AT-533

AT-533 is a potent Hsp90 and HSV inhibitor. AT-533 suppresses tumor growth and angiogenesis by blocking the HIF-1α/VEGF/VEGFR-2 signaling pathway. AT-533 also inhibits the activation of the downstream pathways, including Akt/mTOR/p70S6K , Erk1/2 and FAK . AT-533 inhibits the tube formation, cell migration, and invasion of human umbilical vein endothelial cells (HUVECs) In Vitro AT-533 (0-1350 nM; 24 h or 48 h) inhibits 20 ng/mL VEGF-induced tube formation, cell migration, and invasion of HUVECs. AT-533 (2 μM or 75 μM; 24 h) inhibits the HIF-1α/VEGF signaling pathway in hypoxia-induced breast cancer cells, as well as inhibiting Akt/mTOR/p70S6K, Erk1/2, and FAK phosphorylation. AT-533 (10 nM, 50 nM; 48 h) shows anti-angiogenic ability in chorioallantoic membrane (CAM) model. AT-533 (0.5 μM; 2 h, 4 h) decreases TNF-α, IL-1β and IL-6 production in RAW264.7 and BV2 cells induced by HSV-1. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: Human umbilical vein endothelial cells (HUVECs): MCF-7 and MDA-MB-231 Concentration: 0, 5.6, 16.7, 50, 150, 450, and 1350 nM Incubation Time: 12 h, 24 h, 48 h, and 72 h Result: Inhibited cell viability at 48 h with an IC 50 value of 50.1 nM. Western Blot AnalysisCell Line: MCF-7 cells and MDA-MB-231 cells Concentration: 5 nM, 10 nM, 50 nM, and 75 nM Incubation Time: 24 h Result: Inhibited the phosphorylation of VEGF-2, Akt, mTOR, Erk1/2, FAK. In Vivo AT-533 (10 mg/kg; i.p.; once daily for 21 d) suppresses the expression of the HIF-1α/VEGF signaling pathway-related proteins in MDA-MB-231 breast cancer xenografts tumor model in mouse . AT-533 (1, 2 and 4 mg/kg; i.p.; once daily for 30 d) has no mortality, loss of appetite and body weight, adverse reactions in Sprague-Dawley rats in subacute toxicity test. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male C57BL/6 mice with MDA-MB-231 breast cancer xenografts Dosage: 10 mg/kg; Administration: Intraperitoneal injection; once daily for 21 days Result: Significantly downregulated HIF-1α and VEGF expression. Form:Solid IC50& Target:HSP90 HSV-1 ERK1 ERK2 NF-κB Akt HIF-1α VEGF/VEGFR-2

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