L, Martinez D, Li Y, Wood A, Kim S, Parasuraman S, Delach S, Cole KA, Krupa S, Boehm M, Peters M, Caponigro G, Maris JM. Preclinical Therapeutic Synergy of MEK1/2 and CDK4/6 Inhibition in Neuroblastoma. Clin Cancer Res. 2016 Oct 11. doi: 10.1158/1078-0432.CCR-16-1131. [Epub ahead of print] PubMed PMID: 27729458.

15: Sumi NJ, Kuenzi BM, Knezevic CE, Remsing Rix LL, Rix U. Chemoproteomics Reveals Novel Protein and Lipid Kinase Targets of Clinical CDK4/6 Inhibitors in Lung Cancer. ACS Chem Biol. 2015 Dec 18;10(12):2680-6. doi: 10.1021/acschembio.5b00368. PubMed PMID: 26390342; PubMed Central PMCID: PMC4684772.

16: O'Sullivan CC. CDK4/6 inhibitors for the treatment of advanced hormone receptor positive breast cancer and beyond: 2016 update. Expert Opin Pharmacother. 2016 Aug;17(12):1657-67. doi: 10.1080/14656566.2016.1201072. Review. PubMed PMID: 27322766.

17: Vidula N, Rugo HS. Cyclin-Dependent Kinase 4/6 Inhibitors for the Treatment of Breast Cancer: A Review of Preclinical and Clinical Data. Clin Breast Cancer. 2016 Feb;16(1):8-17. doi: 10.1016/j.clbc.2015.07.005. Review. PubMed PMID: 26303211.

18: Hamilton E, Infante JR. Targeting CDK4/6 in patients with cancer. Cancer Treat Rev. 2016 Apr;45:129-38. doi: 10.1016/j.ctrv.2016.03.002. Review. PubMed PMID: 27017286.

19: Konecny GE. Cyclin-dependent kinase pathways as targets for women's cancer treatment. Curr Opin Obstet Gynecol. 2016 Feb;28(1):42-8. doi: 10.1097/GCO.0000000000000243. Review. PubMed PMID: 26642065.

20: Pabla N, Gibson AA, Buege M, Ong SS, Li L, Hu S, Du G, Sprowl JA, Vasilyeva A, Janke LJ, Schlatter E, Chen T, Ciarimboli G, Sparreboom A. Mitigation of acute kidney injury by cell-cycle inhibitors that suppress both CDK4/6 and OCT2 functions. Proc Natl Acad Sci U S A. 2015 Apr 21;112(16):5231-6. doi: 10.1073/pnas.1424313112. PubMed PMID: 25848011; PubMed Central PMCID: PMC4413320.