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| | Urea, N'-(4,5,6,11,12,13-hexahydro-2-Methyl-4-oxo-11-propyl-2H-indazolo[5,4-a]pyrrolo[3,4-c]carbazol-8-yl)-N-Methyl-N-phenyl- Basic information |
| Product Name: | Urea, N'-(4,5,6,11,12,13-hexahydro-2-Methyl-4-oxo-11-propyl-2H-indazolo[5,4-a]pyrrolo[3,4-c]carbazol-8-yl)-N-Methyl-N-phenyl- | | Synonyms: | Urea, N'-(4,5,6,11,12,13-hexahydro-2-Methyl-4-oxo-11-propyl-2H-indazolo[5,4-a]pyrrolo[3,4-c]carbazol-8-yl)-N-Methyl-N-phenyl-;DRYABXKGCXCACQ-UHFFFAOYSA-N;CEP-14083 | | CAS: | 856692-39-2 | | MF: | C31H30N6O2 | | MW: | 518.61 | | EINECS: | | | Product Categories: | | | Mol File: | 856692-39-2.mol | ![Urea, N'-(4,5,6,11,12,13-hexahydro-2-Methyl-4-oxo-11-propyl-2H-indazolo[5,4-a]pyrrolo[3,4-c]carbazol-8-yl)-N-Methyl-N-phenyl- Structure](CAS/GIF/856692-39-2.gif) |
| | Urea, N'-(4,5,6,11,12,13-hexahydro-2-Methyl-4-oxo-11-propyl-2H-indazolo[5,4-a]pyrrolo[3,4-c]carbazol-8-yl)-N-Methyl-N-phenyl- Chemical Properties |
| Boiling point | 833.7±65.0 °C(Predicted) | | density | 1.40±0.1 g/cm3(Predicted) | | pka | 13.95±0.20(Predicted) |
| | Urea, N'-(4,5,6,11,12,13-hexahydro-2-Methyl-4-oxo-11-propyl-2H-indazolo[5,4-a]pyrrolo[3,4-c]carbazol-8-yl)-N-Methyl-N-phenyl- Usage And Synthesis |
| Description | CEP-14083 is a potent ALK inhibitor that has shown activity in an NPM/ALK–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. | | Uses | CEP-14083 is a ATP-competitive ALK kinase inhibitor with an IC50 value in enzymatic assays of 2 nM. CEP-14083 also inhibits other kinases, such as insulin receptor (IR), vascular endothelial growth factor receptor 2 (VEGFR2), angiopoietin-1 receptor (TIE2) and dual leucine zipper kinase (DLK). CEP-14083 suppresses CD274 mRNA expression and the NPM/ALK function in the NPM/ALK-carrying T cell lymphoma (ALK+TCL) cells. CEP-14083 is promising for research of lymphoma[1][2]. | | References | [1] Puig de la Bellacasa R, et al. ALK and ROS1 as a joint target for the treatment of lung cancer: a review. Transl Lung Cancer Res. 2013 Apr;2(2):72-86. DOI:10.3978/j.issn.2218-6751.2013.03.1 [2] Marzec M, et al. 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 |
| | Urea, N'-(4,5,6,11,12,13-hexahydro-2-Methyl-4-oxo-11-propyl-2H-indazolo[5,4-a]pyrrolo[3,4-c]carbazol-8-yl)-N-Methyl-N-phenyl- Preparation Products And Raw materials |
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