Art. -Nr.: HY-112929

DT-061

19 Cited Publications

Kundenbewertung

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.

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Reinheit: 99.83%
CAS. Nr.: 1809427-19-7
Formel: C₂₅H₂₃F₃N₂O₅S
Molecular Weight:520.52

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

DT-061 Chemical Structure

CAS. Nr.: 1809427-19-7

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vivo
Chemical Information
Publications (19)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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^[1].

IC₅₀ & Target

PP2A^[1].

Cellular Effect

Cell Line	Type	Value	Description	References
FL5.12	IC₅₀	15.2 μM Compound: 5; SMAP	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	[PMID: 31383588]
NCI-H358	GI₅₀	5 x 10³ nM Compound: 3; DT-061	Anticancer activity against human NCI-H358 cells Anticancer activity against human NCI-H358 cells	[PMID: 34156850]

In Vivo

DT-061 (5 mg/kg, oral gavage, 4 weeks) shows single-agent activity in inhibiting H358 or H441 xenograft growth. Additionally, the combination of DT-061 and AZD6244 is more significantly efficient^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

6- to 8-week-old male BALB/c nu/nu mice injected with H441 cells (5 × 10⁶)^[1].
Dosage:

5 mg/kg.
Administration:

Oral gavage for 4 weeks.
Result:

Showed activity in inhibiting tumor growth.

Chemical Information

CAS. Nr. 1809427-19-7
Appearance Solid
Molecular Weight 520.52
Formel C₂₅H₂₃F₃N₂O₅S
Color Off-white to light yellow
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (19)

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Journal Impact Factor

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
bioRxiv

2026 Jan 25.
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
Research Square Print

2023 Feb 13.
Authorea

2022.
bioRxiv

June 17, 2021.
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

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9212 mL

9.6058 mL

19.2116 mL

5 mM

0.3842 mL

1.9212 mL

3.8423 mL

10 mM

0.1921 mL

0.9606 mL

1.9212 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.00 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Kauko O, et al. PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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
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

Keywords

DT-061

19 Cited Publications

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DT-061

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) DT-061

Biologische Aktivität

Chemical Information

Publications (19)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

DT-061

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) DT-061

Biologische Aktivität

Chemical Information

Publications (19)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

DT-061 Related Classifications

HY-112929 Related Classifications