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ML-265

 
Catalog No.
C4181
肿瘤特异性PKM2激活剂
组合的产品项目
规格价格库存 数量
5mg
¥ 1,054.00
现货
10mg
¥ 1,572.00
现货
25mg
¥ 2,854.00
Ship with 10-15 days

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A

背景

ML-265 (TEPP-46) is a potent and selective PKM2 activator [1][2].

Pyruvate kinase catalyzes the final step in glycolysis and transfers the phosphate group from phosphoenolpyruvate (PEP) to adenosine diphosphate (ADP) to yield adenosine triphosphate (ATP) and pyruvate. Pyruvate kinase M2 (PKM2) is considerably less active and expressed in highly proliferative cells including all cancer cell lines and tumors, which require high amounts of glucose for proliferation [1][2].

ML-265 is a potent and selective PKM2 activator with AC50 value of 92 nM. ML-265 exhibits high selectivity over PKM1, PKR and PKL. ML-265 decreased the Km of PKM2 for PEP in a way similar to the endogenous activator FBP. ML-265 also increased PKM2 activity by promoting the tetrameric state [1].

In mice with A549 xenograft tumors, ML-265 exhibited good oral bioavailability with relatively low clearance, long half-life. ML-265 (150 mg/kg) readily achieved maximal PKM2 activation. In mice bearing H1299 xenograft tumors, ML-265 inhibited tumor growth, suggesting that increased pyruvate kinase activity can impair tumorigenesis [1][2].

References:
[1].  Anastasiou D, Yu Y, Israelsen WJ, et al. Pyruvate kinase M2 activators promote tetramer formation and suppress tumorigenesis. Nat Chem Biol. 2012 Oct;8(10):839-47.
[2].  Walsh MJ, Brimacombe KR, Anastasiou D, et al. ML265: A potent PKM2 activator induces tetramerization and reduces tumor formation and size in a mouse xenograft model. Probe Reports from the NIH Molecular Libraries Program [Internet].

化学属性

StorageStore at -20°C
M.Wt372.5
Cas No.1221186-53-3
FormulaC17H16N4O2S2
SynonymsCID-44246499,NCGC00186528,TEPP-46
Solubility≥37.3 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
Chemical Name6-[(3-aminophenyl)methyl]-4,6-dihydro-4-methyl-2-(methylsulfinyl)-5H-thieno[2’,3’:4,5]pyrrolo[2,3-d]pyridazin-5-one
SDFDownload SDF
Canonical SMILESCS(C1=CC(N2C)=C(S1)C3=C2C(N(CC4=CC(N)=CC=C4)N=C3)=O)=O
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化学结构

ML-265