产品
编 号：F763066
分子式：C25H25N3O3
分子量：415.48
分子式：C25H25N3O3
分子量：415.48
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规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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结构图
CAS No: 1313439-71-2
产品详情
生物活性：
ALM301 is an orally active highly specific AKT inhibitor with IC50 values of 0.13 μM, 0.09 μM and 2.75 μM for AKT1, AKT2 and AKT3, respectively. ALM301 inhibits AKT phosphorylation and modulates downstream signalling in vitro. ALM301 can inhibit cancer cell proliferation and tumor growth.
体内研究：
ALM301 (10, 30 and 100 mg/kg; p.o.; single dosage) inhibits pAKTS473 in tumors and suppresses tumor growth.ALM301 (3 or 10 mg/kg; p.o.; q.d. for 49 days) shows better tumor inhibition ability when combined with Tamoxifen (HY-13757A).Animal Model:BALB/c mice (bearing A549 xenografts)
Dosage:10, 30 and 100 mg/kg
Administration:p.o.; single dosage
Result:Increased total plasma concentrations dose-dependently that resulted in almost total abrogation of measurable pAKTS473 in tumors at all timepoints over 24 h.Exhibited the tumour growth inhibition (TGI) of 23, 31 and 41% at 10, 30 and 100 mg/kg, respectively.
Animal Model:BALB/c mice (bearing PIK3CA-mutant MCF-7 xenografts)
Dosage:3 or 10 mg/kg
Administration:p.o.; q.d. for 49 days
Result:Showed significant tumour regressions of 57% and 50% at 3 and 10 mg/kg, respectively, when combined with Tamoxifen (HY-13757A) (5 mg/kg; q.d.).
体外研究：
ALM301 (0.001-10 μM; 72 h) inhibits the proliferation of cancer cells, and PI3KCA-mutant MCF-7 cells is the most sensitive; increases sub-G0 population in a dose-dependent manner.ALM301 (1 μM; 1 h) inhibits AKT phosphorylation in MCF-7 and sustains up to 48 h, with an EC50 value of 0.47 μM.
ALM301 is an orally active highly specific AKT inhibitor with IC50 values of 0.13 μM, 0.09 μM and 2.75 μM for AKT1, AKT2 and AKT3, respectively. ALM301 inhibits AKT phosphorylation and modulates downstream signalling in vitro. ALM301 can inhibit cancer cell proliferation and tumor growth.
体内研究：
ALM301 (10, 30 and 100 mg/kg; p.o.; single dosage) inhibits pAKTS473 in tumors and suppresses tumor growth.ALM301 (3 or 10 mg/kg; p.o.; q.d. for 49 days) shows better tumor inhibition ability when combined with Tamoxifen (HY-13757A).Animal Model:BALB/c mice (bearing A549 xenografts)
Dosage:10, 30 and 100 mg/kg
Administration:p.o.; single dosage
Result:Increased total plasma concentrations dose-dependently that resulted in almost total abrogation of measurable pAKTS473 in tumors at all timepoints over 24 h.Exhibited the tumour growth inhibition (TGI) of 23, 31 and 41% at 10, 30 and 100 mg/kg, respectively.
Animal Model:BALB/c mice (bearing PIK3CA-mutant MCF-7 xenografts)
Dosage:3 or 10 mg/kg
Administration:p.o.; q.d. for 49 days
Result:Showed significant tumour regressions of 57% and 50% at 3 and 10 mg/kg, respectively, when combined with Tamoxifen (HY-13757A) (5 mg/kg; q.d.).
体外研究：
ALM301 (0.001-10 μM; 72 h) inhibits the proliferation of cancer cells, and PI3KCA-mutant MCF-7 cells is the most sensitive; increases sub-G0 population in a dose-dependent manner.ALM301 (1 μM; 1 h) inhibits AKT phosphorylation in MCF-7 and sustains up to 48 h, with an EC50 value of 0.47 μM.
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