RIBOCICLIB HYDROCHLORIDE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C23H30N8O.ClH
Molecular Weight	470.998
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

Cl.CN(C)C(=O)C1=CC2=CN=C(NC3=CC=C(C=N3)N4CCNCC4)N=C2N1C5CCCC5

InChI

InChIKey=JZRSIQPIKASMEV-UHFFFAOYSA-N

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

HIDE SMILES / InChI

Description
Sources: https://newdrugapprovals.org/2015/10/19/ribociclib/
Curator's Comment: Description was created based on several sources, including https://www.novartis.com/news/media-releases/novartis-cdk46-inhibitor-lee011-ribociclib-receives-fda-breakthrough-therapy https://www.ncbi.nlm.nih.gov/pubmed/26995305

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. CDK4/6 inhibitor LEE011 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. Overexpression of CDK4/6, as seen in certain types of cancer, causes cell cycle deregulation. Ribociclib is in phase III clinical trials by Novartis for the treatment of postmenopausal women with advanced breast cancer. Phase II clinical trials are also in development for the treatment of liposarcoma, ovarian cancer, fallopian tube cancer, peritoneum cancer, endometrial cancer, and gastrointestinal cancer. Preregistration for Breast cancer (First-line therapy, Combination therapy, Late-stage disease) in the USA (PO) in November 2016.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
IMR-5 3 Target ID: CHEMBL2366209 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24045179	Inhibitor 8297	126.0 nM [IC50]
SH-SY5Y 3 Target ID: CHEMBL614910 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24045179	Inhibitor 8297	154.0 nM [IC50]
Cyclin-dependent kinase 4 22 Target ID: CHEMBL331 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26995305	Inhibitor 8297	10.0 nM [IC50]
Cyclin-dependent kinase 6 12 Target ID: CHEMBL2508 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26995305	Inhibitor 8297	39.0 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
(HER2)-negative advanced or metastatic breast cancer 3 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf	Primary		Approved 8429	KISQALI Approved Use KISQALI is a kinase inhibitor indicated in combination with an aromatase inhibitor as initial endocrine-based therapy for the treatment of postmenopausal women with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic breast cancer. Launch Date 2017
Breast cancer 434 Sources: http://adisinsight.springer.com/drugs/800033186	Primary		Phase III 656	Unknown Approved Use Unknown

C_max

Value	Dose	Co-administered	Analyte	Population
1168 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/27336726	600 mg 1 times / day multiple, oral dose: 600 mg route of administration: Oral experiment type: MULTIPLE co-administered: LETROZOLE	LETROZOLE	RIBOCICLIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
4714 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/27336726	600 mg 1 times / day multiple, oral dose: 600 mg route of administration: Oral experiment type: MULTIPLE co-administered: LETROZOLE	LETROZOLE	RIBOCICLIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
30 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/27336726	600 mg 1 times / day multiple, oral dose: 600 mg route of administration: Oral experiment type: MULTIPLE co-administered: LETROZOLE	LETROZOLE	RIBOCICLIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
30% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209092s004lbl.pdf			RIBOCICLIB plasma	Homo sapiens

