購物車 
-
CEP-8983
- 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
| 貨品編碼 | 規格 | 純度 | 價格 (￥) | 現價(￥) | 特價(￥) | 庫存描述 | 數量 | 總計 (￥) |
|---|
| 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). |
| 產品說明 | CEP-8983(CAS:374071-46-2):僅限應用于工業或者科學研究過程中非醫療目的，不應用于人類或動物的臨床診斷以及治過程療，該產品非藥用，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 |
| [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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