产品
编 号：F477413
分子式：C21H23Cl2N5O2S
分子量：480.41
分子式：C21H23Cl2N5O2S
分子量：480.41
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
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1mg
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5mg
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10mg
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50mg
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100mg
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结构图
CAS No: 847559-80-2
产品详情
生物活性：
VER-82576 (NVP-BEP800) is a potent, orally available and selective Hsp90 inhibitor, with an IC50 of 58 nM for Hsp90β; VER-82576 also slightly blocks Grp94 and Trap-1, with IC50s of 4.1 and 5.5 μM, respectively.
体内研究：
VER-82576 (NVP-BEP800; 15 or 30 mg/kg, p.o.) shows antitumor activities in A375 cancer xenografts and BT-474 xenograft-bearing mice.
体外研究：
VER-82576 (NVP-BEP800) is a potent and selective Hsp90 inhibitor, with an IC50 of 58 nM for Hsp90β and is >70-fold selective against Grp94 and Trap-1, with IC50s of 4.1 ± 1.1 and 5.5 ± 0.48 μM. VER-82576 potently inhibits the proliferation of tumor cells, with GI50s ranging from 38 nM in A375 cells to 1050 nM in PC3 cells, with an average GI50 of 245 nM. VER-82576 (250-1250 nM) depletes client proteins in human cancer cell lines in vitro. VER-82576 (NVP-BEP800; 200 nM) shows no significant effect on the ionizing radiation (IR) dose-response curves of A549 cells, and is less toxic to SNB19 cells. VER-82576 in combination with IR results in more severe DNA damage in both A549 and SNB19 cell lines than each treatment alone and also protracts the kinetics of DNA damage repair in SNB19 cells. VER-82576 (NVP-BEP800; 0.05, 0.1 or 0.2 μM) dose-dependently decreases the viability and induces apoptosis of glioblastoma cells. VER-82576 (0.2 μM) suppresses the expression of IKKβ protein but does not alter the levels of IKKβ mRNA in T98G cells. VER-82576 (0.2 μM) suppresses the expression of heat shock protein 70.
VER-82576 (NVP-BEP800) is a potent, orally available and selective Hsp90 inhibitor, with an IC50 of 58 nM for Hsp90β; VER-82576 also slightly blocks Grp94 and Trap-1, with IC50s of 4.1 and 5.5 μM, respectively.
体内研究：
VER-82576 (NVP-BEP800; 15 or 30 mg/kg, p.o.) shows antitumor activities in A375 cancer xenografts and BT-474 xenograft-bearing mice.
体外研究：
VER-82576 (NVP-BEP800) is a potent and selective Hsp90 inhibitor, with an IC50 of 58 nM for Hsp90β and is >70-fold selective against Grp94 and Trap-1, with IC50s of 4.1 ± 1.1 and 5.5 ± 0.48 μM. VER-82576 potently inhibits the proliferation of tumor cells, with GI50s ranging from 38 nM in A375 cells to 1050 nM in PC3 cells, with an average GI50 of 245 nM. VER-82576 (250-1250 nM) depletes client proteins in human cancer cell lines in vitro. VER-82576 (NVP-BEP800; 200 nM) shows no significant effect on the ionizing radiation (IR) dose-response curves of A549 cells, and is less toxic to SNB19 cells. VER-82576 in combination with IR results in more severe DNA damage in both A549 and SNB19 cell lines than each treatment alone and also protracts the kinetics of DNA damage repair in SNB19 cells. VER-82576 (NVP-BEP800; 0.05, 0.1 or 0.2 μM) dose-dependently decreases the viability and induces apoptosis of glioblastoma cells. VER-82576 (0.2 μM) suppresses the expression of IKKβ protein but does not alter the levels of IKKβ mRNA in T98G cells. VER-82576 (0.2 μM) suppresses the expression of heat shock protein 70.
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