Doses

Dose	Population	Adverse events
280 mg/m2 1 times / day steady, oral Dose: 280 mg/m2, 1 times / day Route: oral Route: steady Dose: 280 mg/m2, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/28432176	unhealthy, 2.0 years (range: 1.0–17.0) n = 5 Health Status: unhealthy Condition: Malignant Rhabdoid Tumors \| Neuroblastoma Age Group: 2.0 years (range: 1.0–17.0) Sex: M+F Population Size: 5 Sources: https://pubmed.ncbi.nlm.nih.gov/28432176	DLT: Fatigue... Dose limiting toxicities: Fatigue (grade 3, 1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/28432176
900 mg 1 times / day multiple, oral MTD Dose: 900 mg, 1 times / day Route: oral Route: multiple Dose: 900 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/31285369 https://pubmed.ncbi.nlm.nih.gov/29059492	unhealthy, 49 years (range: 31-66 years) n = 12 Health Status: unhealthy Condition: grade IV glioma Age Group: 49 years (range: 31-66 years) Sex: M+F Population Size: 12 Sources: https://pubmed.ncbi.nlm.nih.gov/31285369 https://pubmed.ncbi.nlm.nih.gov/29059492	Sources: https://pubmed.ncbi.nlm.nih.gov/31285369 https://pubmed.ncbi.nlm.nih.gov/29059492
400 mg 1 times / day steady, oral Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/29059492/	unhealthy, 57.0 years (range: 33–73 years) n = 4 Health Status: unhealthy Condition: Breast cancer\|Esophagus cancer\| Peritoneum cancer Age Group: 57.0 years (range: 33–73 years) Sex: M+F Population Size: 4 Sources: https://pubmed.ncbi.nlm.nih.gov/29059492/	DLT: Febrile neutropenia... Dose limiting toxicities: Febrile neutropenia (grade 3, 1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/29059492/
600 mg 1 times / day steady, oral Dose: 600 mg, 1 times / day Route: oral Route: steady Dose: 600 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/29059492/	unhealthy, 57.0 years (range: 33–73 years) n = 13 Health Status: unhealthy Condition: Breast cancer\|Esophagus cancer\| Peritoneum cancer Age Group: 57.0 years (range: 33–73 years) Sex: M+F Population Size: 13 Sources: https://pubmed.ncbi.nlm.nih.gov/29059492/	DLT: Febrile neutropenia, QT interval prolonged... Dose limiting toxicities: Febrile neutropenia (grade 3, 1 patient) QT interval prolonged (grade 3, 2 patients) Neutropenia (grade 4, 1 patient) Thrombocytopenia (grade 4, 1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/29059492/
470 mg/m2 1 times / day steady, oral MTD Dose: 470 mg/m2, 1 times / day Route: oral Route: steady Dose: 470 mg/m2, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/28432176	unhealthy, 7.0 years (range: 1.0–20.0 years) n = 12 Health Status: unhealthy Condition: Malignant Rhabdoid Tumors \| Neuroblastoma Age Group: 7.0 years (range: 1.0–20.0 years) Sex: M+F Population Size: 12 Sources: https://pubmed.ncbi.nlm.nih.gov/28432176	DLT: Thrombocytopenia... Other AEs: Neutropenia, Leukopenia... Dose limiting toxicities: Thrombocytopenia (grade 4, 2 patients) Other AEs: Neutropenia (grade 3-4, 67%) Leukopenia (grade 1-2, 25%) Leukopenia (grade 3-4, 42%) Anemia (grade 1-2, 50%) Lymphopenia (grade 1-2, 17%) Lymphopenia (grade 3-4, 33%) Thrombocytopenia (grade 1-2, 8%) Thrombocytopenia (grade 3-4, 42%) Vomiting (grade 1-2, 42%) Fatigue (grade 1-2, 33%) Nausea (grade 1-2, 25%) Electrocardiogram QTc interval prolonged (grade 1-2, 25%) Decreased appetite (grade 1-2, 17%) AST increased (grade 1-2, 25%) Asthenia (grade 1-2, 8%) Creatinine increased (grade 1-2, 8%) Sources: https://pubmed.ncbi.nlm.nih.gov/28432176
