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- 2025年12月22日
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- 详细信息
- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
CC-223
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
1228013-30-6
- 规格：
25mg/10mg/5mg/1mg/2mg
| 规格： | 25mg | 产品价格： | ￥2940.0 |
|---|---|---|---|
| 规格： | 10mg | 产品价格： | ￥1590.0 |
| 规格： | 5mg | 产品价格： | ￥970.0 |
| 规格： | 1mg | 产品价格： | ￥413.0 |
| 规格： | 2mg | 产品价格： | ￥580.0 |
| 基本信息 | |
| CAS | No.1228013-30-6 |
| 英文名称 | CC-223 |
| 别名 | CC-223;ATG-008 |
| 分子式 | C21H27N5O3 |
| 分子量 | 397.47 |
| 溶解性 | Soluble in DMSO ≥3mg/mL |
| 纯度 | ≥98% |
| 外观(性状) | Light yellow to yellow Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL | MFCD28976054 |
| SMILES | CC(C)(C1=NC=C(C=C1)C2=CN=C3C(=N2)N(C(=O)CN3)C4CCC(CC4)OC)O |
| InChIKey | UFKLYTOEMRFKAD-UHFFFAOYSA-N |
| InChI | InChI=1S/C21H27N5O3/c1-21(2，28)17-9-4-13(10-22-17)16-11-23-19-20(25-16)26(18(27)12-24-19)14-5-7-15(29-3)8-6-14/h4，9-11，14-15，28H，5-8，12H2，1-3H3，(H，23，24) |
| PubChem CID | 58298316 |
| 靶点 | mTOR |
| 通路 | PI3K/Akt/mTOR |
| 背景说明 | CC-223 是一种有效的 mTOR 激酶抑制剂，抑制 mTORC1 和 mTORC2。 |
| 生物活性 | 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 is a potent， selective， and orally bioavailable inhibitor of mTOR kinase， demonstrating inhibition of mTORC1 (pS6RP and p4EBP1) and mTORC2 [pAKT(S473)] in cellular systems. Onatasertib is selective for mTOR kinase with >200-fold selectivity over the related PI3K-α (IC50=4.0 μM). Of the PI3K related kinases tested， Onatasertib shows no significant inhibition of ATR or SMG1 and inhibits DNA-PK with an IC50 value of 0.84 μM. When screened in a single-point assay against a commercially available panel of 246 kinases， only three kinases other than mTOR are inhibited >80% at 10 μM by Onatasertib. Upon follow-up IC50 value determination， only two are inhibited by Onatasertib with IC50 values below 1 μM; FLT4 (0.651 μM) and cFMS (0.028 μM). The exquisite kinase selectivity of Onatasertib is confirmed upon evaluation in cellular systems using ActivX KiNavtiv profiling. Other than mTOR kinase， no kinase target is identified when HCT 116 or A549 cells are treated for 1 hour with 1 μM Onatasertib and assayed for kinase activity. Onatasertib shows a concentration-dependent reduction in each marker， with IC50 values of 31±2 nM for pS6RP， 405±47 nM for p4EBP1， and 11±10 nM for pAKT(S473) in western blot analysis. Inhibition of these pathway biomarkers is investigated in additional cell types from a variety of tissue origins. Onatasertib inhibits both mTORC1 (S6RP and 4EBP1) and mTORC2 [AKT(S473)] markers across the panel with IC50 ranges of 27 to 184 nM for pS6RP， 120 to 1，050 nM for p4EBP1 and 11 to 150 nM for pAKT(S473) [1]. |
| 细胞实验 | The antitumor activity of Onatasertib in the PC-3 xenograft model is determined using a number of dosing paradigms. Onatasertib significantly inhibits PC-3 tumor growth in a dose- and schedule-dependent manner. Dosing at 10 or 25 mg/kg， once daily， results in 46% (P[1]. |
| 细胞实验 | For other cell panel proliferation assays， CC-223 (1 nM， 100 nM and 1 μM) is spotted via an acoustic dispenser (EDC ATS-100) into an empty 384-well plate. Cells are diluted to desired densities and added directly to the compound-spotted plates. Cells are allowed to grow for 72 hours. Viability is assessed via Cell Titer-Glo. All data are normalized and represented as a percentage of the DMSO-treated cells. Results are then expressed as GI50 and/or IC50 values[1]. |
| 动物实验 | Mice[1] Female 6- to 8-weeks-old CB17 SCID mice are inoculated s.c. with 2×106 PC-3 cells. When tumors reach approximately 125 mm3， mice are randomized and treated once daily， twice daily， or every 2 days orally with vehicle or various doses of CC-223， at a dose volume of 5 mL/kg. The twice-daily doses are administered with a 10 hours separation between the morning and evening doses. Tumor volumes are determined before the initiation of treatment and are considered as the starting volumes. Tumors are measured twice a week for the duration of the study. The long and short axes of each tumor are measured using a digital caliper in millimeters. The tumor volumes are calculated. The tumor volumes are expressed in cubic millimeters (mm3). |
| 激酶实验 | Counter screen against 246 protein kinases is outsourced and completed at a fixed CC-223 concentration (10 μM). Follow-up IC50 value determinations for ephrin type-B receptor 3 kinase (EPHB3)， colony stimulating factor 1 receptor tyrosine kinase (CSF1R or cFMS)， and FMS-related tyrosine kinase 4 (FLT4) are outsourced to Invitrogen[1]. |
| 数据来源文献 | [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. |
| 单位 | 瓶 |
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IC2480 CC-223 抑制剂/拮抗剂/激动剂 索莱宝
￥413 - 2940
