SELICICLIB

Investigational

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C19H26N6O
Molecular Weight	354.4501
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC[C@]([H])(CO)N=c1[nH]c(c2c(n1)n(cn2)C(C)C)NCc3ccccc3

InChI

InChIKey=BTIHMVBBUGXLCJ-OAHLLOKOSA-N

InChI=1S/C19H26N6O/c1-4-15(11-26)22-19-23-17(20-10-14-8-6-5-7-9-14)16-18(24-19)25(12-21-16)13(2)3/h5-9,12-13,15,26H,4,10-11H2,1-3H3,(H2,20,22,23,24)/t15-/m1/s1

HIDE SMILES / InChI

Molecular Formula	C19H26N6O
Molecular Weight	354.4501
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	1 / 1
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/15958589 | https://www.ncbi.nlm.nih.gov/pubmed/26987072 | https://www.ncbi.nlm.nih.gov/pubmed/19938906

Seliciclib (CYC202, R-roscovitine) is a second-generation orally available cyclin-dependent kinases (CDKs) inhibitor that competes for ATP binding sites on these kinases. It is a direct inhibitor of cyclin CDK2/E, CDK2/A and it has inhibitory effects on cyclin H/CDK7, CDK5, and CDK9. CDKs are enzymes that are central to the process of cell division and cell cycle control and play pivotal roles in cancer cell growth and DNA damage repair. Seliciclib exerts an anti-proliferative effect via several key mechanisms: selective downregulation of proliferative and survival proteins and upregulation of p53, leading to growth arrest or apoptosis. The second one is decreasing phosphorylation of Rb and modulating E2F transcriptional activity leading to growth arrest or apoptosis. Seliciclib is currently in phase II clinical trial as a drug candidate for the treatment of Cushing's disease and as a potential therapeutic agent for the treatment of cystic fibrosis (CF). In addition, it is in Phase II trials for non-small cell lung cancer and nasopharyngeal carcinoma.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Cyclin-dependent kinase 2 5 Target ID: CHEMBL301 Sources: https://www.ncbi.nlm.nih.gov/pubmed/12432547	Inhibitor 3315	0.1 µM [IC50]
Cyclin-dependent kinase 9 4 Target ID: CHEMBL3116 Sources: https://www.ncbi.nlm.nih.gov/pubmed/15958589	Inhibitor 3315	0.81 µM [IC50]
Cyclin-dependent kinase 7 Target ID: CHEMBL3055 Sources: https://www.ncbi.nlm.nih.gov/pubmed/15958589	Inhibitor 3315	0.36 µM [IC50]
Cyclin-dependent kinase 5 2 Target ID: CHEMBL4036 Sources: https://www.ncbi.nlm.nih.gov/pubmed/9030781	Inhibitor 3315	0.2 µM [IC50]

Conditions

Condition	Modality	Highest Phase	Product
Cushing’s disease 7 Sources: https://www.ncbi.nlm.nih.gov/pubmed/25942479	Primary	Phase II 394	Unknown Approved Use Unknown
Cystic fibrosis 62 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26987072	Primary	Phase II 394	Unknown Approved Use Unknown
Non-small cell lung cancer 79 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19938906	Primary	Phase II 394	Unknown Approved Use Unknown
Nasopharyngeal carcinoma 3 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19938906	Primary	Phase II 394	Unknown Approved Use Unknown

