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.
CAS 856692-39-2 MFCD56692392
化学结构图
SMILES: CCCn1c2ccc(NC(=O)N(C)c3ccccc3)cc2c2c3c(c4c(c21)CCc1nn(C)cc1-4)C(=O)NC3
化学属性
| Mol. Weight | 518.61 |
|---|---|
| Appearance | Solid powder |
| Solubility | Soluble in DMSO, not in water |
别名和识别编码
| Chemical Name | 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. |
|---|---|
| Formula | C31H30N6O2 |
| Synonym | CEP14083; CEP 14083; CEP-14083. |
| 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 |
| InChI | 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) |
| Canonical SMILES | 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 |
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- 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.
