| Identification | Back Directory | [Name]
4H-Pyrido[1,2-a]pyrimidine-2-carboxamide, N-[[6-[[(cyclohexylmethyl)amino]methyl]imidazo[1,2-a]pyridin-2-yl]methyl]-4-oxo- | [CAS]
2499663-01-1 | [Synonyms]
4H-Pyrido[1,2-a]pyrimidine-2-carboxamide, N-[[6-[[(cyclohexylmethyl)amino]methyl]imidazo[1,2-a]pyridin-2-yl]methyl]-4-oxo- | [Molecular Formula]
C25H28N6O2 | [MDL Number]
MFCD34368521 | [MOL File]
2499663-01-1.mol | [Molecular Weight]
444.53 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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 nMKd = 1.4 nM by SPRusing 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 AMLbut 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. | [storage]
Store at -20°C | [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 |
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