Doses

Dose	Population	Adverse events
1800 mg 2 times / day multiple, oral Highest studied dose Dose: 1800 mg, 2 times / day Route: oral Route: multiple Dose: 1800 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/20822897 Page: p.3246, 3247	unhealthy, ADULT n = 6 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 6 Sources: https://pubmed.ncbi.nlm.nih.gov/20822897 Page: p.3246, 3247	DLT: Asthenia, Hypokalaemia... Dose limiting toxicities: Asthenia (33.3%) Hypokalaemia (33.3%) Sources: https://pubmed.ncbi.nlm.nih.gov/20822897 Page: p.3246, 3247
1250 mg 2 times / day multiple, oral MTD Dose: 1250 mg, 2 times / day Route: oral Route: multiple Dose: 1250 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/20822897 Page: p.3245, 3246	unhealthy, ADULT n = 3 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 3 Sources: https://pubmed.ncbi.nlm.nih.gov/20822897 Page: p.3245, 3246	Sources: https://pubmed.ncbi.nlm.nih.gov/20822897 Page: p.3245, 3246
1600 mg 2 times / day multiple, oral MTD Dose: 1600 mg, 2 times / day Route: oral Route: multiple Dose: 1600 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/20822897 Page: p.3246, 3247	unhealthy, ADULT n = 3 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 3 Sources: https://pubmed.ncbi.nlm.nih.gov/20822897 Page: p.3246, 3247	Sources: https://pubmed.ncbi.nlm.nih.gov/20822897 Page: p.3246, 3247
1600 mg 2 times / day multiple, oral Studied dose Dose: 1600 mg, 2 times / day Route: oral Route: multiple Dose: 1600 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/20822897 Page: p.3245, 3246	unhealthy, ADULT n = 6 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 6 Sources: https://pubmed.ncbi.nlm.nih.gov/20822897 Page: p.3245, 3246	DLT: Hypokalaemia, Asthenia... Dose limiting toxicities: Hypokalaemia (33.3%) Asthenia (33.3%) Vomiting (33.3%) Nausea (33.3%) Sources: https://pubmed.ncbi.nlm.nih.gov/20822897 Page: p.3245, 3246
800 mg 2 times / day multiple, oral Studied dose Dose: 800 mg, 2 times / day Route: oral Route: multiple Dose: 800 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/17179992 Page: p.32	unhealthy, ADULT n = 12 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: FASTED Population Size: 12 Sources: https://pubmed.ncbi.nlm.nih.gov/17179992 Page: p.32	DLT: Hyperglycaemia, Fatigue... Dose limiting toxicities: Hyperglycaemia (8.3%) Fatigue (grade 3, 8.3%) Hyponatraemia (grade 3, 8.3%) Hypokalaemia (grade 4, 8.3%) Skin rash (grade 3, 8.3%) Glycosuria (8.3%) GGT increased (25%) Sources: https://pubmed.ncbi.nlm.nih.gov/17179992 Page: p.32

