Formulation: A solid
Formal Name: N-(2,3-dihydro-1,4-benzodioxin-6-yl)-1,4-dihydro-indeno[1,2-c]pyrazol-3-amine
Purity: ≥98%
Formula Markup: C18H15N3O2
Formula Weight: 305,3
Shelf life (days): 1460
CAS Number: 1421448-26-1
Notes: GN44028 is an inhibitor of HIF-1α transcriptional activity.{51474} It reduces HIF-1α reporter gene expression in HeLa cervical cancer cells (IC50 = 14 nM). GN44028 induces cytotoxicity in HCT116 colorectal, HepG2 hepatic, PC3 prostate, and HeLa cancer cells (IC50s = 2.1, 3.7, 25.4, and 2.1 µM, respectively). It reduces the levels of VEGF, but not HIF-1α or HIF-1α-HIF-1β dimer levels, in HeLa cells when used at concentrations of 0.1 and 1 µM. In vivo, GN44028 (5 mg/kg twice per week), alone or in combination with 5-fluorouracil (Item. No. 14416), decreases tumor volume and the number of lung metastases and increases survival percentage in a CT26 murine colon cancer model.{51475}