CC214-2
Based on 1 Customer Validation
CC214-2 is an oral active and selective mTOR kinase inhibitor. CC214-2 targets to both of mTORC1 (pS6) and mTORC2 (pAktS473). CC214-2 induces autophagy, which is a potential target for host-directed therapy (HDT) in tuberculosis. CC214-2 exhibits synergistic bactericidal and sterilizing activity agasinst tuberculosis (TB), and shortens the treatment duration. CC214-2 also inhibits Rapamycin (HY-10219)-resistant signaling and the growth of glioblastomas in vitro and in vivo.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.41%
- CAS 番号: 1228012-18-7
- 分子式: C20H25N5O3
- 分子量:383.44
-
保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
生物活性
|
mTORC1 |
mTORC2 |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| PC-3 | IC50 |
0.315 μM
Compound: 10b, CC214-2
|
Inhibition of mTORC2 in human PC3 cells assessed as inhibition of AKTS473 phosphorylation after 1 hr by sandwich immunoassay
Inhibition of mTORC2 in human PC3 cells assessed as inhibition of AKTS473 phosphorylation after 1 hr by sandwich immunoassay
|
[PMID: 23414803] |
| PC-3 | IC50 |
0.32 μM
Compound: 26, CC214-2
|
Inhibition of mTORC2 in human PC3 cells assessed as inhibition of Akt phosphorylation at S473 after 1 hr
Inhibition of mTORC2 in human PC3 cells assessed as inhibition of Akt phosphorylation at S473 after 1 hr
|
[PMID: 26083478] |
| PC-3 | IC50 |
0.386 μM
Compound: 10b, CC214-2
|
Inhibition of mTORC1 in human PC3 cells assessed as inhibition of S6 phosphorylation after 1 hr by sandwich immunoassay
Inhibition of mTORC1 in human PC3 cells assessed as inhibition of S6 phosphorylation after 1 hr by sandwich immunoassay
|
[PMID: 23414803] |
| PC-3 | IC50 |
0.39 μM
Compound: 26, CC214-2
|
Inhibition of mTORC1 in human PC3 cells assessed as inhibition of S6 phosphorylation after 1 hr
Inhibition of mTORC1 in human PC3 cells assessed as inhibition of S6 phosphorylation after 1 hr
|
[PMID: 26083478] |
| PC-3 | IC50 |
1.55 μM
Compound: 10b, CC214-2
|
Cytotoxicity against human PC3 cells assessed as growth inhibition after 3 days by WST1 assay
Cytotoxicity against human PC3 cells assessed as growth inhibition after 3 days by WST1 assay
|
[PMID: 23414803] |
CC214-2 (30 mg/kg, 100 mg/kg; po; single dose) inhibits both mTORC1 (pS6) and mTORC2 (pAktS473) in vivo for at least 8 and 24 h, respectively[1].
CC214-2 (30 mg/kg; po) reduces M. tuberculosis CFU numbers and prevents mortality in mice with Chronic M. tuberculosis infection[1].
CC214-2 (50 mg/kg; po; once daily for 6 days) significantly reduces the growth of mouse U87EGFRvIII flank xenografts[2].
CC214-2 (100 mg/kg; po; once every 2 days for 6 days) inhibits mTORC1 and mTORC2 signaling in an intracranial glioblastoma model[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:U87EGFRvIII flank xenografts in mice[2]
-
Dosage:50 mg/kg
-
Administration:PO; once daily for 6 days
-
Result:Inhibited tumor growth.
Similarly activated autophagy in U87EGFRvIII xenografts.
化学情報
-
CAS 番号 1228012-18-7
-
性状 Solid
-
分子量 383.44
-
分子式 C20H25N5O3
-
Color Light yellow to light brown
-
SMILES
O=C1N=C2NC=C(C3=CC=C(C(C)(C)O)N=C3)N=C2N(CC4CCOCC4)C1
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 62.5 mg/mL (163.00 mM; ultrasonic and warming and heat to 70°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
-
データシート (273 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
取扱説明書 (2659 KB)
参考文献
[1]. Gini B, et al. The mTOR kinase inhibitors, CC214-1 and CC214-2, preferentially block the growth of EGFRvIII-activated glioblastomas. Clin Cancer Res. 2013 Oct 15;19(20):5722-32. [Content Brief]
[2]. Tasneen R, et al. Dual mTORC1/mTORC2 Inhibition as a Host-Directed Therapeutic Target in Pathologically Distinct Mouse Models of Tuberculosis. Antimicrob Agents Chemother. 2021;65(7):e0025321. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6080 mL | 13.0398 mL | 26.0797 mL | 65.1992 mL |
| 5 mM | 0.5216 mL | 2.6080 mL | 5.2159 mL | 13.0398 mL | |
| 10 mM | 0.2608 mL | 1.3040 mL | 2.6080 mL | 6.5199 mL | |
| 15 mM | 0.1739 mL | 0.8693 mL | 1.7386 mL | 4.3466 mL | |
| 20 mM | 0.1304 mL | 0.6520 mL | 1.3040 mL | 3.2600 mL | |
| 25 mM | 0.1043 mL | 0.5216 mL | 1.0432 mL | 2.6080 mL | |
| 30 mM | 0.0869 mL | 0.4347 mL | 0.8693 mL | 2.1733 mL | |
| 40 mM | 0.0652 mL | 0.3260 mL | 0.6520 mL | 1.6300 mL | |
| 50 mM | 0.0522 mL | 0.2608 mL | 0.5216 mL | 1.3040 mL | |
| 60 mM | 0.0435 mL | 0.2173 mL | 0.4347 mL | 1.0867 mL | |
| 80 mM | 0.0326 mL | 0.1630 mL | 0.3260 mL | 0.8150 mL | |
| 100 mM | 0.0261 mL | 0.1304 mL | 0.2608 mL | 0.6520 mL |