856692-39-2
Chemical Structure
CEP-14083
- CAS No.: 856692-39-2
- Formula:C31H30N6O2
- Molecular Weight:518.61
IUPAC 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
InChIKey: GOIITZJBPPEODD-UHFFFAOYSA-N
SMILES: CN1N=C2CCC3=C4N(C5=CC=C(C=C5C4=C(CNC6=O)C6=C3C2=C1)NC(N(C7=CC=CC=C7)C)=O)CCC
Biological Activity: 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].
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CEP-14083 | 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. | |||||||||||||||||||||
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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. [Content Brief]
- [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. [Content Brief]
