STM2457 [2499663-01-1]

Référence HY-134836-1mg

Conditionnement : 1mg

Marque : MedChemExpress

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Description

STM2457 is a first-in-class, highly potent, selective and orally active METTL3 inhibitor with an IC50 of 16.9 nM. STM2457 can be used for the research of acute myeloid leukaemia (AML)[1][2].

Cellular Effect
Cell Line Type Value Description References
EOL1 IC50
1.94 μM
Compound: 3b; STM2457
Antiproliferative activity against human EOL1 cells assessed as inhibition of cell proliferation and measured after 7 days by CellTiter-Glo assay
Antiproliferative activity against human EOL1 cells assessed as inhibition of cell proliferation and measured after 7 days by CellTiter-Glo assay
[PMID: 36692498]
HL-60 IC50
10.3 μM
Compound: 3b; STM2457
Antiproliferative activity against human HL-60 cells assessed as inhibition of cell proliferation and measured after 7 days by CellTiter-Glo assay
Antiproliferative activity against human HL-60 cells assessed as inhibition of cell proliferation and measured after 7 days by CellTiter-Glo assay
[PMID: 36692498]
Huh-7 GI50
0.6 μM
Compound: 8; STM2457
Growth inhibition of human Huh-7 cells
Growth inhibition of human Huh-7 cells
[PMID: 38805939]
Kasumi 1 IC50
0.7 μM
Compound: 3b; STM2457
Antiproliferative activity against human Kasumi 1 cells assessed as inhibition of cell proliferation and measured after 7 days by CellTiter-Glo assay
Antiproliferative activity against human Kasumi 1 cells assessed as inhibition of cell proliferation and measured after 7 days by CellTiter-Glo assay
[PMID: 36692498]
MOLM-13 IC50
1.04 μM
Compound: 3b; STM2457
Antiproliferative activity against human MOLM-13 cells assessed as inhibition of cell proliferation and measured after 7 days by CellTiter-Glo assay
Antiproliferative activity against human MOLM-13 cells assessed as inhibition of cell proliferation and measured after 7 days by CellTiter-Glo assay
[PMID: 36692498]
NCI-H1975 IC50
65.8 μM
Compound: STM2457
Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
[PMID: 39291017]
NOMO-1 IC50
0.6 μM
Compound: 3b; STM2457
Antiproliferative activity against human NOMO-1 cells assessed as inhibition of cell proliferation and measured after 7 days by CellTiter-Glo assay
Antiproliferative activity against human NOMO-1 cells assessed as inhibition of cell proliferation and measured after 7 days by CellTiter-Glo assay
[PMID: 36692498]
OCI-AML2 IC50
1.78 μM
Compound: 3b; STM2457
Antiproliferative activity against human OCI-AML2 cells assessed as inhibition of cell proliferation and measured after 7 days by CellTiter-Glo assay
Antiproliferative activity against human OCI-AML2 cells assessed as inhibition of cell proliferation and measured after 7 days by CellTiter-Glo assay
[PMID: 36692498]
OCI-AML-3 IC50
3.2 μM
Compound: 3b; STM2457
Antiproliferative activity against human OCI-AML-3 cells assessed as inhibition of cell proliferation and measured after 7 days by CellTiter-Glo assay
Antiproliferative activity against human OCI-AML-3 cells assessed as inhibition of cell proliferation and measured after 7 days by CellTiter-Glo assay
[PMID: 36692498]
PC-9 IC50
69.15 μM
Compound: STM2457
Antiproliferative activity against human PC-9 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human PC-9 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
[PMID: 39291017]
THP-1 IC50
1.5 μM
Compound: 3b; STM2457
Antiproliferative activity against human THP-1 cells assessed as inhibition of cell proliferation and measured after 7 days by CellTiter-Glo assay
Antiproliferative activity against human THP-1 cells assessed as inhibition of cell proliferation and measured after 7 days by CellTiter-Glo assay
[PMID: 36692498]
In Vitro

STM2457 (Compound 72) inhibits MOLM13 cells proliferation with an IC50 of 8.699 μM[1].

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

Solvant et solubilité
In Vitro: 

DMSO : 100 mg/mL (224.96 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2496 mL 11.2478 mL 22.4957 mL
5 mM 0.4499 mL 2.2496 mL 4.4991 mL
View the 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.

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (4.68 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (4.68 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 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  50% PEG300    50% Saline

    Solubility: 3.33 mg/mL (7.49 mM); Clear solution; Need ultrasonic

  • Protocol 2

    Add each solvent one by one:  20% HP-β-CD in Saline

    Solubility: 5 mg/mL (11.25 mM); Clear solution; Need ultrasonic

Pureté et documentation
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