600 mg 1 times / day steady, oral Recommended Dose: 600 mg, 1 times / day Route: oral Route: steady Dose: 600 mg, 1 times / day Co-administed with:: letrozole Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf	unhealthy, adult n = 334 Health Status: unhealthy Condition: postmenopausal Age Group: adult Sex: F Population Size: 334 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf	Disc. AE: Neutropenia, Neutropenia... Other AEs: Urinary tract infection, Urinary tract infection... AEs leading to discontinuation/dose reduction: Neutropenia (grade 3, 50%) Neutropenia (grade 4, 10%) Vomiting (2%) ALT increased (grade 1-2, 36%) ALT increased (grade 3, 8%) ALT increased (grade 4, 2%) AST increased (grade 1-2, 37%) AST increased (grade 3, 6%) AST increased (grade 4, 1%) QT interval prolonged (grade 2, 1 patient) Hypokalemia (grade 3, 1 patient) Other AEs: Urinary tract infection (grade 1-2, 10%) Urinary tract infection (grade 3, 1%) Neutropenia (grade 1-2, 15%) Leukopenia (grade 1-2, 12%) Leukopenia (grade 3, 20%) Leukopenia (grade 4, 1%) Anemia (grade 1-2, 16%) Anemia (grade 3, 1%) Anemia (grade 4, <1%) Lymphopenia (grade 1-2, 4%) Lymphopenia (grade 3, 6%) Lymphopenia (grade 4, 1%) Decreased appetite (grade 1-2, 17%) Decreased appetite (grade 3, 2%) Headache (grade 1-2, 21%) Headache (grade 3, <1%) Insomnia (grade 1-2, 11%) Insomnia (grade 3, <1%) Dyspnea (grade 1-2, 11%) Dyspnea (grade 3, 1%) Back pain (grade 1-2, 18%) Back pain (grade 3, 2%) Nausea (grade 1-2, 50%) Nausea (grade 3, 2%) Diarrhea (grade 1-2, 34%) Diarrhea (grade 3, 1%) Vomiting (grade 1-2, 25%) Vomiting (grade 3, 4%) Constipation (grade 1-2, 24%) Constipation (grade 3, 1%) Stomatitis (grade 1-2, 11%) Stomatitis (grade 3, <1%) Abdominal pain (grade 1-2, 10%) Abdominal pain (grade 3, 1%) Alopecia (grade 1-2, 33%) Rash (grade 1-2, 16%) Rash (grade 3, 1%) Pruritus (grade 1-2, 13%) Pruritus (grade 3, 1%) Fatigue (grade 1-2, 34%) Fatigue (grade 3, 2%) Fatigue (grade 4, <1%) Pyrexia (grade 1-2, 12%) Pyrexia (grade 3, <1%) Edema peripheral (grade 1-2, 12%) Blood bilirubin increased (grade 1-2, 8%) Blood bilirubin increased (grade 3, 8%) Blood bilirubin increased (grade 4, 2%) Leukocyte count decreased (grade 1-2, 59%) Leukocyte count decreased (grade 3, 31%) Leukocyte count decreased (grade 4, 3%) Neutrophil count decreased (grade 1-2, 33%) Neutrophil count decreased (grade 3, 49%) Neutrophil count decreased (grade 4, 11%) Hemoglobin decreased (grade 1-2, 55%) Hemoglobin decreased (grade 3, 2%) Lymphocyte count decreased (grade 1-2, 37%) Lymphocyte count decreased (grade 3, 12%) Lymphocyte count decreased (grade 4, 2%) Platelet count decreased (grade 1-2, 27%) Platelet count decreased (grade 3, 1%) Platelet count decreased (grade 4, <1%) Creatinine increased (grade 1-2, 19%) Creatinine increased (grade 3, 1%) Phosphate decreased (grade 1-2, 7%) Phosphate decreased (grade 3, 5%) Phosphate decreased (grade 4, 1%) Potassium decreased (grade 1-2, 9%) Potassium decreased (grade 3, 1%) Potassium decreased (grade 4, 1%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf

