GN44028

GN44028 is an inhibitor of HIF-1alpha transcriptional activity. It reduces HIF-1alpha 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-1alpha or HIF-1alpha-HIF-1beta 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.Formal Name: N-(2,3-dihydro-1,4-benzodioxin-6-yl)-1,4-dihydro-indeno[1,2-c]pyrazol-3-amine. CAS Number: 1421448-26-1. Molecular Formula: C18H15N3O2. Formula Weight: 305.3. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: Methanol: soluble. lambdamax: 264 nm. SMILES: C1(NN=C2NC3=CC=C4OCCOC4=C3)=C2CC5=CC=CC=C15. InChi Code: InChI=1S/C18H15N3O2/c1-2-4-13-11(3-1)9-14-17(13)20-21-18(14)19-12-5-6-15-16(10-12)23-8-7-22-15/h1-6,10H,7-9H2,(H2,19,20,21). InChi Key: CGZKSZVSWAAUHE-UHFFFAOYSA-N.