CCT 137690
Cat. No.:YN270074
CAS No. :1095382-05-0
产品名称: | CCT 137690 |
CAS No.: | 1095382-05-0 |
Chemical Name: | 6-bromo-7-[4-[(5-methyl-3-isoxazolyl)methyl]-1-piperazinyl]-2-[4-(4-methyl-1-piperazinyl)phenyl]-3H-imidazo[4,5-b]pyridine |
Synonyms: | CCT137690 |
分子量: | 551.48 |
分子式: | C₂₆H₃₁BrN₈O |
SMILES: | CC1=CC(CN(CC2)CCN2C3=C4C(NC(C5=CC=C(N6CCN(C)CC6)C=C5)=N4)=NC=C3Br)=NO1 |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | CCT 137690是有效的,有口服活性的极光激酶 (aurora) 抑制剂,对极光激酶A,B,C的IC50值分别为15,25 和19 nM。 |
IC50和靶点: | [{name:"Aurora A:15 nM (IC50)"},{name: "Aurora B:25 nM (IC50)"},{name: "Aurora C:19 nM (IC50)"}] |
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Clinical Trial: | |
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Bavetsias, V., Crumpler, S., Sun, C., et al.Optimization of imidazo[4,5-b]pyridine-based kinase inhibitors: Identification of a dual FLT3/Aurora kinase inhibitor as an orally bioavailable preclinical development candidate for the treatment of acute myeloid leukemiaJ. Med. Chem.55(20),8721-8734(2012)
Faisal, A., Vaughan, L., Bavetsias, V., et al.The aurora kinase inhibitor CCT137690 downregulates MYCN and sensitizes MYCN-amplified neuroblastoma in vivoMol. Cancer Ther.10(11),2115-2123(2011)
Moore, A.S., Faisal, A., Gonzalez de Castro, D., et al.Selective FLT3 inhibition of FLT3-ITD+ acute myeloid leukaemia resulting in secondary D835Y mutation: a model for emerging clinical resistance patternsLeukemia26(7),1462-1470(2012)
Wu, X., Liu, W., Cao, Q., et al.Inhibition of Aurora B by CCT137690 sensitizes colorectal cells to radiotherapyJ. Exp. Clin. Cancer Res.33,1-9(2014)