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
- MSDS File:
- SDS
- TDS File:
- TDS
| 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 | $95.3 | 2026-04-30 | Buy |
| Sigma-Aldrich | SML3360 | STM2457 ≥98% (HPLC) | 2499663-01-1 | 25MG | $309 | 2026-04-30 | Buy |
| Cayman Chemical | 34280 | STM2457 ≥98% | 2499663-01-1 | 5mg | $91 | 2026-04-30 | Buy |
| Cayman Chemical | 34280 | STM2457 ≥98% | 2499663-01-1 | 10mg | $171 | 2026-04-30 | Buy |
| Cayman Chemical | 34280 | STM2457 ≥98% | 2499663-01-1 | 25mg | $379 | 2026-04-30 | 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 | |
|---|---|---|---|---|---|
| Jinan Jiuli Biotechnology Co. , Ltd. | 15865264761 | 486064515@qq.com | China | 4999 | 58 |
| Suzhou Meidi Senuo Pharmaceutical Technology Co., Ltd. | 13771642864 | snhuyu_2008@126.com | China | 1186 | 58 |
| RD International Technology Co., Limited | 18024082417 | market@ubiochem.com | China | 9831 | 58 |
| ShangHai Caerulum Pharma Discovery Co., Ltd. | 18149758185 18149758185 | sales-cpd@caerulumpharma.com | China | 3493 | 58 |
| Hangzhou J&H Chemical Co., Ltd. | 0571-87396432 | sales@jhechem.com | China | 14905 | 59 |
| Shanghai Lollane Biological Technology Co.,Ltd. | 021-52996696，15000506266 15000506266 | China | 4860 | 55 | |
| Shanghai EFE Biological Technology Co., Ltd. | 021-65675885 18964387627 | info@efebio.com | China | 9799 | 58 |
| Shanghai YuanYe Biotechnology Co., Ltd. | 15026964105 | 2881489226@qq.com | China | 89667 | 60 |
| ShangHai Biochempartner Co.,Ltd | 177-54423994 17754423994 | 2853530910@QQ.com | China | 8000 | 62 |
| Shanghai SuperLan Chemcial Technique Centre | 0-2022843681 15618226720 | chaolaichem@foxmail.com | China | 9996 | 58 |