AEs

AE	Significance	Dose	Population
Asthenia	33.3% DLT	1800 mg 2 times / day multiple, oral Highest studied dose Dose: 1800 mg, 2 times / day Route: oral Route: multiple Dose: 1800 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/20822897 Page: p.3246, 3247	unhealthy, ADULT n = 6 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 6 Sources: https://pubmed.ncbi.nlm.nih.gov/20822897 Page: p.3246, 3247
Hypokalaemia	33.3% DLT	1800 mg 2 times / day multiple, oral Highest studied dose Dose: 1800 mg, 2 times / day Route: oral Route: multiple Dose: 1800 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/20822897 Page: p.3246, 3247	unhealthy, ADULT n = 6 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 6 Sources: https://pubmed.ncbi.nlm.nih.gov/20822897 Page: p.3246, 3247
Asthenia	33.3% DLT	1600 mg 2 times / day multiple, oral Studied dose Dose: 1600 mg, 2 times / day Route: oral Route: multiple Dose: 1600 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/20822897 Page: p.3245, 3246	unhealthy, ADULT n = 6 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 6 Sources: https://pubmed.ncbi.nlm.nih.gov/20822897 Page: p.3245, 3246
Hypokalaemia	33.3% DLT	1600 mg 2 times / day multiple, oral Studied dose Dose: 1600 mg, 2 times / day Route: oral Route: multiple Dose: 1600 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/20822897 Page: p.3245, 3246	unhealthy, ADULT n = 6 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 6 Sources: https://pubmed.ncbi.nlm.nih.gov/20822897 Page: p.3245, 3246
Nausea	33.3% DLT	1600 mg 2 times / day multiple, oral Studied dose Dose: 1600 mg, 2 times / day Route: oral Route: multiple Dose: 1600 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/20822897 Page: p.3245, 3246	unhealthy, ADULT n = 6 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 6 Sources: https://pubmed.ncbi.nlm.nih.gov/20822897 Page: p.3245, 3246
Vomiting	33.3% DLT	1600 mg 2 times / day multiple, oral Studied dose Dose: 1600 mg, 2 times / day Route: oral Route: multiple Dose: 1600 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/20822897 Page: p.3245, 3246	unhealthy, ADULT n = 6 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: UNKNOWN Population Size: 6 Sources: https://pubmed.ncbi.nlm.nih.gov/20822897 Page: p.3245, 3246
GGT increased	25% DLT	800 mg 2 times / day multiple, oral Studied dose Dose: 800 mg, 2 times / day Route: oral Route: multiple Dose: 800 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/17179992 Page: p.32	unhealthy, ADULT n = 12 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: FASTED Population Size: 12 Sources: https://pubmed.ncbi.nlm.nih.gov/17179992 Page: p.32
Glycosuria	8.3% DLT	800 mg 2 times / day multiple, oral Studied dose Dose: 800 mg, 2 times / day Route: oral Route: multiple Dose: 800 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/17179992 Page: p.32	unhealthy, ADULT n = 12 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: FASTED Population Size: 12 Sources: https://pubmed.ncbi.nlm.nih.gov/17179992 Page: p.32
Hyperglycaemia	8.3% DLT	800 mg 2 times / day multiple, oral Studied dose Dose: 800 mg, 2 times / day Route: oral Route: multiple Dose: 800 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/17179992 Page: p.32	unhealthy, ADULT n = 12 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: FASTED Population Size: 12 Sources: https://pubmed.ncbi.nlm.nih.gov/17179992 Page: p.32
Fatigue	grade 3, 8.3% DLT	800 mg 2 times / day multiple, oral Studied dose Dose: 800 mg, 2 times / day Route: oral Route: multiple Dose: 800 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/17179992 Page: p.32	unhealthy, ADULT n = 12 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: FASTED Population Size: 12 Sources: https://pubmed.ncbi.nlm.nih.gov/17179992 Page: p.32
Hyponatraemia	grade 3, 8.3% DLT	800 mg 2 times / day multiple, oral Studied dose Dose: 800 mg, 2 times / day Route: oral Route: multiple Dose: 800 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/17179992 Page: p.32	unhealthy, ADULT n = 12 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: FASTED Population Size: 12 Sources: https://pubmed.ncbi.nlm.nih.gov/17179992 Page: p.32
Skin rash	grade 3, 8.3% DLT	800 mg 2 times / day multiple, oral Studied dose Dose: 800 mg, 2 times / day Route: oral Route: multiple Dose: 800 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/17179992 Page: p.32	unhealthy, ADULT n = 12 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: FASTED Population Size: 12 Sources: https://pubmed.ncbi.nlm.nih.gov/17179992 Page: p.32
Hypokalaemia	grade 4, 8.3% DLT	800 mg 2 times / day multiple, oral Studied dose Dose: 800 mg, 2 times / day Route: oral Route: multiple Dose: 800 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/17179992 Page: p.32	unhealthy, ADULT n = 12 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: FASTED Population Size: 12 Sources: https://pubmed.ncbi.nlm.nih.gov/17179992 Page: p.32

