C3TD879
Based on 1 Customer Validation
C3TD879 is a Type I kinase inhibitor that potently inhibits CITK catalytic activity (IC50 = 12 nM). C3TD879 binds directly to full-length human CITK in cells (NanoBRET Kd < 10 nM). C3TD879 is a chemical probe suitable for interrogating the complex biology of CITK.
For research use only. We do not sell to patients.
- Purity: 98.41%
- CAS No.: 2850259-33-3
- Formula: C22H28N4O
- Molecular Weight:364.48
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Storage:Powder -20°C, 3 years , 4°C, 2 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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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
IC50: 12 nM (Citron kinase, CITK)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 786-0 | GI50 |
<2 μM
Compound: 58; C3TD879
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Antiproliferative activity against human 786-0 Panel cells assessed as cell viability incubated for 48 hrs by CellTiter-Glo cell viability assay
Antiproliferative activity against human 786-0 Panel cells assessed as cell viability incubated for 48 hrs by CellTiter-Glo cell viability assay
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[PMID: 38330278] |
| COLO 205 | GI50 |
<2 μM
Compound: 58; C3TD879
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Antiproliferative activity against human COLO 205 Panel cells assessed as cell viability incubated for 48 hrs by CellTiter-Glo cell viability assay
Antiproliferative activity against human COLO 205 Panel cells assessed as cell viability incubated for 48 hrs by CellTiter-Glo cell viability assay
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[PMID: 38330278] |
| Hs-578T | GI50 |
<2 μM
Compound: 58; C3TD879
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Antiproliferative activity against human Hs-578T cells assessed as cell viability incubated for 48 hrs by CellTiter-Glo cell viability assay
Antiproliferative activity against human Hs-578T cells assessed as cell viability incubated for 48 hrs by CellTiter-Glo cell viability assay
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[PMID: 38330278] |
| Panel NCI-60 (60 carcinoma cell lines) | GI50 |
7 μM
Compound: 58; C3TD879
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Antiproliferative activity against human Panel NCI-60 (60 carcinoma cell lines) assessed as cell viability incubated for 48 hrs by CellTiter-Glo cell viability assay
Antiproliferative activity against human Panel NCI-60 (60 carcinoma cell lines) assessed as cell viability incubated for 48 hrs by CellTiter-Glo cell viability assay
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[PMID: 38330278] |
C3TD879 demonstrates a promising profile in vitro, with low microsomal intrinsic clearance, modest PPB fraction unbound, high permeability, and low inhibition of key CYP enzymes[1].
C3TD879 (100 μM) can bind to and stabilize recombinant CITKKD purified from E. coli or insect cells[1].
C3TD879 (0.1 nM-100 μM) binds directly to NL-CITKKD (Kd = 0.3 nM) and full length NL-CITK (Kd = 9.5 nM) in intact HEK293 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2850259-33-3
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Appearance Solid
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Molecular Weight 364.48
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Formula C22H28N4O
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Color White to off-white
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SMILES
CC1=CC(NC([C@H](N)CC(C)(C)C)=O)=CC=C1C2=C3C(NC(C)=C3)=NC=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (274.36 mM; Need ultrasonic; 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: ≥ 2.5 mg/mL (6.86 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (6.86 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Purity & Documentation
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Data Sheet (274 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
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 | 2.7436 mL | 13.7182 mL | 27.4363 mL | 68.5909 mL |
| 5 mM | 0.5487 mL | 2.7436 mL | 5.4873 mL | 13.7182 mL | |
| 10 mM | 0.2744 mL | 1.3718 mL | 2.7436 mL | 6.8591 mL | |
| 15 mM | 0.1829 mL | 0.9145 mL | 1.8291 mL | 4.5727 mL | |
| 20 mM | 0.1372 mL | 0.6859 mL | 1.3718 mL | 3.4295 mL | |
| 25 mM | 0.1097 mL | 0.5487 mL | 1.0975 mL | 2.7436 mL | |
| 30 mM | 0.0915 mL | 0.4573 mL | 0.9145 mL | 2.2864 mL | |
| 40 mM | 0.0686 mL | 0.3430 mL | 0.6859 mL | 1.7148 mL | |
| 50 mM | 0.0549 mL | 0.2744 mL | 0.5487 mL | 1.3718 mL | |
| 60 mM | 0.0457 mL | 0.2286 mL | 0.4573 mL | 1.1432 mL | |
| 80 mM | 0.0343 mL | 0.1715 mL | 0.3430 mL | 0.8574 mL | |
| 100 mM | 0.0274 mL | 0.1372 mL | 0.2744 mL | 0.6859 mL |
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