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AT13148 是一种 ATP 竞争性 AGC 激酶口服抑制剂,能够抑制 Akt1/Akt2/Akt3、p70S6K、PKA 和 ROCKI/ROCKII 的活性,IC50值分别为 38/402/50、8、3 和 6 nM/4 nM。


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AT13148 是一种 ATP 竞争性 AGC 激酶口服抑制剂,能够抑制 Akt1/Akt2/Akt3、p70S6K、PKA 和 ROCKI/ROCKII 的活性,IC50值分别为 38/402/50、8、3 和 6 nM/4 nM。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 392 | In stock | |
| 5 mg | ¥ 967 | In stock | |
| 10 mg | ¥ 1,420 | In stock | |
| 25 mg | ¥ 2,380 | In stock | |
| 50 mg | ¥ 3,570 | In stock | |
| 100 mg | ¥ 5,670 | In stock | |
| 1 mL x 10 mM (in DMSO) | ¥ 987 | In stock |
AT13148 相关产品
| 产品描述 | AT13148 is an oral-active and ATP-competitive, multi-AGC kinase inhibitor for Akt1/2/3, p70S6K, PKA, and ROCKI/II. |
| 靶点活性 | ROCK2:4 nM, Chk2:860 nM, Aurora B:1840 nM, RSK1:85 nM, Akt2:402 nM, PKA:3 nM, Akt3:50 nM, SGK3:63 nM, ROCK1:6 nM, Akt1:38 nM, p70 S6K:8 nM |
| 体外活性 | 在人肿瘤异种移植物模型中,口服AT13148(50 mg/kg)能够抑制AKT 和p70S6K AGC激酶,表现出抗肿瘤活性. |
| 体内活性 | 在PTEN缺陷型MES-SA细胞中,AT13148能够抑制AKT 和 p70S6K信号。对于PI3K-AKT-mTOR 或 RAS-RAF通路反常的癌细胞系(GI50=1.5-3.8 μM),AT13148能够抑制多重AGC激酶,从而抑制癌细胞增殖。 |
| 激酶实验 | In vitro kinase assays: AT13148 is assayed against 40 kinases and the percentage inhibition at 10 μM of AT13148 is determined. Individual IC50 values are measured for selected kinases using ATP concentrations equivalent to the Km for each enzyme. |
| 细胞实验 | Cytotoxicity is determined using a 72 h Alamar Blue assay or a 96 h SRB assay. (Only for Reference) |
| 分子量 | 313.78 |
| 分子式 | C17H16ClN3O |
| CAS No. | 1056901-62-2 |
| Smiles | NC[C@@](O)(c1ccc(Cl)cc1)c1ccc(cc1)-c1cn[nH]c1 |
| 密度 | 1.328 g/cm3 (Predicted) |
| 颜色 | White |
| 物理性状 | Solid |
| 存储 | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| 溶解度信息 | H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: < 1 mg/mL (insoluble or slightly soluble) DMSO: 58 mg/mL (184.84 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| 体内实验配方 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.37 mM), Sonication is recommended. 请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。 | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
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