Sourcing

Vendor/Aggregator	ID	URL
1PlusChem LLC	1P003ULO	https://www.1pchem.com/search?query=1P003ULO
AChemBlock	M15131	http://www.achemblock.com/catalogsearch/result/?q=M15131
AK Scientific	X7381	https://aksci.com/item_detail.php?cat=X7381
AOBIOUS INC	AOB2095	http://aobious.com/aobious/search?search_query=AOB2095
Ambeed	A300507	http://www.ambeed.com/search/Search.html?keyword=A300507
Angene	AGN-PC-0QFT1T	http://www.angenechemical.com/productshow/AGN-PC-0QFT1T.html
AstaTech	40772	http://astatechinc.com/CPSResult.php?CRNO=40772
AstaTech	44091	http://astatechinc.com/CPSResult.php?CRNO=44091
BOC Sciences	186692-44-4	http://www.bocsci.com/description.asp?cas=186692-44-4
BOC Sciences	186692-46-6	http://www.bocsci.com/description.asp?cas=186692-46-6
Cayman Chemical	10009569	http://www.caymanchem.com/app/template/Product.vm/catalog/10009569
Chem Scene	CS-0016	http://www.chemscene.com/goproductList/searchProductList?productObj=CS-0016
ChemShuttle	109815	https://www.chemshuttle.com/catalogsearch/result/?q=109815
ChemShuttle	169545	https://www.chemshuttle.com/catalogsearch/result/?q=169545
Debye Scientific	DB-014986	https://www.debyesci.com/index.php?id=product&ext[cno]=DB-014986
Fluorochem	M02443	http://www.fluorochem.co.uk/Products/Product?code=M02443
Hairui	HR121539	http://www.hairuichem.com/en/product/search.do?q=HR121539
KeyOrganics	AS-56277	http://www.keyorganicsinc.com/bionet/catalogsearch/result?q=AS-56277
Lab Network	LN01309105	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01309105
Lab Network	LN01354423	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01354423
Lab Seeker	SC-85946	http://www.labseeker.com/search.php?keywords=SC-85946&category=0
LabSeeker	SC-85946	http://www.labseeker.com/search.php?keywords=SC-85946&category=0
Matrix Scientific	146699	http://www.matrixscientific.com/146699.html
MedChem Express	HY-30237	https://www.medchemexpress.com/search.html?q=HY-30237&ft=&fa=&fp=
MolPort	MolPort-003-959-463	https://www.molport.com/shop/molecule-link/MolPort-003-959-463
Molnova	M12883	https://www.molnova.com/en/serch-list.html?keywords=M12883
MuseChem	M039487	https://www.musechem.com/product/M039487.html
ShangHai Biochempartner	BCP000089	http://www.biochempartner.com/search_BCP000089
ShangHai Biochempartner	BCP01760	http://www.biochempartner.com/search_BCP01760
ShangHai Biochempartner	BCP19053	http://www.biochempartner.com/search_BCP19053
TargetMol	T2095	https://www.targetmol.com/search?keyword=T2095
Toronto Research Chemicals	R684000	https://www.trc-canada.com/product-detail/?CatNum=R684000
eMolecules	1988824	https://orderbb.emolecules.com/search/#?query=1988824
eMolecules	299993222	https://orderbb.emolecules.com/search/#?query=299993222
eMolecules	594108	https://orderbb.emolecules.com/search/#?query=594108
eNovation Chemicals	D572855	https://www.enovationchem.com/Products.asp?SEARCHTEXT=D572855&searchbtn.x=0&searchbtn.y=0
mcule	MCULE-7286831836	https://mcule.com/MCULE-7286831836/
mcule	MCULE-8307455670	https://mcule.com/MCULE-8307455670/
mcule	MCULE-9773570692	https://mcule.com/MCULE-9773570692/

