产品
编 号:F514752
分子式:C25H30F3N5O4
分子量:521.53
产品类型
结构图
CAS No: 908115-27-5
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产品详情
生物活性:
SNX-5422 (PF-04929113), a prodrug of SNX-2112, is an orally active Hsp90 inhibitor, with a Kd of 41 nM, and also induces Her-2 degradation, with an IC50 of 37?nM.
体内研究:
SNX-5422 (50 mg/kg, p.o.) efficiently inhibits tumor growth of HT-29 human colon tumor xenograft model after administration 3 times a week for 3 weeks (qod×3/2×3). SNX-5422 (20, 40 mg/kg, p.o.) markedly inhibits multiple myeloma (MM) tumor growth and angiogenesis in mice.
体外研究:
SNX-5422 is an orally active Hsp90 inhibitor, with a Kd of 41 nM, and also induces Her-2 degradation, with an IC50 of 37?nM. SNX-5422 exhibits potent effects on Her2 and p-ERK stability in AU565 cells and p-S6 in A375 cells, with IC50s of 5?±?1, 11?±?3, and 61?±?22 nM, respectively. SNX-5422 also induces Hsp70 in A375 cells with an IC50 of 13?±?3 nM. SNX-5422 (SNX5422; 0.5, 1, 2, 5, and 10 μM) reduces cell viability in a concentration-dependent manner. Moreover, SNX-5422 (1, 3, 5, 7 μM) in combination with equal amounts of HDAC inhibitors (PXD101, SAHA, and TSA) synergistically induces cell death via suppression of PI3K/Akt/mTOR signaling in ATC cells.