Onatasertib

产品说明书

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Chemical Structure| 1228013-30-6 同义名 : Cc-223; ATG-008
CAS号 : 1228013-30-6
货号 : A846093
分子式 : C21H27N5O3
纯度 : 99%+
分子量 : 397.47
MDL号 : MFCD28976054
存储条件：

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(62.9 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • mTOR

    mTOR, IC50:16 nM
描述 Onatasertib (CC-223) is a potent, selective, and orally bioavailable inhibitor of mTOR kinase, with an IC50 value for mTOR kinase of 16 nM. Onatasertib inhibits both mTORC1 and mTORC2[1]. In vitro, Onatasertib has capability to inhibit markers of mTORC1 (S6RP and 4EBP1) and mTORC2 [AKT(S473)] across a range of IC50 values: 27 to 184 nM for pS6RP, 120 to 1,050 nM for p4EBP1, and 11 to 150 nM for pAKT(S473)][1].
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
human PC3 cells Function assay 1 h Inhibition of mTORC2 in human PC3 cells assessed as inhibition of Akt phosphorylation at S473 after 1 hr, IC50=0.01 μM 26083478
human PC3 cells Function assay 1 h Inhibition of mTORC1 in human PC3 cells assessed as inhibition of S6 phosphorylation after 1 hr 26083478
human PC3 cells Function assay 1 h Inhibition of mTORC1 in human PC3 cells assessed as inhibition of S6 phosphorylation after 1 hr 26083478
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.52mL

0.50mL

0.25mL

12.58mL

2.52mL

1.26mL

25.16mL

5.03mL

2.52mL
参考文献

[1]Mortensen DS, et al. CC-223, a Potent and Selective Inhibitor of mTOR Kinase: In Vitro and In Vivo Characterization. Mol Cancer Ther. 2015 Jun;14(6):1295-305.