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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 | |
2 mg | ¥ 576 | In stock | |
5 mg | ¥ 892 | In stock | |
10 mg | ¥ 1,380 | In stock | |
25 mg | ¥ 2,480 | In stock | |
50 mg | ¥ 3,980 | 待询 | |
1 mL x 10 mM (in DMSO) | ¥ 981 | 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, p70 S6K:8 nM, Akt1:38 nM, RSK1:85 nM, SGK3:63 nM, Akt2:402 nM, ROCK1:6 nM, PKA:3 nM, Aurora B:1840 nM, Akt3:50 nM, Chk2:860 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) |
存储 | 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. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
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以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。
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