An inhibitor of TOPK (IC50 = 2.6 nM); selectively inhibits growth of patient-derived AML cells over normal CD34+ cells; inhibits growth of small cell lung

OTS514 – 1 mg

Brand:
Cayman
CAS:
1338540-63-8
Storage:
-20
UN-No:
De Minimis - 3077 / 9

OTS514 is an inhibitor of lymphokine-activated killer T cell-originated protein kinase (TOPK; IC50 = 2.6 nM), a serine-threonine kinase often overexpressed and transactivated in several types of cancer.{32494,37578} OTS514 (10 nM) selectively inhibits growth of patient-derived acute myeloid leukemia (AML) cells over normal CD34+ cells. It shows similar growth inhibitory effects in multiple small cell lung, kidney, and ovarian cancer cell lines (IC50s = 0.4-42.6 nM).{37579,37580,32493} In vivo, OTS514 (25 and 50 mg/kg) increases survival in a peritoneal mouse dissemination model of ovarian cancer. It also dose-dependently inhibits tumor growth in an A549 mouse xenograft model when administered at doses of 1, 2.5, and 5 mg/kg.{32494}  

 

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Description

An inhibitor of TOPK (IC50 = 2.6 nM); selectively inhibits growth of patient-derived AML cells over normal CD34+ cells; inhibits growth of small cell lung, kidney, and ovarian cancer cell lines (IC50s = 0.4-42.6 nM); increases survival in a peritoneal mouse dissemination model of ovarian cancer at 25 and 50 mg/kg; dose-dependently inhibits tumor growth in an A549 mouse xenograft model at 1, 2.5, and 5 mg/kg

Formal name: 9-[4-[(1R)-2-amino-1-methylethyl]phenyl]-8-hydroxy-6-methyl-thieno[2,3-c]quinolin-4(5H)-one

Synonyms: 

Molecular weight: 364.5

CAS: 1338540-63-8

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Serine/Threonine Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling

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