产品
编 号：F715483
分子式：C30H33N5O3
分子量：511.61
分子式：C30H33N5O3
分子量：511.61
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 2451862-42-1
产品详情
生物活性：
GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models.
体内研究：
GSK778 (15?mg/kg/BID; i.p. for 30 days) offers a superior survival advantage to iBET-BD2 in the aggressive MLL-AF9 AML model.?GSK778 (15?mg/kg/BID; s.c. for 14 days) reduces the production of anti-keyhole limpet hemocyanin (KLH) IgM and is well tolerated.?GSK778 exhibits Cmax (85 ng/mL), Tmax (1.48 h) and AUC∞ (132 ng.h/mL) following oral administration (10?mg/kg) in mice.Animal Model:6-8 weeks female C57BL/6 mice are injected with MLL-AF9 cells
Dosage:15?mg/kg/BID
Administration:I.p. injections for 30 days
Result:Increased the survival rate of leukemia mice.
Animal Model:Male CD1 mice
Dosage:10?mg/kg (Pharmacokinetic Analysis)
Administration:P.o. administration
Result:Cmax (85 ng/mL), Tmax (1.48 h); AUC∞ (132 ng.h/mL).
体外研究：
GSK778 inhibits BRD BD2 with the IC50s of 3950 nM (BRD2 BD2), 1210 nM (BRD3 BD2), 5843 nM (BRD4 BD2), and 17451 nM (BRDT BD2), respectively.?GSK778 (0.01-10 μM; 72 hours) inhibits the proliferative activity of human primary CD4+ T cells and the production of effector cytokines including IFNγ, IL-17A and IL-22.?GSK778 (0.001-10 μM; 5 days) has a more pronounced effect on the growth and viability of MDA-453, MOLM-13, K562, MV4-11, THP-1, and MDA-MB-231 cells.?GSK778 (1000 nM; 72 hours) inhibits proliferation, induces a cell cycle arrest and apoptosis in MV4-11, MOLM13, MDA-MB-231 and MB453 cells.?GSK778 (1000 nM; 12 days) reduces the clonogenic capacity of primary human AML cells.
GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models.
体内研究：
GSK778 (15?mg/kg/BID; i.p. for 30 days) offers a superior survival advantage to iBET-BD2 in the aggressive MLL-AF9 AML model.?GSK778 (15?mg/kg/BID; s.c. for 14 days) reduces the production of anti-keyhole limpet hemocyanin (KLH) IgM and is well tolerated.?GSK778 exhibits Cmax (85 ng/mL), Tmax (1.48 h) and AUC∞ (132 ng.h/mL) following oral administration (10?mg/kg) in mice.Animal Model:6-8 weeks female C57BL/6 mice are injected with MLL-AF9 cells
Dosage:15?mg/kg/BID
Administration:I.p. injections for 30 days
Result:Increased the survival rate of leukemia mice.
Animal Model:Male CD1 mice
Dosage:10?mg/kg (Pharmacokinetic Analysis)
Administration:P.o. administration
Result:Cmax (85 ng/mL), Tmax (1.48 h); AUC∞ (132 ng.h/mL).
体外研究：
GSK778 inhibits BRD BD2 with the IC50s of 3950 nM (BRD2 BD2), 1210 nM (BRD3 BD2), 5843 nM (BRD4 BD2), and 17451 nM (BRDT BD2), respectively.?GSK778 (0.01-10 μM; 72 hours) inhibits the proliferative activity of human primary CD4+ T cells and the production of effector cytokines including IFNγ, IL-17A and IL-22.?GSK778 (0.001-10 μM; 5 days) has a more pronounced effect on the growth and viability of MDA-453, MOLM-13, K562, MV4-11, THP-1, and MDA-MB-231 cells.?GSK778 (1000 nM; 72 hours) inhibits proliferation, induces a cell cycle arrest and apoptosis in MV4-11, MOLM13, MDA-MB-231 and MB453 cells.?GSK778 (1000 nM; 12 days) reduces the clonogenic capacity of primary human AML cells.
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备