DT-061
Based on 19 publication(s) in Google Scholar
DT-061 is an orally bioavailable activator of protein phosphatase 2A (PP2A) and could be applied in the therapy of KRAS-mutant and MYC-driven tumorigenesis.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.83%
- CAS No.: 1809427-19-7
- Formule: C25H23F3N2O5S
- Masse moléculaire:520.52
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Stockage:Powder -20°C, 3 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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) DT-061
More- Transl Neurodegener. 2024 Aug 2;13(1):39. [Abstract]
- EMBO J. 2022 Jul 18;41(14):e110611. [Abstract]
- Biochem Pharmacol. 2024 Jun:224:116217. [Abstract]
- Mol Cancer Ther. 2021 Apr;20(4):676-690. [Abstract]
- Biochim Biophys Acta Mol Basis Dis. 2025 Aug 18;1871(8):168016. [Abstract]
- J Biol Chem. 2020 Mar 27;295(13):4194-4211. [Abstract]
- Biochim Biophys Acta Mol Cell Res. 2024 Oct 20;1872(1):119864. [Abstract]
- Development. 2025 Jun 18:dev.204532. [Abstract]
- PLoS One. 2022 May 26;17(5):e0268635. [Abstract]
- Oncol Lett. 2022 Mar;23(3):101. [Abstract]
- Biochem Biophys Res Commun. 2021 May 7:552:23-29. [Abstract]
- bioRxiv. 2026 Jan 25.
- bioRxiv. 2025 Nov 24:2025.11.21.689510. [Abstract]
- bioRxiv. 2025 Sep 16:2025.09.10.675396. [Abstract]
- bioRxiv. 2025 Jul 18:2025.07.14.664742. [Abstract]
- Research Square Print. 2023 Feb 13.
- Authorea. 2022.
- bioRxiv. June 17, 2021.
- Ann Transl Med. 2021 Mar;9(6):446. [Abstract]
Activité biologique
PP2A[1].
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Cell Line
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Type | Value | Description | References |
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| FL5.12 | IC50 |
15.2 μM
Compound: 5; SMAP
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Inhibition of protein phosphatase 2A in mouse FL5.12 cells assessed as reduction in cell viability incubated for 48 hrs by propidium iodide staining based flow cytometric analysis
Inhibition of protein phosphatase 2A in mouse FL5.12 cells assessed as reduction in cell viability incubated for 48 hrs by propidium iodide staining based flow cytometric analysis
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[PMID: 31383588] |
| NCI-H358 | GI50 |
5 x 103 nM
Compound: 3; DT-061
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Anticancer activity against human NCI-H358 cells
Anticancer activity against human NCI-H358 cells
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[PMID: 34156850] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:6- to 8-week-old male BALB/c nu/nu mice injected with H441 cells (5 × 106)[1].
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Dosage:5 mg/kg.
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Administration:Oral gavage for 4 weeks.
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Result:Showed activity in inhibiting tumor growth.
Chemical Information
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CAS No. 1809427-19-7
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Appearance Solid
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Masse moléculaire 520.52
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Formule C25H23F3N2O5S
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Color Off-white to light yellow
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SMILES
O=S(C1=CC=C(OC(F)(F)F)C=C1)(N[C@H]2[C@H](O)[C@@H](N3C4=C(C=CC=C4)OC5=CC=CC=C35)CCC2)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (19)
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Journal Impact Factor
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Most Recent
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Transl Neurodegener
Neuronal double-stranded DNA accumulation induced by DNase II deficiency drives tau phosphorylation and neurodegeneration. [Abstract]2024 Aug 2;13(1):39. PMID: 39095921 -
EMBO J
Chemogenetic profiling reveals PP2A-independent cytotoxicity of proposed PP2A activators iHAP1 and DT-061. [Abstract]2022 Jul 18;41(14):e110611. PMID: 35695070 -
