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MedKoo product information:
Seliciclib: Seliciclib is an
orally bioavailable, small-molecule cyclin-dependent kinase (CDK)
inhibitor with potential proapoptotic and antineoplastic activities.
Seliciclib primarily inhibits CDK2/E, CDK2/A, CDK7 and CDK9 by competing
for their ATP binding sites, leading to a disruption of cell cycle
progression. In addition, this agent appears to interfere with
CDK-mediated phosphorylation of the carboxy-terminal domain of RNA
polymerase II, inhibiting RNA polymerase II-dependent transcription,
which may result in the down-regulation of antiapoptotic proteins such
as induced myeloid leukemia cell differentiation protein Mcl-1. CDKs,
serine/threonine kinases that play an important role in cell cycle
regulation, are overexpressed in various malignancies. Mcl-1 belongs to
the Bcl-2 family of antiapoptotic proteins and is a protein crucial to
the survival of a range of tumor cell types. Check for
active clinical trials or
closed clinical trials using this agent. (NCI
Cyclacel Pharmaceuticals, Inc.
MedKoo Code#: 202580
R-roscovitine. Code name: CYC202. CYC 202; R-Roscovitine; Roscovitin; Roscovitine; Seliciclib
MedKoo Code#: 202580
Chemical Formula: C19H26N6O
Exact Mass: 354.21681
Molecular Weight: 354.44
Elemental Analysis: C, 64.38; H, 7.39; N,
23.71; O, 4.51
Availability and price:
) is in stock.
Estimated delivery time: 4-6 days.
50mg / $380.00
100mg / $650.00
200mg / $850.00
500 mg /$1,550.00
Multiple grams in stock at low
To inquire quotation and lead time or to ask questions, please send email to
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will respond your email shortly. We offer big discount for orders of bulk quantities.
Product will be shipped with
supporting analytical data.
Information about this agent
Phase I trial of Selicilib:
Fifty-six patients received a total of 218 cycles of seliciclib.
Dose-Limiting Toxicities (DLT) consisting of nausea, vomiting, asthenia
and hypokalaemia occurred at 1600 mg bid for schedule A and in schedule
C, DLT of hypokalaemia and asthenia occurred at 1800 mg bid. The
evaluation of longer treatment duration in schedule B was discontinued
because of unacceptable toxicity at lower doses. Other adverse events
included transient serum creatinine increases and liver dysfunctions.
Pharmacokinetic data showed that exposure to seliciclib and its
carboxylate metabolite increased with increasing dose. Soluble
cytokeratin 18 fragments allowed monitoring of seliciclib-induced cell
death in the blood of patients treated with seliciclib at doses above
800 mg/d. One partial response in a patient with hepatocellular
carcinoma and sustained tumour stabilisations were observed. The MTD and
RD for seliciclib are 1250 mg bid for 5d every 3 weeks and 1600 mg bid
for 3d every 2 weeks, respectively. (Eur J Cancer. 2010
1: Coley HM, Safuwan NA, Chivers P, Papacharalbous E,
Giannopoulos T, Butler-Manuel S, Madhuri K, Lovell DP, Crook T. The
cyclin-dependent kinase inhibitor p57(Kip2) is epigenetically regulated
in carboplatin resistance and results in collateral sensitivity to the
CDK inhibitor seliciclib in ovarian cancer. Br J Cancer. 2012 Jan 10.
doi: 10.1038/bjc.2011.566. [Epub ahead of print] PubMed PMID: 22233925.
2: Sheryanna AM, Smith J, Bhangal G, Barnett A, McClue S, Tam FW, Cook
T, Pusey CD. Treatment with a cyclin-dependent kinase inhibitor,
seliciclib, is effective in reducing glomerular macrophage numbers and
the severity of established experimental glomerulonephritis. Nephrology
(Carlton). 2011 May;16(4):410-6. doi: 10.1111/j.1440-1797.2010.01416.x.
PubMed PMID: 21518118.
3: Le Tourneau C, Faivre S, Laurence V, Delbaldo C, Vera K, Girre V,
Chiao J, Armour S, Frame S, Green SR, Gianella-Borradori A, Diéras V,
Raymond E. Phase I evaluation of seliciclib (R-roscovitine), a novel
oral cyclin-dependent kinase inhibitor, in patients with advanced
malignancies. Eur J Cancer. 2010 Dec;46(18):3243-50. Epub 2010 Sep 6.
PubMed PMID: 20822897.
4: Rajnai Z, Méhn D, Beéry E, Okyar A, Jani M, Tóth GK, Fülöp F, Lévi F,
Krajcsi P. ATP-binding cassette B1 transports seliciclib (R-roscovitine),
a cyclin-dependent kinase inhibitor. Drug Metab Dispos. 2010
Nov;38(11):2000-6. Epub 2010 Aug 10. PubMed PMID: 20699410.
5: Federico M, Symonds CE, Bagella L, Rizzolio F, Fanale D, Russo A,
Giordano A. R-Roscovitine (Seliciclib) prevents DNA damage-induced
cyclin A1 upregulation and hinders non-homologous end-joining (NHEJ) DNA
repair. Mol Cancer. 2010 Aug 4;9:208. PubMed PMID: 20684776; PubMed
Central PMCID: PMC3224749.
6: Aldoss IT, Tashi T, Ganti AK. Seliciclib in malignancies. Expert Opin
Investig Drugs. 2009 Dec;18(12):1957-65. PubMed PMID: 19938906.
7: Rogalińska M, Błoński JZ, Komina O, Góralski P, Zołnierczyk JD,
Piekarski H, Robak T, Kiliańska ZM, Wesierska-Gadek J. R-roscovitine (Seliciclib)
affects CLL cells more strongly than combinations of fludarabine or
cladribine with cyclophosphamide: Inhibition of CDK7 sensitizes leukemic
cells to caspase-dependent apoptosis. J Cell Biochem. 2010 Jan
1;109(1):217-35. PubMed PMID: 19911397.
8: Iurisci I, Filipski E, Sallam H, Harper F, Guettier C, Maire I,
Hassan M, Iacobelli S, Lévi F. Liver circadian clock, a pharmacologic
target of cyclin-dependent kinase inhibitor seliciclib. Chronobiol Int.
2009 Aug;26(6):1169-88. PubMed PMID: 19731111.
9: Hui AB, Yue S, Shi W, Alajez NM, Ito E, Green SR, Frame S, O'Sullivan
B, Liu FF. Therapeutic efficacy of seliciclib in combination with
ionizing radiation for human nasopharyngeal carcinoma. Clin Cancer Res.
2009 Jun 1;15(11):3716-24. Epub 2009 May 26. PubMed PMID: 19470731.
10: Hsieh WS, Soo R, Peh BK, Loh T, Dong D, Soh D, Wong LS, Green S,
Chiao J, Cui CY, Lai YF, Lee SC, Mow B, Soong R, Salto-Tellez M, Goh BC.
Pharmacodynamic effects of seliciclib, an orally administered cell cycle
modulator, in undifferentiated nasopharyngeal cancer. Clin Cancer Res.
2009 Feb 15;15(4):1435-42. PubMed PMID: 19228744.
11: Appleyard MV, O'Neill MA, Murray KE, Paulin FE, Bray SE, Kernohan
NM, Levison DA, Lane DP, Thompson AM. Seliciclib (CYC202, R-roscovitine)
enhances the antitumor effect of doxorubicin in vivo in a breast cancer
xenograft model. Int J Cancer. 2009 Jan 15;124(2):465-72. PubMed PMID:
(Keyword; CAS#; MedKoo code#)