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Chemical Structure| 1809427-19-7 Chemical Structure| 1809427-19-7

Structure of DT-061
CAS No.: 1809427-19-7

Chemical Structure| 1809427-19-7

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DT-061 is an oral activator of protein phosphatase 2A (PP2A). DT-061 can be used in the treatment of kras mutation and MYC-driven tumorigenesis.

Synonyms: SMAP

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Product Details of DT-061

CAS No. :1809427-19-7
Formula : C25H23F3N2O5S
M.W : 520.52
SMILES Code : 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
Synonyms :
SMAP
MDL No. :MFCD31813712

Safety of DT-061

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
H293T cells 20 or 30 μM 1 hour To directly test the effect of DT-061 on B56α trimers using the NanoBRET system, results showed an increase in B56α-specific PP2A trimerization upon DT-061 treatment Cell. 2020 Apr 30;181(3):688-701.e16.
H358 cells 30 μM 1-2 hours To monitor the effect of DT-061 on PP2A heterotrimer formation, results showed a significant 3-6 fold increase in luciferase fragment complementation within 1-2 hours after DT-061 treatment Cell. 2020 Apr 30;181(3):688-701.e16.
H441 cells 10 μM 24 hours To assess the apoptosis-inducing effect of DT-061 on H441 cells Sci Transl Med. 2018 Jul 18;10(450):eaaq1093.
H358 cells 10 μM 24 hours To assess the apoptosis-inducing effect of DT-061 on H358 cells Sci Transl Med. 2018 Jul 18;10(450):eaaq1093.
Bax/Bak double-knockout MEC1 cells 12, 16, 20 μM 12 hours To validate that DT-061 can induce apoptosis even in the absence of Bax/Bak, results showed that DT-061 induced apoptosis via the mPTP pathway. J Clin Invest. 2023 Jul 3;133(13):e155938.
Chronic lymphocytic leukemia cells 12, 16, 20 μM 18 hours To evaluate the apoptosis-inducing effect of DT-061 on CLL cells, results showed that DT-061 induced apoptosis via mitochondrial permeability transition pores (mPTP) independent of the Bax/Bak pathway. J Clin Invest. 2023 Jul 3;133(13):e155938.
HeLa 20 µM 2 h To detect the effect of DT-061 on PP2A-B56 complexes, no binding or activity changes were observed EMBO J. 2022 Jul 18;41(14):e110611.
HEK-293T 20 µM 30 min To detect the effect of DT-061 on PP2A-B56 complexes, no binding or activity changes were observed EMBO J. 2022 Jul 18;41(14):e110611.
Human aortic smooth muscle cells (SMCs) 5 μM 24 hours To evaluate the effect of DT-061 on PDGF-induced proliferation of SMCs. Results showed that DT-061 significantly inhibited PDGF-induced proliferation of SMCs. Transplantation. 2024 Mar 1;108(3):e36-e48.
Chronic lymphocytic leukemia cells 15 μM 24 hours To evaluate the effect of DT-061 on CLL cell survival and apoptosis, results showed that DT-061 reduced the percentage of viable CLL cells in a dose-dependent manner and increased the proportion of apoptotic cells. Cell Death Dis. 2022 Sep 1;13(9):755.
FLT3-ITD AML primary cells 10 μM 48 hours Enhanced FLT3 inhibitor apoptosis induction in FLT3-ITD AML primary cells Mol Cancer Ther. 2021 Apr;20(4):676-690.
Wild-type mouse bone marrow-derived monocytes 10 µM 24 hours Enhanced cell migration Int J Mol Sci. 2025 Jan 11;26(2):572.
Ba/F3-ITD cells 10 μM 48 hours Enhanced FLT3 inhibitor growth suppression and apoptosis induction in Ba/F3-ITD cells Mol Cancer Ther. 2021 Apr;20(4):676-690.
MV4-11 cells 10 μM 48 hours Enhanced FLT3 inhibitor growth suppression and apoptosis induction in MV4-11 cells Mol Cancer Ther. 2021 Apr;20(4):676-690.
Pcdh7-deficient mouse bone marrow-derived monocytes 10 µM 24 hours Failed to restore impaired cell migration Int J Mol Sci. 2025 Jan 11;26(2):572.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice H358 lung cancer xenograft model Subcutaneous injection 5 mg/kg Twice daily for 29 days To evaluate the effect of DT-061 on B56α-PP2A heterotrimer composition, results showed a significant increase, roughly two-fold, in B56α trimers after DT-061 treatment Cell. 2020 Apr 30;181(3):688-701.e16.
Rag2−/−γC−/− mice CLL xenograft model Oral gavage 15 mg/kg Twice daily, continuous treatment To evaluate the antitumor efficacy of DT-061 in vivo, results showed that DT-061 significantly inhibited the growth of both WT and Bax/Bak-DKO CLL cells, independent of the Bax/Bak pathway. J Clin Invest. 2023 Jul 3;133(13):e155938.
Mice (C57BL/6) Mouse heterotopic heart transplantation model Oral gavage 5 mg/kg Twice daily, starting on the day of transplantation until the completion of experiments To evaluate the effect of DT-061 on heart transplant rejection in mice. Results showed that DT-061 significantly prolonged cardiac allograft survival and alleviated acute cardiac rejection. Transplantation. 2024 Mar 1;108(3):e36-e48.
Mice Eµ-TCL1 chronic lymphocytic leukemia model Oral gavage 5 mg/kg Once daily for 28 days To evaluate the effect of DT-061 on CLL cell burden in vivo, results showed that DT-061 reduced leukemic burden in peripheral blood, spleen, and bone marrow, accompanied by a decrease in N1-ICD expression. Cell Death Dis. 2022 Sep 1;13(9):755.
NSG mice MV4-11-luc xenograft model Intravenous injection 5 mg/kg Every other day starting from Day 7 post-inoculation DT-061 enhanced gilteritinib's growth suppression in MV4-11-luc xenograft model Mol Cancer Ther. 2021 Apr;20(4):676-690.
Nude mice KRAS-driven lung cancer mouse models Oral gavage 5 mg/kg Once daily for 4 weeks To evaluate the antitumor effect of the combination therapy of PP2A activator DT-061 and MEK inhibitor AZD6244 Sci Transl Med. 2018 Jul 18;10(450):eaaq1093.
Nude mice KRAS-driven lung cancer mouse models Oral gavage 5 mg/kg Once daily for 4 weeks To evaluate the antitumor effect of the combination of PP2A activator DT-061 and MEK inhibitor AZD6244 Sci Transl Med. 2018 Jul 18;10(450):eaaq1093

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.92mL

0.38mL

0.19mL

9.61mL

1.92mL

0.96mL

19.21mL

3.84mL

1.92mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
 

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