| ML-265tumor-specific PKM2 activator |
Sample solution is provided at 25 µL, 10mM.
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- Purity = 96.30%
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| Cas No. | 1221186-53-3 | SDF | Download SDF |
| Synonyms | CID-44246499,NCGC00186528,TEPP-46 | ||
| Chemical Name | 6-[(3-aminophenyl)methyl]-4,6-dihydro-4-methyl-2-(methylsulfinyl)-5H-thieno[2’,3’:4,5]pyrrolo[2,3-d]pyridazin-5-one | ||
| Canonical SMILES | CS(C1=CC(N2C)=C(S1)C3=C2C(N(CC4=CC(N)=CC=C4)N=C3)=O)=O | ||
| Formula | C17H16N4O2S2 | M.Wt | 372.5 |
| Solubility | ≥37.3mg/mL in DMSO | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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].
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然后往容器中滴液体直至读数为0.70时就可以了
我们每天长时间都在实验室里和移液器（俗称“枪”）打交道，枪已经成为实验室标配，因为它是很多实验过程和分析的基础。但正因为如此，我们都认为它很简单，就像走路和呼吸一样自然，不需要你花任何心思，它就可以做你想做的事情。但事实真的是这样吗？
事实上，枪虽小但往往关系到实验结果的准确性，有小伙伴经常抱怨枪老出问题：
1.用了一段时间就不准漏液了？
2.液体容易倒吸？
3.移液排不干净？……
到底是哪里出问题了呢，你有没有碰到这样的迷之困惑？
当当当，福利到，来自梅特勒-托利多瑞宁移液技术专家自告奋勇来解答大伙儿的困惑，有任何关于移液器使用的问题欢迎来和我们探讨共同进步哟~
最后感谢丁香园支持本活动！
我们会每天抽时间统一回复大家的问题，专家答疑截止12月31日哦！
塑料类工具灭菌有什么需要注意的吗？谢谢！
2、吸液：用右手的拇指和中指捏住移液管的上端，将管的下口插入欲吸取的溶液中，插入
不要太浅或太深，一般为10～20mm处，太浅会产生吸空，把溶液吸到洗耳球内弄脏溶液，
太深又会在管外沾附溶液过多。左手拿洗耳球，接在管的上口把溶液慢慢吸入，先吸入该管 容量的1/3
左右，用右手的食指按住管口，取出，横持，并转动管子使溶液接触到刻度以上 部位，以置换内壁的水分，然后将溶液从管的下口放出并弃去，如此用反复洗3
次后，即可 吸取溶液至刻度以上，立即用右手的食指按住管口。 3、调节液面：将移液管向上提升离开液面，管的末端仍靠在盛溶液器皿的内壁上，管身保
持直立，略为放松食指（有时可微微转动吸管）使管内溶液慢慢从下口流出，直至溶液的弯
月面底部与标线相切为止，立即用食指压紧管口。将尖端的液滴靠壁去掉，移出移液管，插 入承接溶液的器皿中。
4、放出溶液：承接溶液的器皿如是锥形瓶，应使锥形瓶倾斜30°，移液管直立，管下端紧
靠锥形瓶内壁，稍松开食指，让溶液沿瓶壁慢慢流下，流完后管尖端接触瓶内壁约15 秒后，
再将移液管移去，残留在管末端的少量溶液，不可用外力强使其流出，因较准时已考虑了末 端保留的溶液的体积。
大家做溶出曲线稀释溶液时有某有再用移液枪？移液枪量取1ml的体积准确不？
