STM2457
- Product Name
- STM2457
- CAS No.
- 2499663-01-1
- Chemical Name
- STM2457
- Synonyms
- STM2457;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
- Formula Weight
- 444.53
- MOL File
- 2499663-01-1.mol
STM2457 Property
- 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
N-Bromosuccinimide Price
- Product number
- SML3360
- Product name
- STM2457
- Purity
- ≥98% (HPLC)
- Packaging
- 5MG
- Price
- $86.5
- Updated
- 2024/03/01
- Product number
- SML3360
- Product name
- STM2457
- Purity
- ≥98% (HPLC)
- Packaging
- 25MG
- Price
- $280
- Updated
- 2024/03/01
- Product number
- 028229
- Product name
- STM2457
- Packaging
- 003
- Price
- $400
- Updated
- 2021/12/16
- Product number
- 028229
- Product name
- STM2457
- Packaging
- 002
- Price
- $280
- Updated
- 2021/12/16
STM2457 Chemical Properties,Usage,Production
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.
STM2457 Preparation Products And Raw materials
Raw materials
Preparation Products
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