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Akt1 and Akt2-IN-1 纯度: 99.59%
Akt1 and Akt2-IN-1 是一种有效的变构抑制剂, 抑制 Akt1 (IC50=3.5 nM) 和 Akt2 (IC50=42 nM)。
Akt1 and Akt2-IN-1 Chemical Structure
CAS No. : 893422-47-4
规格 | 价格 | 是否有货 | 数量 |
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10 mM * 1 mL in DMSO | ¥4155 | In-stock | |
5 mg | ¥3500 | In-stock | |
10 mg | ¥5000 | In-stock | |
50 mg | ¥15000 | In-stock | |
100 mg | ¥21000 | In-stock | |
200 mg | 询价 | ||
500 mg | 询价 |
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生物活性 |
Akt1 and Akt2-IN-1 is an allosteric inhibitor of Akt1 (IC50=3.5 nM) and Akt2 (IC50=42 nM), with potent and balanced activity. |
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IC50 & Target[1] |
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体外研究 (In Vitro) |
Consistent with the allosteric mode of inhibition, Akt1 and Akt2-IN-1 (Compound 17) is dependent on the PH-domain for Akt inhibition, is selective for Akt1/2 over Akt3 (IC50=1900 nM), and is highly selective over other members of the AGC family of kinases (>50 μM vs PKA, PKC, SGK). Akt1 and Akt2-IN-1 (Compound 17) has moderate activity in an hERG binding assay (IC50=5610 nM) and is a substrate for human P-glycoprotein[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 (In Vivo) |
Akt1 and Akt2-IN-1 (Compound 17) is well tolerated in at exposures that provide high levels of Akt1 and 2 inhibition in vivo. Akt1 and Akt2-IN-1 (Compound 17) has also been shown to inhibit the growth of A2780 tumors in vivo when used as monotherapy. Akt1 and Akt2-IN-1 (Compound 17) has potent inhibitory activity against Akt1 and 2 in vivo in a mouse lung and efficacy in a tumor xenograft model. Akt1 and Akt2-IN-1 (Compound 17) shows good pharmacokinetics in rat with a low clearance of 4.6 mL/min/kg and a half-life of 3.8 h. Due to the improved cell potency, physical properties, and rodent pharmacokinetics of Akt1 and Akt2-IN-1 (Compound 17), tolerability and Akt inhibition are assessed in mice. Using an acute dosing schedule (IP dosing of 50 mg/kg at times 0, 3, and 8 h), administration of Akt1 and Akt2-IN-1 (Compound 17) is well tolerated in mice and shows high levels of Akt inhibition in mouse lung[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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分子量 |
539.63 |
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Formula |
C33H29N7O |
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CAS 号 |
893422-47-4 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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溶解性数据 |
In Vitro:
DMSO : ≥ 35 mg/mL (64.86 mM) * “≥” means soluble, but saturation unknown. 配制储备液
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 |
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参考文献 |
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