AEs

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1737	substrate 1037	substrate 1217	inhibitor 1612

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
Nav1.5 97 Cav1.2 45 CYP3A 214 CYP1A2 1524 CYP2E1 882 CYP3A4/5 278 BCRP 699 OCT2 647 MATE1 306 BSEP 402	FMO3 67 BCRP 561 P-gp 1537 CYP1A2 1054 CYP2J2 56 CYP3A5 395 CYP2A6 543 CYP2B6 664 CYP2C8 693 CYP2C18 138 CYP2C19 991 CYP2E1 667

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
MATE1 308	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209092Orig1s000MultidisciplineR.pdf#page=66 Page: 66.0	yes [Ki 1.7 uM]
OCT2 648	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209092Orig1s000MultidisciplineR.pdf#page=66 Page: 66.0	yes [Ki 1.9 uM]
CYP1A2 1692	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209092Orig1s000MultidisciplineR.pdf#page=66 Page: 66.0	yes [Ki 13 uM]	no (co-administration study) Comment: The effect of multiple doses of 400 mg ribociclib on caffeine was minimal, with Cmax decreased by 10% and AUC increased slightly by 20%. Only weak inhibitory effects on CYP1A2 substrates are predicted using PBPK modeling at 600 mg ribociclib once daily dose and there is no need for dose adjustment Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209092Orig1s000MultidisciplineR.pdf#page=66 Page: 66.0
BCRP 773	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209092Orig1s000MultidisciplineR.pdf#page=66 Page: 66.0	yes [Ki 24 uM]
CYP2E1 970	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209092Orig1s000MultidisciplineR.pdf#page=66 Page: 66.0	yes [Ki 24.5 uM]
CYP3A4/5 335	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209092Orig1s000MultidisciplineR.pdf#page=66 Page: 66.0	yes [Ki 30 uM]
BSEP 403	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209092Orig1s000MultidisciplineR.pdf#page=66 Page: 66.0	yes [Ki 4.7 uM]
CYP3A 298	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209092Orig1s000MultidisciplineR.pdf#page=63 Page: 63.0	yes	yes (co-administration study) Comment: Coadministration of midazolam (CYP3A4 substrate) with multiple doses of 400 mg ribociclib increased the midazolam exposure by 3.8-fold. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209092Orig1s000MultidisciplineR.pdf#page=63 Page: 63.0

Drug as victim

Target	Modality	Activity	Clinical evidence
CYP1A2 1054	substrate 3367 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7287031/ Page: -	minor
CYP2J2 56	substrate 3367 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7287031/ Page: -	minor
CYP3A5 395	substrate 3367 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7287031/ Page: -	minor
CYP2A6 543	substrate 3367 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7287031/ Page: -	no
CYP2B6 664	substrate 3367 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7287031/ Page: -	no
CYP2C18 138	substrate 3367 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7287031/ Page: -	no
CYP2C19 991	substrate 3367 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7287031/ Page: -	no
CYP2C8 693	substrate 3367 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7287031/ Page: -	no
CYP2C9 1037	substrate 3367 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7287031/ Page: -	no
CYP2D6 1217	substrate 3367 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7287031/ Page: -	no
CYP2E1 667	substrate 3367 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7287031/ Page: -	no
BCRP 561	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209092Orig1s000MultidisciplineR.pdf#page=74 Page: 74.0	weak
P-gp 1537	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209092Orig1s000MultidisciplineR.pdf#page=65 Page: 65.0	weak
FMO3 67	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209092Orig1s000MultidisciplineR.pdf#page=33 Page: 33.0	yes
CYP3A4 1737	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209092Orig1s000MultidisciplineR.pdf#page=33 Page: 33.0	yes	yes (co-administration study) Comment: In a dedicated drug-interaction trial, concomitant ritonavir (a strong CYP3A4 inhibitor) increased a single dose ribociclib's Cmax by 1.7-fold and the AUC by 3.2-fold Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209092Orig1s000MultidisciplineR.pdf#page=33 Page: 33.0

Tox targets

Target	Modality	Metabolite
Cav1.2 49	inhibitor 1626 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209092Orig1s000MultidisciplineR.pdf#page=39 Page: 39.0
Nav1.5 100	inhibitor 1626 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209092Orig1s000MultidisciplineR.pdf#page=39 Page: 39.0
hERG 1647	inhibitor 1626 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209092Orig1s000MultidisciplineR.pdf#page=38 Page: 38.0
hERG 1647	inhibitor 1626 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209092Orig1s000MultidisciplineR.pdf#page=38 Page: 38.0	LEQ803 3

