TAS0612
Based on 1 Customer Validation
TAS0612 is the orally active inhibitor of RSK、AKT and S6K. TAS0612 has antitumor activity.
For research use only. We do not sell to patients.
- Purity: 98.83%
- CAS No.: 2148902-58-1
- Formula: C27H34F3N9O2
- Molecular Weight:573.61
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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
Biological Activity
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p70S6K |
TAS0612 (0.25-5.0 μM, 48 h) inhibits the growth of B-cell-like diffuse large B-cell lymphoma (DLBCL) cell with IC50s of 0.41-6.73 μM[2].
TAS0612 (0.25-5.0 μM, 48 h) arrests the cell cycle of KPUM-UH1 at G1 phase, arrests Daudi, HBL1 and FL18 at G2/M phase, induces apoptosis in cells KPUM-UH1, Daudi, HBL1 and FL18[2].
TAS0612 (0.25-5.0 μM, 24 h) promotes the expression of tumor suppressor protein TP53INP1 in cells KPUM-UH1, Daudi and FL18[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Daudi, Raji, HBL1, DLBCL2, FL518, FL18, KPUM-UH1, KPUM-MS3
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Concentration:0.25-5.0 μM
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Incubation Time:48 h
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Result:Inhibited the cell growth.
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Cell Line:KPUM-UH1, Daudi, HBL1 and FL18
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Concentration:0.25-5.0 μM
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Incubation Time:48 h
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Result:Induced apoptosis.
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Cell Line:KPUM-UH1, Daudi, HBL1 and FL18
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Concentration:0.25-5.0 μM
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Incubation Time:6-24 h
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Result:Upregulated the expression of TP53INP1.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mouse OPM-2 xenograft models[3]
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Dosage:30-90 mg/kg
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Administration:po, once daily for 2 weeks
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Result:Inhibited the tumor growth.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2148902-58-1
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Appearance Solid
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Molecular Weight 573.61
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Formula C27H34F3N9O2
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Color White to off-white
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SMILES
O=C1NC2=NC=NC(N3CCC(CC3)C4=NC(C5=NN=C(C(F)(F)F)O5)=CC=C4NCCNC(C)(C)C)=C2C1(C)C
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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 : 50 mg/mL (87.17 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: ≥ 2.5 mg/mL (4.36 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.
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 (279 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]. Koji Ichikawa, et al. TAS0612, a novel RSK, AKT, and S6K inhibitor, exhibits antitumor effects in preclinical tumor models. Mol Cancer Ther. 2023. [Content Brief]
[2]. Katsuragawa-Taminishi Y, et al., Triple targeting of RSK, AKT, and S6K as pivotal downstream effectors of PDPK1 by TAS0612 in B-cell lymphomas. Cancer Sci. 2023 Dec;114(12):4691-4705. [Content Brief]
[3]. Okamoto H, et al., Robust anti-myeloma effect of TAS0612, an RSK/AKT/S6K inhibitor, with venetoclax regardless of cytogenetic abnormalities. Leukemia. 2025 Jan;39(1):211-221. [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 |
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| DMSO | 1 mM | 1.7433 mL | 8.7167 mL | 17.4334 mL | 43.5836 mL |
| 5 mM | 0.3487 mL | 1.7433 mL | 3.4867 mL | 8.7167 mL | |
| 10 mM | 0.1743 mL | 0.8717 mL | 1.7433 mL | 4.3584 mL | |
| 15 mM | 0.1162 mL | 0.5811 mL | 1.1622 mL | 2.9056 mL | |
| 20 mM | 0.0872 mL | 0.4358 mL | 0.8717 mL | 2.1792 mL | |
| 25 mM | 0.0697 mL | 0.3487 mL | 0.6973 mL | 1.7433 mL | |
| 30 mM | 0.0581 mL | 0.2906 mL | 0.5811 mL | 1.4528 mL | |
| 40 mM | 0.0436 mL | 0.2179 mL | 0.4358 mL | 1.0896 mL | |
| 50 mM | 0.0349 mL | 0.1743 mL | 0.3487 mL | 0.8717 mL | |
| 60 mM | 0.0291 mL | 0.1453 mL | 0.2906 mL | 0.7264 mL | |
| 80 mM | 0.0218 mL | 0.1090 mL | 0.2179 mL | 0.5448 mL |
TAS0612 Related Classifications
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