TC-A 2317 hydrochloride
Based on 1 Customer Validation
TC-A 2317 hydrochloride is an orally active Aurora A kinase inhibitor (Ki=1.2 nM). TC-A 2317 hydrochloride exhibits excellent selectivity to Aurora B kinase (Ki=101 nM) and other 60 kinases, good cell permeability and good PK profile. Antitumor activity.
For research use only. We do not sell to patients.
- Purity: 99.57%
- CAS No.: 1245907-03-2
- Formula: C19H29ClN6O
- Molecular Weight:392.93
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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All Aurora Kinase Isoforms
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Biological Activity
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Aurora A 1.2 nM (Ki) |
Aurora B 101 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
115 nM
Compound: 6
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Antiproliferative activity against human HCT116 cells
Antiproliferative activity against human HCT116 cells
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[PMID: 20573509] |
TC-A 2317 hydrochloride (Compound 6) inhibits proliferation of HCT116 cells with an IC50 of 115 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
TC-A 2317 hydrochloride shows good PK profile; Cmax value is 4930 nM (Tmax=1.2 h) and serum concentration after 24 h is 52 nM (T1/2=3.3 h) at 30 mg/kg po in rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:HCT-116 Xenograft mice mode[1]
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Dosage:P.o.; daily for 14 days
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Administration:30 mg/kg
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Result:Growth of tumor was inhibited by 59% after 14 days.
Chemical Information
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CAS No. 1245907-03-2
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Appearance Solid
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Molecular Weight 392.93
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Formula C19H29ClN6O
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Color White to off-white
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SMILES
N#CC1=C(C)C=C(NC2=NNC(C)=C2)N=C1NC(C)CCCC(C)(O)C.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 100 mg/mL (254.50 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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 (6.36 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 (6.36 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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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 (271 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 (sealed storage, away from moisture). 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 | 2.5450 mL | 12.7249 mL | 25.4498 mL | 63.6246 mL |
| 5 mM | 0.5090 mL | 2.5450 mL | 5.0900 mL | 12.7249 mL | |
| 10 mM | 0.2545 mL | 1.2725 mL | 2.5450 mL | 6.3625 mL | |
| 15 mM | 0.1697 mL | 0.8483 mL | 1.6967 mL | 4.2416 mL | |
| 20 mM | 0.1272 mL | 0.6362 mL | 1.2725 mL | 3.1812 mL | |
| 25 mM | 0.1018 mL | 0.5090 mL | 1.0180 mL | 2.5450 mL | |
| 30 mM | 0.0848 mL | 0.4242 mL | 0.8483 mL | 2.1208 mL | |
| 40 mM | 0.0636 mL | 0.3181 mL | 0.6362 mL | 1.5906 mL | |
| 50 mM | 0.0509 mL | 0.2545 mL | 0.5090 mL | 1.2725 mL | |
| 60 mM | 0.0424 mL | 0.2121 mL | 0.4242 mL | 1.0604 mL | |
| 80 mM | 0.0318 mL | 0.1591 mL | 0.3181 mL | 0.7953 mL | |
| 100 mM | 0.0254 mL | 0.1272 mL | 0.2545 mL | 0.6362 mL |
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