Sourcing

Vendor/Aggregator	ID	URL
AA Blocks	AA003A9C	https://www.aablocks.com/goods/Goods/detail?id=AA003A9C
AK Scientific, Inc. (AKSCI)	2513AH	http://www.aksci.com/item_detail.php?cat=2513AH
AK Scientific, Inc. (AKSCI)	SYN1213	http://www.aksci.com/item_detail.php?cat=SYN1213
Aaron Chemicals	AR003B14	http://www.aaronchem.com/1211441-98-3
Achemo Scientific Limited	AC-92785	http://www.achemo.com/search/?Keyword=1211441-98-3
Achemtek	0102-015188	http://www.achemtek.com/1211441-98-3
Acorn PharmaTech	ACN-040728	http://www.acornpharmatech.com/
Adooq BioScience	A13549	https://www.adooq.com/lee011.html
Alsachim	3243	http://www.alsachim.com/product-C4518-glo.bal-view.html
Ambinter	Amb22586452	http://www.ambinter.com/reference/22586452
Angel Pharmatech	AG-11323	http://www.angelpharmatech.com/1211441-98-3.html
Angene	AGN-PC-0WAMDE	http://www.angenechemical.com/productshow/AGN-PC-0WAMDE.html
ApexBio Technology	A8641	http://www.apexbt.com/lee011.html
Ark Pharm	AK174906	http://www.arkpharminc.com/products/1211441-98-3.html
AvaChem Scientific	6736	https://www.avachem.com/productSearch.asp?6736
Axon MedChem	2273	https://www.axonmedchem.com/product/2273
BOC Sciences	1328934-40-2	https://isotope.bocsci.com/product/ribociclib-d6-cas-1328934-40-2-351224.html
BOC Sciences	1211441-98-3	https://www.bocsci.com/ribociclib-cas-1211441-98-3-item-462559.html
BioChemPartner	BCP08804	http://www.biochempartner.com/1211441-98-3-BCP08804
BioCrick	BCC3926	http://www.biocrick.com/LEE011-BCC3926.html
BioSynth	J-690066	https://www.biosynth.com/en/products/all-products/products/J-690079.html
Boerchem	BC600363	http://www.boerchem.com/?product_43198.html
Chem Scene	CS-1750	http://www.chemscene.com/1211441-98-3.html
ChemWise	AR60115	http://www.chemwisellc.com/product/ribociclib-lee011/
ChemieTek	CT-LEE011	http://www.chemietek.com/lee011-details.aspx
Chemspace	CSSB00015190620	https://chem-space.com/CSSB00015190620
Clearsynth	CS-O-32732	https://www.clearsynth.com/en/CSO32732.html
Clearsynth	CS-T-30953	https://www.clearsynth.com/en/CST30953.html
DAOGE BIOPHARMA	DG21-13348	https://www.daogechem.com/product/1211441-98-3.html
DC Chemicals	DC7453	http://www.dcchemicals.com/product_show-Ribociclib_LEE011_.html
Debye Scientific	DA-35904	http://www.debyesci.com/cas_1211441-98-3.html
Excenen	EX-A304	http://www.excenen.com/searchresultlist.php?id=1211441-98-3
Finetech	FT-0700117	http://www.finetechnology-ind.com/prod/detail/pub/1211441-98-3.html
Hairui	HR142611	http://www.hairuichem.com/en/product/1211441-98-3.html
Lab Network	LN01328196	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01328196
Lancrix Chemicals	824360	http://www.lancrix.com/product/detail-14-1323.htm
Matrix Scientific	147253	https://www.matrixscientific.com/147253.html
MedChem Express	HY-15777	https://www.medchemexpress.com/LEE011.html
MuseChem	I000792	https://www.musechem.com/product/I000792.html
Parchem	47527	https://www.parchem.com/chemical-supplier-distributor/Ribociclib-------047527.aspx
Smolecule	S002107	http://www.smolecule.com/products/s002107
Smolecule	S541384	http://www.smolecule.com/products/s541384
Sun-shine Chemical	LEE011	http://www.sun-shinechem.com/1211441-98-3.html
Synblock Inc	SB18480	http://www.synblock.com/product/1211441-98-3.html
THE BioTek	bt-253544	https://www.thebiotek.com/product/inhibitors/bt-253544
THE BioTek	bt-280472	https://www.thebiotek.com/product/inhibitors/bt-280472
Tocris	7050	https://www.tocris.com/products/ribociclib_7050
TubePharm	Tube013	http://www.tubepharm.com/product/1211441-98-3,1256963-02-6-en.html
abcr GmbH	AB453201	http://www.abcr.com/shop/en/AB453201
eNovation Chemicals	D372453	http://www.enovationchem.com/productDetails.asp?productID=D372453
eNovation Chemicals	Y0974892	https://www.enovationchem.com/ProductDetails.asp?ProductID=Y0974892
iChemical	EBD3317897	http://www.ichemical.com/products/1211441-98-3.html?utm_source=PubChem&utm_medium=website&utm_campaign=product%20catalogs

