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CEP-8983

NMR下載 COA and HPLC MSDS下載
names：
11-methoxy-4,5,6,7-tetrahydro-1H-cyclopenta[a]pyrrolo[3,4-c]carbazole-1,3(2H)-dione
CAS號：
374071-46-2
MDL Number：
MF(分子式)： C18H14N2O3 MW(分子量)： 306.321
EINECS: Reaxys Number:
Pubchem ID: Brand:BIOFOUNT

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中文別名	CEP-8983
英文別名	CEP-8983; CEP 8983; CEP8983; CK-102; CK102; CK 102.
CAS號	374071-46-2
Inchi	InChI=1S/C18H14N2O3/c1-23-11-7-3-6-10-13(11)14-15-12(17(21)20-18(15)22)8-4-2-5-9(8)16(14)19-10/h3,6-7,19H,2,4-5H2,1H3,(H,20,21,22)
InchiKey	BWVHYDYUKQEFHG-UHFFFAOYSA-N
分子式 Formula	C18H14N2O3
分子量 Molecular Weight	306.321
溶解度Solubility
性狀	Solid powder
儲藏條件 Storage conditions	Dry, dark and store at 0-4℃ for short term (days to weeks) or -20℃ for long term (Store correctly 2-3years).

產(chǎn)品說明	CEP-8983(CAS:374071-46-2):僅限應(yīng)用于工業(yè)或者科學(xué)研究過程中非醫(yī)療目的，不應(yīng)用于人類或動物的臨床診斷以及治過程療，該產(chǎn)品非藥用，非食用。
Introduction	CEP-8983, also known CK-102, is a PARP inhibitor potentially for the treatment of solid tumours. CEP-8983 synergizes with bendamustine in chronic lymphocytic leukemia cells in vitro. CEP-8983, increases the sensitivity of chemoresistant tumor cells to temozolomide and irinotecan but does not potentiate myelotoxicity.
Application1
Application2
Application3

警示圖
危險性	Warning
危險性警示
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備注

[1]Awada A, Campone M, Varga A, Aftimos P, Frenel JS, Bahleda R, Gombos A, Bourbouloux E, Soria JC. An open-label, dose-escalation study to evaluate the safety and pharmacokinetics of CEP-9722 (a PARP-1 and PARP-2 inhibitor) in combination with gemcitabine and cisplatin in patients with advanced solid tumors. Anticancer Drugs. 2016 Apr;27(4):342-8. doi: 10.1097/CAD.0000000000000336. PubMed PMID: 26796987.

[2]Plummer R, Stephens P, Aissat-Daudigny L, Cambois A, Moachon G, Brown PD, Campone M. Phase 1 dose-escalation study of the PARP inhibitor CEP-9722 as monotherapy or in combination with temozolomide in patients with solid tumors. Cancer Chemother Pharmacol. 2014 Aug;74(2):257-65. doi: 10.1007/s00280-014-2486-9. PubMed PMID: 24880570; PubMed Central PMCID: PMC4112042.

[3] Jian W, Xu HG, Chen J, Xu ZX, Levitt JM, Stanley JA, Yang ES, Lerner SP, Sonpavde G. Activity of CEP-9722, a poly (ADP-ribose) polymerase inhibitor, in urothelial carcinoma correlates inversely with homologous recombination repair response to DNA damage. Anticancer Drugs. 2014 Sep;25(8):878-86. doi: 10.1097/CAD.0000000000000114. PubMed PMID: 24714082.

[4] Lawlor D, Martin P, Busschots S, Thery J, O'Leary JJ, Hennessy BT, Stordal B. PARP Inhibitors as P-glyoprotein Substrates. J Pharm Sci. 2014 Jun;103(6):1913-20. doi: 10.1002/jps.23952. PubMed PMID: 24700236.

[5] Dilley RL, Poh W, Gladstone DE, Herman JG, Showel MM, Karp JE, McDevitt MA, Pratz KW. Poly(ADP-ribose) polymerase inhibitor CEP-8983 synergizes with bendamustine in chronic lymphocytic leukemia cells in vitro. Leuk Res. 2014 Mar;38(3):411-7. doi: 10.1016/j.leukres.2013.12.019. PubMed PMID: 24439051; PubMed Central PMCID: PMC4142574.

6: Michels J, Vitale I, Senovilla L, Enot DP, Garcia P, Lissa D, Olaussen KA, Brenner C, Soria JC, Castedo M, Kroemer G. Synergistic interaction between cisplatin and PARP inhibitors in non-small cell lung cancer. Cell Cycle. 2013 Mar 15;12(6):877-83. doi: 10.4161/cc.24034. PubMed PMID: 23428903; PubMed Central PMCID: PMC3637345.7: Olaussen KA, Adam J, Vanhecke E, Vielh P, Pirker R, Friboulet L, Popper H, Robin A, Commo F, Thomale J, Kayitalire L, Filipits M, Le Chevalier T, André F, Brambilla E, Soria JC. PARP1 impact on DNA repair of platinum adducts: preclinical and clinical read-outs. Lung Cancer. 2013 May;80(2):216-22. doi: 10.1016/j.lungcan.2013.01.014. PubMed PMID: 23410825.8: Miknyoczki S, Chang H, Grobelny J, Pritchard S, Worrell C, McGann N, Ator M, Husten J, Deibold J, Hudkins R, Zulli A, Parchment R, Ruggeri B. The selective poly(ADP-ribose) polymerase-1(2) inhibitor, CEP-8983, increases the sensitivity of chemoresistant tumor cells to temozolomide and irinotecan but does not potentiate myelotoxicity. Mol Cancer Ther. 2007 Aug;6(8):2290-302. PubMed PMID: 17699724.

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