| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C27H34F3N9O2 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
TAS0612 is an orally active inhibitor of RSK, AKT and S6K. It exhibits antitumor activity[1]. It is supplied as a white to off-white solid (C27H34F3N9O2, MW 573.61) at 98.83% purity.
Physical & Chemical Properties
| CAS Number | 2148902-58-1 |
|---|---|
| Molecular Formula | C27H34F3N9O2 |
| Molecular Weight | 573.61 g/mol |
| Purity | 98.83% |
| Appearance | Solid |
| Color | White to off-white |
| 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 |
| Target | p70S6K |
| Signaling Pathway | PI3K/Akt/mTOR; MAPK/ERK Pathway; Apoptosis |
| Solubility | In Vitro: DMSO: 50 mg/mL (87.17 mM; Requires sonication and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 50 mg/mL (87.17 mM) | requires sonication and warming and heat to 60°C; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.5 mg/mL (4.36 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.5 mg/mL (4.36 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
TAS0612 (0.25-5.0 μM, 48 h) suppresses growth of B-cell-like diffuse large B-cell lymphoma (DLBCL) cells, with IC50s of 0.41-6.73 μM[2]. TAS0612 (0.25-5.0 μM, 48 h) arrests KPUM-UH1 cells at G1 phase, arrests Daudi, HBL1 and FL18 cells at G2/M phase, and induces apoptosis in KPUM-UH1, Daudi, HBL1 and FL18 cells[2]. TAS0612 (0.25-5.0 μM, 24 h) increases expression of the tumor suppressor protein TP53INP1 in KPUM-UH1, Daudi and FL18 cells[2].
Cell Viability Assay[2]
| Cell Line | Daudi, Raji, HBL1, DLBCL2, FL518, FL18, KPUM-UH1, KPUM-MS3 |
|---|---|
| Concentration | 0.25-5.0 μM |
| Incubation Time | 48 h |
| Result | Inhibited the cell growth. |
Apoptosis Analysis[2]
| Cell Line | KPUM-UH1, Daudi, HBL1 and FL18 |
|---|---|
| Concentration | 0.25-5.0 μM |
| Incubation Time | 48 h |
| Result | Induced apoptosis. |
Real Time qPCR[2]
| Cell Line | KPUM-UH1, Daudi, HBL1 and FL18 |
|---|---|
| Concentration | 0.25-5.0 μM |
| Incubation Time | 6-24 h |
| Result | Upregulated the expression of TP53INP1. |
In Vivo
In mouse OPM-2 xenograft models, TAS0612 (30-90 mg/kg, po, once daily for 2 weeks) displays antitumor efficacy[3].
| Animal Model | Mouse OPM-2 xenograft models[3] |
|---|---|
| Dosage | 30-90 mg/kg |
| Administration | po, once daily for 2 weeks |
| Result | Inhibited the tumor growth. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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