target/VEGFR/2

VEGFR-2-IN-51 (compound 19) 作为一种口服活性的双靶点抑制剂,针对VEGFR-2 (IC50=15.33 μM) 和tubulin (IC50=0.76 μM) 显示出了抗肿瘤活性.该化合物通过降低线粒体膜电位并提高活性氧 (ROS) 的水平来诱导肿瘤细胞的凋亡 (apoptosis).它还通过阻断VEGFR-2 PI3K AKT信号通路实现抗血管生成的效果.此外,VEGFR-2-IN-51 在对抗胃癌细胞系MGC-803时表现出极佳的抗增殖活性,其IC50值仅为0.005 μM.

The Immuno-Oncology Screening Library consists of 2 plates and contains more than 90 cancer and immunology-associated compounds in a 96-well Matrix tube rack format as 10 mM stock solutions in DMSO. This library includes a variety of immuno-oncology target modulators, including but not limited to, adenosine, CCR, CXCR, and TLR agonists and antagonists, BTK, PI3K, VEGFR, and BRAF inhibitors, PD-1/PDL-1 interaction inhibitors, and HDAC inhibitors. Please review the product insert for a full list of targets. Stability data is not available for the compounds as supplied in the screening library.

PTC299 ((4-chlorophenyl) (1S)-6-chloro-1-(4-methoxyphenyl)-1,3,4,9-tetrahydropyrido[3,4-b]indole-2-carboxylate) 是一种口服活性的 VEGFA mRNA 翻译抑制剂，可选择性地抑制转录后水平的 VEGF 蛋白合成。它还是二氢乳酸脱氢酶 (DHODH) 的有效抑制剂，可研究血液系统恶性肿瘤。