vegfr-2-in-9

VEGFR-2-IN-9 (KDR-in-4) is a potent KDR/VEGFR2 inhibitor with an IC50 of 7 nM, suitable for breast cancer research.

EGFR/VEGFR2-IN-3 (compound 9) is an effective inhibitor of EGFR and VEGFR-2, demonstrating IC50 values of 0.129 µM for EGFR, 0.142 µM for VEGFR-2, and 3.428 µM for COX-2. This compound exhibits cytotoxic properties and induces cell apoptosis (apoptosis) as well as cell cycle arrest at the G2/M phase.

HDAC1-IN-9 (13c) is an HDAC1 inhibitor. It inhibits the HDAC1 enzyme with an IC50 value of 1.07 µM. This compound exhibits the strongest antiproliferative activity against HT-29 (human colon adenocarcinoma cells), with an IC50 of 1.78 μM. In HCT-116 (human colon cancer cells), HDAC1-IN-9 significantly induces apoptosis. Additionally, HDAC1-IN-9 possesses antiangiogenic properties, reducing the expression levels of VEGFR-2 and phosphorylated VEGFR-2 (pVEGFR-2) by approximately 80%.

Apoptotic agent-4 (Compound 9) is an apoptosis inducer. It inhibits VEGFR-2 with an IC50 of 0.5717 μM. Apoptotic agent-4 also suppresses the proliferation of cancer cells, causing cell cycle arrest in the G2/M and Pre-G1 phases.

hCA/VEGFR-2-IN-5 (compound 9) is an indolinone phenylsulfonamide and a potential dual inhibitor of hCA IX/XII and VEGFR-2, which are associated with cancer. The compound has IC50 values of 0.38 μM for VEGFR-2, 40 nM for hCA IX, and 3.2 nM for hCA XII. It exhibits antitumor activity.

OSI-930, an orally active inhibitor of c-Kit and the vascular endothelial growth factor receptor-2 (VEGFR-2), targets cancer cell proliferation and blood vessel growth (angiogenesis) in tumors.