PubMed

Title	Date	PubMed
Indirubin-3'-monoxime, a derivative of a Chinese antileukemia medicine, inhibits P-TEFb function and HIV-1 replication.	2005 Dec 2	16284457
Potentiation of the lethality of the histone deacetylase inhibitor LAQ824 by the cyclin-dependent kinase inhibitor roscovitine in human leukemia cells.	2005 Nov	16275999
Improved tumor control through circadian clock induction by Seliciclib, a cyclin-dependent kinase inhibitor.	2006 Nov 15	17108108
The cyclin-dependent kinase inhibitor seliciclib (R-roscovitine; CYC202) decreases the expression of mitotic control genes and prevents entry into mitosis.	2007 Dec 15	18075315
Cyclin-dependent kinase inhibitor seliciclib shows in vitro activity in diffuse large B-cell lymphomas.	2007 Jan	17325859
A phase I trial of the selective oral cyclin-dependent kinase inhibitor seliciclib (CYC202; R-Roscovitine), administered twice daily for 7 days every 21 days.	2007 Jan 15	17179992
Seliciclib (CYC202; r-roscovitine) in combination with cytotoxic agents in human uterine sarcoma cell lines.	2007 Jan-Feb	17352243
Inhibition of HIV-1 replication by P-TEFb inhibitors DRB, seliciclib and flavopiridol correlates with release of free P-TEFb from the large, inactive form of the complex.	2007 Jul 11	17625008
Gateways to clinical trials.	2007 Jul-Aug	17922073
Gateways to clinical trials.	2007 Jun	17805439
'Seed' analysis of off-target siRNAs reveals an essential role of Mcl-1 in resistance to the small-molecule Bcl-2/Bcl-XL inhibitor ABT-737.	2007 Jun 7	17173063
AKT and CDK5/p35 mediate brain-derived neurotrophic factor induction of DARPP-32 in medium size spiny neurons in vitro.	2007 Mar 9	17209049
The effects of the CDK inhibitor seliciclib alone or in combination with cisplatin in human uterine sarcoma cell lines.	2007 May	17300833
Mitotic arrest-associated apoptosis induced by sodium arsenite in A375 melanoma cells is BUBR1-dependent.	2008 Aug 15	18501396
Human cytomegalovirus IE1 protein enhances herpes simplex virus type 1-induced syncytial formation in U373MG cells.	2008 Dec	19119451
Small-molecule Bcl-2 antagonists as targeted therapy in oncology.	2008 Dec	19079626
You never know: Cdk inhibitors as anti-cancer drugs.	2008 Dec 15	19066455
Polycystic kidney diseases: from molecular discoveries to targeted therapeutic strategies.	2008 Feb	17975706
Synergistic inhibition of ErbB signaling by combined treatment with seliciclib and ErbB-targeting agents.	2008 Jul 1	18594016
Metabolism of the trisubstituted purine cyclin-dependent kinase inhibitor seliciclib (R-roscovitine) in vitro and in vivo.	2008 Mar	18048486
The separation of antagonist from agonist effects of trisubstituted purines on CaV2.2 (N-type) channels.	2008 May	18221369
Lysine methylation of HIV-1 Tat regulates transcriptional activity of the viral LTR.	2008 May 22	18498648
Effect of seliciclib (CYC202, R-roscovitine) on lymphocyte alloreactivity and acute kidney allograft rejection in rat.	2008 May 27	18497689
Role of caspases, calpain and cdk5 in ammonia-induced cell death in developing brain cells.	2008 Nov	18722528
Molecular therapies for systemic lupus erythematosus: clinical trials and future prospects.	2009	19591653
Regulation of HIV-1 transcription in cells of the monocyte-macrophage lineage.	2009 Dec 23	20030845
Pharmacodynamic effects of seliciclib, an orally administered cell cycle modulator, in undifferentiated nasopharyngeal cancer.	2009 Feb 15	19228744
Seliciclib (CYC202, R-roscovitine) enhances the antitumor effect of doxorubicin in vivo in a breast cancer xenograft model.	2009 Jan 15	19003963
Therapeutic efficacy of seliciclib in combination with ionizing radiation for human nasopharyngeal carcinoma.	2009 Jun 1	19470731
Development of cell-cycle inhibitors for cancer therapy.	2009 Mar	19370178
Gateways to clinical trials.	2009 Nov	20094643
Delayed treatment with systemic (S)-roscovitine provides neuroprotection and inhibits in vivo CDK5 activity increase in animal stroke models.	2010 Aug 12	20711428
R-Roscovitine (Seliciclib) prevents DNA damage-induced cyclin A1 upregulation and hinders non-homologous end-joining (NHEJ) DNA repair.	2010 Aug 4	20684776
Phase I evaluation of seliciclib (R-roscovitine), a novel oral cyclin-dependent kinase inhibitor, in patients with advanced malignancies.	2010 Dec	20822897
Role of senescence and mitotic catastrophe in cancer therapy.	2010 Jan 21	20205872
Caffeine prevents transcription inhibition and P-TEFb/7SK dissociation following UV-induced DNA damage.	2010 Jun 21	20574533
Probing the probes: fitness factors for small molecule tools.	2010 Jun 25	20609406
Inhibition of human immunodeficiency virus type-1 by cdk inhibitors.	2010 Mar 24	20334651
Graphic rule for drug metabolism systems.	2010 May	20446902
Proliferative suppression by CDK4/6 inhibition: complex function of the retinoblastoma pathway in liver tissue and hepatoma cells.	2010 May	20100483
Application of new drugs in chronic lymphocytic leukemia.	2010 May 10	21415964
ATP-binding cassette B1 transports seliciclib (R-roscovitine), a cyclin-dependent kinase inhibitor.	2010 Nov	20699410
Role of NOXA and its ubiquitination in proteasome inhibitor-induced apoptosis in chronic lymphocytic leukemia cells.	2010 Sep	20378569
Cyclin-dependent kinase activity controls the onset of the HCMV lytic cycle.	2010 Sep 9	20844576
Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity.	2011 Oct 30	22037377
Use of ATP analogs to inhibit HIV-1 transcription.	2012 Oct 10	22771113
A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.	2013 Apr 15	23398362
Comparative structural and functional studies of 4-(thiazol-5-yl)-2-(phenylamino)pyrimidine-5-carbonitrile CDK9 inhibitors suggest the basis for isotype selectivity.	2013 Feb 14	23252711
Synergism of cyclin-dependent kinase inhibitors with camptothecin derivatives in small cell lung cancer cell lines.	2014 Feb 17	24549232
Aryl hydrocarbon receptor-dependent up-regulation of the heterodimeric amino acid transporter LAT1 (SLC7A5)/CD98hc (SLC3A2) by diesel exhaust particle extract in human bronchial epithelial cells.	2016 Jan 1	26621329