Biochem Pharmacol
Identification of a new class of activators of the Hippo pathway with antitumor activity in vitro and in vivo. [Abstract]2024 Jun:224:116217. PMID: 38641306 -
Mol Cancer Ther
PP2A-activating Drugs Enhance FLT3 Inhibitor Efficacy through AKT Inhibition-Dependent GSK-3β-Mediated c-Myc and Pim-1 Proteasomal Degradation. [Abstract]2021 Apr;20(4):676-690. PMID: 33568357 -
Biochim Biophys Acta Mol Basis Dis
Nitroxoline upregulates low-density lipoprotein receptors expression, enhances lipid metabolism, and reduces hepatic steatosis and atherosclerosis in Apoe-/- mice. [Abstract]2025 Aug 18;1871(8):168016. PMID: 40835212 -
J Biol Chem
Phosphoproteome and drug-response effects mediated by the three protein phosphatase 2A inhibitor proteins CIP2A, SET, and PME-1. [Abstract]2020 Mar 27;295(13):4194-4211. PMID: 32071079 -
Biochim Biophys Acta Mol Cell Res
IL-17A's role in exacerbating radiation-induced lung injury: Autophagy impairment via the PP2A-mTOR pathway. [Abstract]2024 Oct 20;1872(1):119864. PMID: 39437853 -
Development
Distinct FGF-FGFR sets regulate inhibitory presynaptic differentiation from parvalbumin- and somatostatin-positive interneurons. [Abstract]2025 Jun 18:dev.204532. PMID: 40554746 -
PLoS One
Potential of phenothiazines to synergistically block calmodulin and reactivate PP2A in cancer cells. [Abstract]2022 May 26;17(5):e0268635. PMID: 35617282 -
Oncol Lett
PP2A promotes apoptosis and facilitates docetaxel sensitivity via the PP2A/p-eIF4B/XIAP signaling pathway in prostate cancer. [Abstract]2022 Mar;23(3):101. PMID: 35154432 -
Biochem Biophys Res Commun
SWATH-MS proteomics of PANC-1 and MIA PaCa-2 pancreatic cancer cells allows identification of drug targets alternative to MEK and PI3K inhibition. [Abstract]2021 May 7:552:23-29. PMID: 33740661 -
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bioRxiv
Sphingosine-1-phosphate receptor modulators resensitize FLT3-ITD acute myeloid leukemia cells with NRAS mutations to FLT3 inhibitors. [Abstract]2025 Nov 24:2025.11.21.689510. PMID: 41341164 -
bioRxiv
A Human Neuronal Co-Culture System Reveals Early Tumor-Neuron Communication and Targetable Pathways in Glioblastoma. [Abstract]2025 Sep 16:2025.09.10.675396. PMID: 41000938 -
bioRxiv
PP2A activation drives aberrant macropinocytosis and cell death in pancreatic ductal adenocarcinoma. [Abstract]2025 Jul 18:2025.07.14.664742. PMID: 40791444 -
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Ann Transl Med
Cyclin G2 promotes the formation of smooth muscle cells derived foam cells in atherosclerosis via PP2A/NF-κB/LOX-1 pathway. [Abstract]2021 Mar;9(6):446. PMID: 33850843
Solvant et solubilité
DMSO : 125 mg/mL (240.14 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: ≥ 2.08 mg/mL (4.00 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: 2.08 mg/mL (4.00 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Pureté et documentation
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Fiche technique (277 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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Instruction de manipulation (2659 KB)
Références
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 | 1.9212 mL | 9.6058 mL | 19.2116 mL | 48.0289 mL |
| 5 mM | 0.3842 mL | 1.9212 mL | 3.8423 mL | 9.6058 mL | |
| 10 mM | 0.1921 mL | 0.9606 mL | 1.9212 mL | 4.8029 mL | |
| 15 mM | 0.1281 mL | 0.6404 mL | 1.2808 mL | 3.2019 mL | |
| 20 mM | 0.0961 mL | 0.4803 mL | 0.9606 mL | 2.4014 mL | |
| 25 mM | 0.0768 mL | 0.3842 mL | 0.7685 mL | 1.9212 mL | |
| 30 mM | 0.0640 mL | 0.3202 mL | 0.6404 mL | 1.6010 mL | |
| 40 mM | 0.0480 mL | 0.2401 mL | 0.4803 mL | 1.2007 mL | |
| 50 mM | 0.0384 mL | 0.1921 mL | 0.3842 mL | 0.9606 mL | |
| 60 mM | 0.0320 mL | 0.1601 mL | 0.3202 mL | 0.8005 mL | |
| 80 mM | 0.0240 mL | 0.1201 mL | 0.2401 mL | 0.6004 mL | |
| 100 mM | 0.0192 mL | 0.0961 mL | 0.1921 mL | 0.4803 mL |
DT-061 Related Classifications
HY-112929 Related Classifications
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