STM2457
- CAS No.
- 2499663-01-1
- Chemical Name:
- STM2457
- Synonyms
- STM2457;STM2457 ，S9870;STM2457, 10 mM in DMSO;leukaemia,Apoptosis,cancer,STM-2457,autoimmune diseases,STM2457,inhibit,STM 2457,myeloid,Inhibitor;N-((6-(((Cyclohexylmethyl)amino)methyl)imidazo[1,2-a]pyridin-2-yl)methyl)-4-oxo-4H-pyrido[1,2-a]pyrimidine-2-carboxamide;4H-Pyrido[1,2-a]pyrimidine-2-carboxamide, N-[[6-[[(cyclohexylmethyl)amino]methyl]imidazo[1,2-a]pyridin-2-yl]methyl]-4-oxo-;4-Oxo-4H-pyrido[1,2-a]pyrimidine-2-carboxylic acid {6-[(cyclohexylmethyl-amino)-methyl]-imidazo[1,2-a]pyridin-2-ylmethyl}-amide;N - (6- (((cyclohexylmethyl) amino) methyl) imidazolo [1,2-a] pyridin-2-yl) methyl) -4-oxo-4H-pyridino [1,2-a] pyrimidin-2-formamide
- CBNumber:
- CB28670993
- Molecular Formula:
- C25H28N6O2
- Molecular Weight:
- 444.53
- MDL Number:
- MFCD34368521
- MOL File:
- 2499663-01-1.mol
| Density | 1.35±0.1 g/cm3(Predicted) |
|---|---|
| storage temp. | Store at -20°C |
| solubility | DMSO : 270 mg/mL |
| form | A solid |
| pka | 13.74±0.20(Predicted) |
| color | White to yellow |
| InChIKey | OBERVORNENYOLE-UHFFFAOYSA-N |
| SMILES | C12C=CC=CN1C(=O)C=C(C(NCC1=CN3C(=N1)C=CC(CNCC1CCCCC1)=C3)=O)N=2 |
| UNSPSC Code | 12352200 |
| NACRES | NA.21 |
STM2457 price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | SML3360 | STM2457 ≥98% (HPLC) | 2499663-01-1 | 5MG | $84.45 | 2025-07-31 | Buy |
| Sigma-Aldrich | SML3360 | STM2457 ≥98% (HPLC) | 2499663-01-1 | 25MG | $273.6 | 2025-07-31 | Buy |
| DC Chemicals | 028229 | STM2457 | 2499663-01-1 | 002 | $280 | 2021-12-16 | Buy |
| DC Chemicals | 028229 | STM2457 | 2499663-01-1 | 003 | $400 | 2021-12-16 | Buy |
STM2457 Chemical Properties,Uses,Production
Uses
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].
Definition
ChEBI: STM2457 is a secondary carboxamide resulting from the formal condensation of the carboxy group of 4-oxo-4H-pyrido[1,2-a]pyrimidine-2-carboxylic acid with the primary amino group of 1-[2-(aminomethyl)imidazo[1,2-a]pyridin-6-yl]-N-(cyclohexylmethyl)methanamine. It is a highly potent and selective first-in-class small molecule inhibitor of METTL3 (N6-adenosine-methyltransferase 70 kDa subunit) enzyme activity and exhibits anti-leukaemic activity. It has a role as an EC 2.1.1.348 (mRNA m6A methyltransferase) inhibitor, an antineoplastic agent and an apoptosis inducer. It is an imidazopyridine, a secondary carboxamide, a secondary amino compound and a pyridopyrimidine.
Biological Activity
STM2457 is a potent and highly selective SAM-binding site METTL3 (MT-A70) m6A methyltransferase inhibitor (IC50 = 16.9 nM, Kd = 1.4 nM by SPR, using METTL3-METTL14 complex; no potency toward other RNA/DNA/protein methyltransferases or 486 kinases). STM2457 selectively inhibits human AML proliferation (IC50 = 0.6-10.3 μM) and the clonogenic potential of primary mouse AML, but not normal mouse haematopoietic stem/progenitor or human cord blood CD34+ cells. STM2457 impairs the expansion of AML patient-derived xenografts in mice in vivo (50 mg/kg i.p.) and significantly prolongs the animalμs lifespan. STM2457 is also reported to restrict β-coronavirus replication and spread.
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. DOI:10.1038/s41586-021-03536-w
STM2457 Preparation Products And Raw materials
Raw materials
Preparation Products
STM2457 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 33024 | 60 |
| BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19552 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354; +17819995354 | marketing@targetmol.com | United States | 32376 | 58 |
| Henan Alfa Chemical Co., Ltd | +8615838112936 | alfa10@alfachem.cn | China | 13006 | 58 |
| Nextpeptide Inc | +86-0571-81612335 +8613336028439 | sales@nextpeptide.com | China | 19908 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
| Nantong HI-FUTURE Biology Co., Ltd. | +undefined18051384581 | sales@chemhifuture.com | China | 3135 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354; | support@targetmol.com | United States | 38838 | 58 |
| LEAPCHEM CO., LTD. | +86-852-30606658 | market18@leapchem.com | China | 43340 | 58 |
| Aladdin Scientific | tp@aladdinsci.com | United States | 57505 | 58 |
| Supplier | Advantage |
|---|---|
| ATK CHEMICAL COMPANY LIMITED | 60 |
| BOC Sciences | 58 |
| TargetMol Chemicals Inc. | 58 |
| Henan Alfa Chemical Co., Ltd | 58 |
| Nextpeptide Inc | 58 |
| InvivoChem | 58 |
| Nantong HI-FUTURE Biology Co., Ltd. | 58 |
| TargetMol Chemicals Inc. | 58 |
| LEAPCHEM CO., LTD. | 58 |
| Aladdin Scientific | 58 |
