| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg | |||
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| Other Sizes |
| Targets |
(1S,2S,3R)-DT-061 targets protein phosphatase 2A (PP2A), a serine/threonine phosphatase that negatively regulates multiple oncogenic signaling pathways. Activation of PP2A by DT-061 and its enantiomers has therapeutic potential for KRAS-mutant and MYC-driven tumorigenesis.
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| ln Vitro |
In vitro, (1S,2S,3R)-DT-061 activates PP2A, leading to dephosphorylation of PP2A substrates and inhibition of cell proliferation in KRAS-mutant cancer cells. DT-061, the parent compound, has demonstrated anti-proliferative effects in various cancer cell lines, though specific data for the (1S,2S,3R) enantiomer are limited.
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| ln Vivo |
In vivo, DT-061 has demonstrated efficacy in preclinical models of KRAS-mutant and MYC-driven cancers. As the enantiomer of DT-061, (1S,2S,3R)-DT-061 is expected to exhibit similar or distinct pharmacological properties depending on stereospecific interactions with PP2A.
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| Enzyme Assay |
For in vitro enzyme/receptor binding assays, (1S,2S,3R)-DT-061 is evaluated using recombinant PP2A holoenzyme in phosphatase activity assays. The compound is incubated with the enzyme and a phosphopeptide substrate, and activation of PP2A is measured by the increase in phosphate release. Activity is compared to the parent compound DT-061.
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| Cell Assay |
For in vitro cellular assays, (1S,2S,3R)-DT-061 is dissolved in DMSO and applied to cancer cell lines, particularly those with KRAS mutations or MYC amplification. Cell proliferation, apoptosis, and PP2A substrate phosphorylation (e.g., p-AKT, p-MYC) are assessed using Western blotting, MTT assays, or flow cytometry.
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| Animal Protocol |
In vivo animal studies with (1S,2S,3R)-DT-061 typically involve oral administration in mouse xenograft models of KRAS-mutant or MYC-driven cancers. Tumor growth inhibition, body weight, and pharmacodynamic markers (e.g., PP2A activity, substrate phosphorylation) are monitored.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for (1S,2S,3R)-DT-061 are limited. DT-061 is orally bioavailable. The compound has a molecular weight of 520.52 and is soluble in DMSO at 125 mg/mL. For in vivo formulations, 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline is recommended.
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| Toxicity/Toxicokinetics |
Toxicology data for (1S,2S,3R)-DT-061 are limited. As a PP2A activator, the compound may have broad effects on cellular signaling. DT-061 has been studied in preclinical cancer models with acceptable tolerability. Not approved for human use.
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| References | |
| Additional Infomation |
(1S,2S,3R)-DT-061 (CAS#: 1809427-20-0) has the molecular formula C2₅H23F3N2O₅S and molecular weight 520.52. The chemical name is N-[(1S,2S)-2-hydroxy-3-(10H-phenoxazin-10-yl)cyclohexyl]-4-(trifluoromethoxy)benzene-1-sulfonamide. It is a research reagent only.
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| Molecular Formula |
C25H22F3N2O5S
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|---|---|
| Molecular Weight |
519.51279592514
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| Exact Mass |
520.127
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| CAS # |
1809427-20-0
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| Related CAS # |
DT-061;1809427-19-7
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| PubChem CID |
118374168
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| Appearance |
White to off-white solid powder
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| LogP |
5.4
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
36
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| Complexity |
824
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| Defined Atom Stereocenter Count |
3
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| SMILES |
S(C1C=CC(=CC=1)OC(F)(F)F)(N[C@H]1CCC[C]([C@@H]1O)N1C2C=CC=CC=2OC2C=CC=CC1=2)(=O)=O |^1:17|
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| InChi Key |
WGKGADVPRVLHHZ-SNYIIPAISA-N
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| InChi Code |
InChI=1S/C25H23F3N2O5S/c26-25(27,28)35-16-12-14-17(15-13-16)36(32,33)29-18-6-5-9-21(24(18)31)30-19-7-1-3-10-22(19)34-23-11-4-2-8-20(23)30/h1-4,7-8,10-15,18,21,24,29,31H,5-6,9H2/t18-,21+,24+/m0/s1
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| Chemical Name |
N-[(1S,2S,3R)-2-hydroxy-3-phenoxazin-10-ylcyclohexyl]-4-(trifluoromethoxy)benzenesulfonamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~240.14 mM)
H2O : < 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.00 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.00 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9249 mL | 9.6245 mL | 19.2489 mL | |
| 5 mM | 0.3850 mL | 1.9249 mL | 3.8498 mL | |
| 10 mM | 0.1925 mL | 0.9624 mL | 1.9249 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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