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374071-46-2
  • names:

    11-methoxy-4,5,6,7-tetrahydro-1H-cyclopenta[a]pyrrolo[3,4-c]carbazole-1,3(2H)-dione

  • CAS号:

    374071-46-2

    MDL Number:
  • MF(分子式): C18H14N2O3 MW(分子量): 306.321
  • EINECS: Reaxys Number:
  • Pubchem ID: Brand:BIOFOUNT
CEP-8983
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中文别名 CEP-8983
英文别名 CEP-8983; CEP 8983; CEP8983; CK-102; CK102; CK 102.
CAS号 374071-46-2
SMILES O=C1NC(C2=C1C3=C(C4=C2CCC4)NC5=C3C(OC)=CC=C5)=O
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
闪点 FP
熔点 Melting point
沸点 Boiling point
Polarizability极化度
密度 Density
蒸汽压 Vapor Pressure
溶解度Solubility
性状 Solid powder
储藏条件 Storage conditions Dry, dark and store at 0-4℃ for short term (days to weeks) or -20℃ for long term (Store correctly 2-3years).
产品说明 CEP-8983(CAS:374071-46-2):仅限应用于工业或者科学研究过程中非医疗目的,不应用于人类或动物的临床诊断以及治过程疗,该产品非药用,非食用。
IntroductionCEP-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
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安全声明
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备注
[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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