An Aurora kinase inhibitor; inhibits Aurora A and B by 82 and 60%

CCT129202 – 5 mg

Brand:
Cayman
CAS:
942947-93-5
Storage:
-20
UN-No:
De Minimis - 3077 / 9

CCT129202 is an Aurora kinase inhibitor that inhibits Aurora A and B by 82 and 60%, respectively, when used at a concentration of 1 μM in cell-free assays.{45586} It is selective for Aurora A and B over a panel of 13 kinases at 1 μM. CCT129202 inhibits growth of COLO 205, SW620, HCT116, HT-29, KW12, HeLa, A2780, OVCAR-8, MDA-MB-157, and MB4-11 cancer cells (GI50s = 0.08-1.2 μM). It induces DNA accumulation and cell cycle arrest at the G2/M phase, as well as apoptosis in HCT116 cells. CCT129202 increases the accumulation of doxorubicin and rhodamine 123 in multidrug-resistant (MDR) KBv200 and MCF-7/adr cells and increases the susceptibility of MDR KBv200, MCF-7/adr, S1-M1-80, and HL60/adr cells to cisplatin (Item No. 13119) and doxorubicin (Item No. 15007).{45587} In vivo, CCT129202 (100 mg/kg) reduces tumor growth in an HCT116 mouse xenograft model.{45586} It also potentiates the antitumor effects of vincristine (Item No. 11764) in a KBv200 mouse xenograft model.{45587}  

 

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Description

An Aurora kinase inhibitor; inhibits Aurora A and B by 82 and 60%, respectively, at 1 μM in cell free assays; selective for Aurora A and B over a panel of 13 kinases at 1 μM; inhibits growth of various cancer cell lines (GI50s = 0.08-1.2 μM); induces DNA accumulation and cell cycle arrest at the G2/M phase, as well as apoptosis in HCT116 cells; increases the accumulation of doxorubicin and rhodamine 123 in MDR KBv200 and MCF-7/adr cells and increases the susceptibility of MDR KBv200, MCF-7/adr, S1-M1-80, and HL60/adr cells to cisplatin and doxorubicin; reduces tumor growth in an HCT116 mouse xenograft model at 100 mg/kg; potentiates the antitumor effects of vincristine in a KBv200 mouse xenograft model

Formal name: 4-[6-chloro-2-[4-(dimethylamino)phenyl]-3H-imidazo[4,5-b]pyridin-7-yl]-N-2-thiazolyl-1-piperazineacetamide

Synonyms: 

Molecular weight: 497

CAS: 942947-93-5

Purity: ≥98%

Formulation: A crystalline solid

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