PubMed

Title	Date	PubMed
		252160882
The landscape of somatic copy-number alteration across human cancers.	2010 Feb 18	20164920
Liver X receptors as regulators of macrophage inflammatory and metabolic pathways.	2011 Aug	21193033
Therapeutic targeting of the cyclin D3:CDK4/6 complex in T cell leukemia.	2012 Oct 16	23079656
A CDK4/6 inhibitor enhances cytotoxicity of paclitaxel in lung adenocarcinoma cells harboring mutant KRAS as well as wild-type KRAS.	2013 Jul	23792647
Dual CDK4/CDK6 inhibition induces cell-cycle arrest and senescence in neuroblastoma.	2013 Nov 15	24045179

Patents

Sample Use Guides

In Vivo Use Guide

Ribociclib oral (3 weeks on/1 week off) in combination with oral once daily letrozole: 600 mg ribociclib QD + 2.5 mg letrozole QD

Route of Administration: Oral

In Vitro Use Guide

Ribociclib significantly reduced proliferation in 12 of 17 human neuroblastoma-derived cell lines by inducing cytostasis at nanomolar concentrations (mean IC50 of 307 nM in sensitive lines)

Name

Type

Language

RIBOCICLIB HYDROCHLORIDE

Common Name

English

7H-PYRROLO(2,3-D)PYRIMIDINE-6-CARBOXAMIDE, 7-CYCLOPENTYL-N,N-DIMETHYL-2-((5-(1-PIPERAZINYL)-2-PYRIDINYL)AMINO)-, HYDROCHLORIDE (1:1)

Systematic Name

English

Code System Code Type Description

DRUG BANK

DBSALT002059

Created by admin on Sat Dec 16 11:13:43 GMT 2023 , Edited by admin on Sat Dec 16 11:13:43 GMT 2023

PRIMARY

FDA UNII

63YF7YKW7E

Created by admin on Sat Dec 16 11:13:43 GMT 2023 , Edited by admin on Sat Dec 16 11:13:43 GMT 2023

PRIMARY

PUBCHEM

67242274

Created by admin on Sat Dec 16 11:13:43 GMT 2023 , Edited by admin on Sat Dec 16 11:13:43 GMT 2023

PRIMARY

CAS

1211443-80-9

Created by admin on Sat Dec 16 11:13:43 GMT 2023 , Edited by admin on Sat Dec 16 11:13:43 GMT 2023

PRIMARY

ACTIVE MOIETY


					TK8ERE8P56

RIBOCICLIB

SUBSTANCE RECORD


					63YF7YKW7E

RIBOCICLIB HYDROCHLORIDE

Details

SMILES

InChI

Originator

Approval Year

Targets

Conditions

Approved Use

Launch Date

Approved Use

Cmax

AUC

T1/2

Funbound

Doses

AEs

Overview

OverviewOther

Drug as perpetrator​

Drug as victim

Tox targets

Sourcing

PubMed

Patents

Sample Use Guides

C_max

T_1/2

F_unbound

Drug as perpetrator