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ML281

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Chemical Structure| 1404437-62-2 同义名 : -
CAS号 : 1404437-62-2
货号 : A476468
分子式 : C22H19N3O2S
纯度 : 99%+
分子量 : 389.47
MDL号 : MFCD25976601
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(269.6 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 The Kirsten rat sarcoma virus (KRAS) oncogene is found in 30% of all human tumors. Downregulation of serine/threonine kinase STK33 is selectively toxic to KRAS-dependent cancer cell lines. ML281 is a potent and selective quinoxalinone-based STK33 inhibitor with an IC50 value of 14nM. It has no effect on the viability of KRAS-dependent cancer cells even at the highest concentration tested (10μM). ML281 shows 700-fold higher selectivity over PKA. It also shows high plasma protein binding in both humans (99.6%) and mice (99.9%). In addition, ML281 is identified as a highly selective inhibitor for FLT3 and KDR[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.57mL

0.51mL

0.26mL

12.84mL

2.57mL

1.28mL

25.68mL

5.14mL

2.57mL
参考文献

[1]Weïwer M, Spoonamore J, Wei J, Guichard B, Ross NT, Masson K, Silkworth W, Dandapani S, Palmer M, Scherer CA, Stern AM, Schreiber SL, Munoz B. A Potent and Selective Quinoxalinone-Based STK33 Inhibitor Does Not Show Synthetic Lethality in KRAS-Dependent Cells. ACS Med Chem Lett. 2012 Dec 13;3(12):1034-1038.