STM2457

Name: STM2457
Brand: MedChemExpress
SKU: HY-134836
Rating: 5.0 (104 reviews)

Cat. No.: HY-134836 Purity: 99.55%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

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).

For research use only. We do not sell to patients.

CAS No. : 2499663-01-1

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
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Customer Review

Based on 104 publication(s) in Google Scholar

104 Publications Citing Use of MCE STM2457

RT-PCR

: STM2457 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Jun 6;16(1):5251.; RT-qPCR data showed m6A methylation and MAPT-paRNA expression with and without STM2457 (10 μM; 24 h) treatment in induced pluripotent stem cell (iPSC)-derived human excitatory neurons (i3Neurons).

: STM2457 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Feb 14;15(1):1353. [Abstract]; STM2457 (50.0 mg/kg, once a week for 5 weeks) was administered. The protein level of testicular METTL3 was measured. n = 6 mice.

: STM2457 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Jun 26;15(1):5410. [Abstract]; Incubated RAS-induced senescent cells with antibodies targeting YTHDF3 and TIAR when treated with DMSO or METTL3 inhibitor (2.5 μM STM2457) for 48 h.

: STM2457 purchased from MedChemExpress. Usage Cited in: Nucleic Acids Res. 2024 May 9:gkae322. [Abstract]; Presenescent WI-38 cells were incubated with the METTL3/METTL14 inhibitor STM2457 (2 μM) or with vehicle alone (DMSO) for 48 h.

: STM2457 purchased from MedChemExpress. Usage Cited in: Cancer Commun (Lond). 2022 Apr;42(4):327-344. [Abstract]; The protein levels of PBX1 and GCH1 decreased in AGS cells treated with STM2457 (10 μM; 0–48 h), while METTL3 levels showed no change (upper panel).

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References
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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-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]
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]
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.

Molecular Weight

444.53

Formula

C₂₅H₂₈N₆O₂

CAS No.

2499663-01-1

Appearance

Solid

Color

White to yellow

SMILES

O=C(C(N=C1N2C=CC=C1)=CC2=O)NCC3=CN4C=C(CNCC5CCCCC5)C=CC4=N3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

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
10 mM	0.2250 mL	1.1248 mL	2.2496 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.68 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.

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
Protocol 3

Add each solvent one by one: 15% Solutol HS 15 10% Cremophor EL 35% PEG400 40% Water
Solubility: 5 mg/mL (11.25 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.57%

Select Batch:

Data Sheet (271 KB) SDS (393 KB)

COA (246 KB) HNMR (250 KB) RP-HPLC (261 KB) MS (70 KB)

Handling Instructions (2659 KB)

References

[1]. Wesley Peter Blackaby, et al. Mettl3 inhibitory compounds. WO2020201773A1.

[2]. Eliza Yankova, et al. Small molecule inhibition of METTL3 as a strategy against myeloid leukaemia. Nature. 2021 Apr 26. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.2496 mL	11.2478 mL	22.4957 mL	56.2392 mL
	5 mM	0.4499 mL	2.2496 mL	4.4991 mL	11.2478 mL
	10 mM	0.2250 mL	1.1248 mL	2.2496 mL	5.6239 mL
	15 mM	0.1500 mL	0.7499 mL	1.4997 mL	3.7493 mL
	20 mM	0.1125 mL	0.5624 mL	1.1248 mL	2.8120 mL
	25 mM	0.0900 mL	0.4499 mL	0.8998 mL	2.2496 mL
	30 mM	0.0750 mL	0.3749 mL	0.7499 mL	1.8746 mL
	40 mM	0.0562 mL	0.2812 mL	0.5624 mL	1.4060 mL
	50 mM	0.0450 mL	0.2250 mL	0.4499 mL	1.1248 mL
	60 mM	0.0375 mL	0.1875 mL	0.3749 mL	0.9373 mL
	80 mM	0.0281 mL	0.1406 mL	0.2812 mL	0.7030 mL
	100 mM	0.0225 mL	0.1125 mL	0.2250 mL	0.5624 mL

STM2457 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

STM24572499663-01-1STM 2457STM-2457ApoptosisMETTL3Methyltransferase-like 3cancermyeloidleukaemiaautoimmune diseasesInhibitorinhibitorinhibit

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STM2457

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STM2457 Related Antibodies

104 Publications Citing Use of MCE STM2457

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