WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406625
Description: CEP-14083 is a potent ALK inhibitor that has shown activity in an NPM/ALKÂ–carrying T-cell lymphoma in vitro study. Presumably, this compound binds to the hinge region of the kinase in an ATP-competitive manner. CEP-14083 displays a potent activity against ALK in enzymatic assays (IC50 = 11 nmol/L). Further, CEP-14083 is also able to inhibit the insulin receptor at a concentration within a nanomolar range. In a preclinical assay, CEP-14083 showed that, via NPM/ALK TK inhibition, it could control the expression of molecules that determine T-cell identity and signaling in lymphoma cells. CEP-14083 has shown preclinical activity in both cell lines and animal models harboring ALK alteration.
MedKoo Cat#: 406625
Chemical Formula: C31H30N6O2
Exact Mass: 518.24302
Molecular Weight: 518.61
Elemental Analysis: C, 71.79; H, 5.83; N, 16.20; O, 6.17
Synonym: CEP14083; CEP 14083; CEP-14083.
IUPAC/Chemical Name: 1-methyl-3-(4-methyl-6-oxo-13-propyl-2,4,6,7,8,13-hexahydro-1H-indazolo[5,4-a]pyrrolo[3,4-c]carbazol-10-yl)-1-phenylurea
InChi Key: GOIITZJBPPEODD-UHFFFAOYSA-N
InChi Code: InChI=1S/C31H30N6O2/c1-4-14-37-25-13-10-18(33-31(39)36(3)19-8-6-5-7-9-19)15-21(25)27-22-16-32-30(38)28(22)26-20(29(27)37)11-12-24-23(26)17-35(2)34-24/h5-10,13,15,17H,4,11-12,14,16H2,1-3H3,(H,32,38)(H,33,39)
SMILES Code: CN(C(NC1=CC=C(N(CCC)C2=C3C4=C(C(NC4)=O)C5=C2CCC6=NN(C)C=C65)C3=C1)=O)C7=CC=CC=C7
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, not in water
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
The following data is based on the product molecular weight 518.61 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.
|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: Marzec M, Halasa K, Liu X, Wang HY, Cheng M, Baldwin D, Tobias JW, Schuster SJ, Woetmann A, Zhang Q, Turner SD, Ã˜dum N, Wasik MA. Malignant transformation of CD4+ T lymphocytes mediated by oncogenic kinase NPM/ALK recapitulates IL-2-induced cell signaling and gene expression reprogramming. J Immunol. 2013 Dec 15;191(12):6200-7. doi: 10.4049/jimmunol.1300744. Epub 2013 Nov 11. PubMed PMID: 24218456; PubMed Central PMCID: PMC3889215.
2: Passoni L, Longo L, Collini P, Coluccia AM, Bozzi F, Podda M, Gregorio A, Gambini C, Garaventa A, Pistoia V, Del Grosso F, Tonini GP, Cheng M, Gambacorti-Passerini C, Anichini A, Fossati-Bellani F, Di Nicola M, Luksch R. Mutation-independent anaplastic lymphoma kinase overexpression in poor prognosis neuroblastoma patients. Cancer Res. 2009 Sep 15;69(18):7338-46. doi: 10.1158/0008-5472.CAN-08-4419. Epub 2009 Sep 1. PubMed PMID: 19723661.
3: Marzec M, Zhang Q, Goradia A, Raghunath PN, Liu X, Paessler M, Wang HY, Wysocka M, Cheng M, Ruggeri BA, Wasik MA. Oncogenic kinase NPM/ALK induces through STAT3 expression of immunosuppressive protein CD274 (PD-L1, B7-H1). Proc Natl Acad Sci U S A. 2008 Dec 30;105(52):20852-7. doi: 10.1073/pnas.0810958105. Epub 2008 Dec 16. PubMed PMID: 19088198; PubMed Central PMCID: PMC2634900.
4: Boccalatte FE, Voena C, Riganti C, Bosia A, D'Amico L, Riera L, Cheng M, Ruggeri B, Jensen ON, Goss VL, Lee K, Nardone J, Rush J, Polakiewicz RD, Comb MJ, Chiarle R, Inghirami G. The enzymatic activity of 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase/IMP cyclohydrolase is enhanced by NPM-ALK: new insights in ALK-mediated pathogenesis and the treatment of ALCL. Blood. 2009 Mar 19;113(12):2776-90. doi: 10.1182/blood-2008-06-161018. Epub 2008 Oct 9. PubMed PMID: 18845790; PubMed Central PMCID: PMC2661863.
5: Wan W, Albom MS, Lu L, Quail MR, Becknell NC, Weinberg LR, Reddy DR, Holskin BP, Angeles TS, Underiner TL, Meyer SL, Hudkins RL, Dorsey BD, Ator MA, Ruggeri BA, Cheng M. Anaplastic lymphoma kinase activity is essential for the proliferation and survival of anaplastic large-cell lymphoma cells. Blood. 2006 Feb 15;107(4):1617-23. Epub 2005 Oct 27. PubMed PMID: 16254137.