Sample Use Guides

In Vivo Use Guide

Cushing Disease: R-roscovitine 400 mg oral administration twice daily for 4 days every week for total of 4 weeks. cystic fibrosis: 200 or 400 mg roscovitine (8) or placebo (4) once daily for 4 cycles of 7 days (4 days "on" and 3 days "off")

Route of Administration: Oral

In Vitro Use Guide

CDK2 inhibitors have been proposed as effective anti-cancer therapeutics. It was shown that CYC202 (R-roscovitine) is a potent inhibitor of recombinant CDK2/cyclin E kinase activity (IC(50) = 0.10 microM) with an average cytotoxic IC(50) of 15.2 microM in a panel of 19 human tumour cell lines, and was also demonstrated selectivity for rapidly proliferating cells over non-proliferating cells. A study of the cell cycle effects of CYC202 in Lovo colorectal carcinoma cells showed that the major effect was not the predicted arrest in one part of the cycle, but rather an induction of cell death from all compartments of the cell cycle.

Substance Class	Chemical Created by `admin` on `Sat Jun 26 15:23:55 UTC 2021` Edited by `admin` on `Sat Jun 26 15:23:55 UTC 2021`
Record UNII	0ES1C2KQ94
Record Status	`Validated (UNII)`
Record Version

Download

Name

Type

Language

SELICICLIB

Official Name

English

AL-39256

Code

English

SELICICLIB [MI]

Common Name

English

R-ROSCOVITINE

Common Name

English

CYC-202

Code

English

(2R)-2-((6-BENZYLAMINO-9-(PROPAN-2-YL)-9H-PURIN-2-YL)AMINO)BUTAN-1-OL

Systematic Name

English

SELICICLIB [INN]

Common Name

English

SELICICLIB [WHO-DD]

Common Name

English

ROSCOVITINE

Common Name

English

NSC-701554

Code

English

ROSCOVITIN

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C2185