| Identification | Back Directory | [Name]
Pyrazolo[3,4-b][1,4]benzodiazepine, 5-(2-chlorophenyl)-1,2-dihydro-7-methoxy-3-methyl- | [CAS]
303196-31-8 | [Synonyms]
R1498
R-1498
R 1498
Pyrazolo[3,4-b][1,4]benzodiazepine, 5-(2-chlorophenyl)-1,2-dihydro-7-methoxy-3-methyl- | [Molecular Formula]
C18H15ClN4O | [MOL File]
303196-31-8.mol | [Molecular Weight]
338.79 |
| Hazard Information | Back Directory | [Description]
R1498 is an inhibitor of cyclin-dependent kinase 2 (CDK2). It is well-tolerated and orally active for hepatocellular carcinoma and gastric cancer treatment and acts via targeting angiogenesis and mitosis pathways. | [Uses]
R1498 is a multi-target kinase inhibitor with anti-angiogenic and anti-proliferative activities. R1498 mainly targets targets such as Aurora kinase and VEGFR2, which are associated with tumor development. R1498 showed moderate in vitro growth inhibition in a variety of tumor cells, with IC50 values in the micromolar range. R1498 showed anti-tumor efficacy superior to sorafenib in a variety of gastric cancer and hepatocellular carcinoma xenograft models, with tumor growth inhibition rates exceeding 80%, and tumor shrinkage was observed in some models. R1498 showed a 10-30% tumor shrinkage rate in three xenograft models derived from human primary gastric cancer tumors, further demonstrating its inhibitory potential. R1498 effectively inhibited Aurora A activity in vivo and reduced tumor vascularization[1]. | [References]
[1] Small molecule R1498 as a well-tolerated and orally active kinase inhibitor for hepatocellular carcinoma and gastric cancer treatment via targeting angiogenesis and mitosis pathways DOI:10.1371/journal.pone.0065264 |
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