CC214-1
Based on 1 Customer Validation
CC214-1 is a potentially efficacious mTOR inhibitor that induces autophagy ,with an IC50 is 0.002 μM. CC214-1 proved to be useful as an in vitro tool compound for the exploration of mTOR kinase biology. CC214-1 can be used for Glioblastoma study.
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- Purity: 98.49%
- CAS No.: 1021920-32-0
- 화학식: C20H21N7O2
- 분자량:391.43
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보관:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
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mTOR 0.002 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| PC-3 | IC50 |
0.018 μM
Compound: 9a, CC214-1
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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
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[PMID: 23414803] |
| PC-3 | IC50 |
0.04 μM
Compound: 9a, CC214-1
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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
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[PMID: 23414803] |
| PC-3 | IC50 |
0.224 μM
Compound: 9a, CC214-1
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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
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[PMID: 23414803] |
CC214-1 (0, 0.1, 1, 2, 5, 10 μM, 8 h; 2 μM, 24 h) synergize with rapamycin (HY-10219), inhibiting mTORC1 signaling and tumor cell proliferation[1].
CC214-1 (2 μM, 24 h) -mediated sensitivity to growth arrest in glioblastoma cells due to EGFRvIII expression and loss of PTEN[1].
CC214-1 (5 μM, 0-48 h) massively lipidates LC3B-I to LC3B-II subtype and induces autophagy in GBM39 cells[1].
CC214-1 has an IC50 of mTOR is 0.002 μM[2].
CC214-1 (0-10 μM, 4days) is efficient in inhibiting T cell activation and the expression of T-cell activation markers[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:glioblastoma
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Concentration:0, 0.1, 1, 2, 5, 10 μM; 2 μM
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Incubation Time:8 h; 24 h
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Result:Inhibited mTORC1 signaling in all glioblastoma cell lines tested, potently suppressing rapamycin-resistant 4E-BP1 and mTORC2 signaling.
Inhibited mTORC1-dependent 4E-BP1 and S6 phosphorylation in EGFRvIII-expressing glioblastoma cells, as well as blocked glioblastoma cells overexpressing wild-type EGFR.
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Cell Line:glioblastoma
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Concentration:2 μM, 5 μM
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Incubation Time:4 h; 0, 4, 12, 24, 48 h
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Result:Induced a transient expression of LC3B-II isoform and the conjugation of Atg12 to Atg5 indicative of the stimulation of the autophagy flux in U87EGFRvIII cell line.
Massively lipidated LC3B-I to LC3B-II subtype and induces autophagy in GBM39 cells.
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Cell Line:glioblastoma
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Concentration:0-10 μM
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Incubation Time:4 day
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Result:Induced TEE cells in CD4+ and CD8+ T cell subsets.
Chemical Information
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CAS No. 1021920-32-0
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Appearance Solid
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분자량 391.43
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화학식 C20H21N7O2
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Color Off-white to gray
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SMILES
O=C1NC2=NC=C(C3=CC=C(C4=NN=CN4)C=C3)N=C2N1CCC5CCOCC5
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 20 mg/mL (51.09 mM; ultrasonic and warming and heat to 60°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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2 mg/mL (5.11 mM); Clear solution
This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2 mg/mL (5.11 mM); Clear solution
This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (278 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[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]. Mortensen DS, et al. Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase. Bioorg Med Chem Lett. 2013 Mar 15;23(6):1588-91. [Content Brief]
[3]. Herrero-Sánchez MC, et al. Effect of mTORC1/mTORC2 inhibition on T cell function: potential role in graft-versus-host disease control. Br J Haematol. 2016 Jun;173(5):754-68. [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 | 2.5547 mL | 12.7737 mL | 25.5474 mL | 63.8684 mL |
| 5 mM | 0.5109 mL | 2.5547 mL | 5.1095 mL | 12.7737 mL | |
| 10 mM | 0.2555 mL | 1.2774 mL | 2.5547 mL | 6.3868 mL | |
| 15 mM | 0.1703 mL | 0.8516 mL | 1.7032 mL | 4.2579 mL | |
| 20 mM | 0.1277 mL | 0.6387 mL | 1.2774 mL | 3.1934 mL | |
| 25 mM | 0.1022 mL | 0.5109 mL | 1.0219 mL | 2.5547 mL | |
| 30 mM | 0.0852 mL | 0.4258 mL | 0.8516 mL | 2.1289 mL | |
| 40 mM | 0.0639 mL | 0.3193 mL | 0.6387 mL | 1.5967 mL | |
| 50 mM | 0.0511 mL | 0.2555 mL | 0.5109 mL | 1.2774 mL |
CC214-1 Related Classifications
HY-154910 Related Classifications
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