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MedKoo Cat#: 206754 | Name: CEP-8983

Description:

WARNING: This product is for research use only, not for human or veterinary use.

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.

Chemical Structure

CEP-8983
CAS#374071-46-2

Theoretical Analysis

MedKoo Cat#: 206754

Name: CEP-8983

CAS#: 374071-46-2

Chemical Formula: C18H14N2O3

Exact Mass: 306.1004

Molecular Weight: 306.32

Elemental Analysis: C, 70.58; H, 4.61; N, 9.15; O, 15.67

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
No Data
Synonym
CEP-8983; CEP 8983; CEP8983; CK-102; CK102; CK 102.
IUPAC/Chemical Name
11-methoxy-4,5,6,7-tetrahydro-1H-cyclopenta[a]pyrrolo[3,4-c]carbazole-1,3(2H)-dione
InChi Key
BWVHYDYUKQEFHG-UHFFFAOYSA-N
InChi Code
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)
SMILES Code
O=C1NC(C2=C1C3=C(C4=C2CCC4)NC5=C3C(OC)=CC=C5)=O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 306.32 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
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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