ALM301 是一种具有口服活性的高特异性AKT抑制剂，对 AKT1、AKT2 和 AKT3 的IC50分别 0.13 μM、0.09 μM 和 2.75 μM。ALM301 抑制 AKT 磷酸化，能在体外其调节下游信号 。ALM301可抑制癌细胞增殖和肿瘤生长。
| 生物活性 | ALM301 is an orally active highly specificAKTinhibitor withIC50values of 0.13 μM, 0.09 μM and 2.75 μM forAKT1,AKT2andAKT3, respectively. ALM301 inhibitsAKTphosphorylation and modulates downstream signallingin vitro. ALM301 can inhibitcancercell proliferation and tumor growth[1]. |
| IC50& Target[1] | AKT1 0.13 μM (IC50) | Akt2 0.09 μM (IC50) | Akt3 2.75 μM (IC50) |
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体外研究
(In Vitro) | 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[1].
ALM301 (1 μM; 1 h) inhibits AKT phosphorylation in MCF-7 and sustains up to 48 h, with an EC50value of 0.47 μM[1].
Cell Proliferation Assay[1] | Cell Line: | MCF-7, T47D, NCI-H460, HCT116 and other cancer cells | | Concentration: | 0.001-10 μM | | Incubation Time: | 72 h | | Result: | Inhibited the proliferation of cancer cells, and PI3KCA-mutant MCF-7 cells was the most sensitive with an IC50of 2.25 μM. |
Western Blot Analysis[1] | Cell Line: | MCF-7 | | Concentration: | 0.001-10 μM | | Incubation Time: | 1, 4, 24 and 48 h | | Result: | Inhibited pAKT and pGSK3β at various concentrations and timepoints up to 48 h. |
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体内研究
(In Vivo) | ALM301 (10, 30 and 100 mg/kg; p.o.; single dosage) inhibits pAKTS473in tumors and suppresses tumor growth[1].
ALM301 (3 or 10 mg/kg; p.o.; q.d. for 49 days) shows better tumor inhibition ability when combined withTamoxifen(HY-13757A)[1].
| Animal Model: | BALB/c mice (bearing A549 xenografts)[1] | | 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 pAKTS473in 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)[1] | | 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 withTamoxifen(HY-13757A) (5 mg/kg; q.d.). |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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