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ML-265
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
ML-265图片
CAS NO:1221186-53-3
包装与价格：
包装价格(元)
5mg电议
10mg电议
25mg电议

产品介绍

化学性质

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
Canonical SMILESCS(C1=CC(N2C)=C(S1)C3=C2C(N(CC4=CC(N)=CC=C4)N=C3)=O)=O
运输条件蓝冰运输或根据您的需求运输。
一般建议为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

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].