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SL327

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Chemical Structure| 305350-87-2 同义名 : -
CAS号 : 305350-87-2
货号 : A139600
分子式 : C16H12F3N3S
纯度 : 98+%
分子量 : 335.347
MDL号 : MFCD06411432
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 70 mg/mL(208.74 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：

2% DMSO+30% PEG 300+5% Tween 80+water 5 mg/mL

生物活性
靶点

  • MEK2

    MEK2, IC50:0.22 μM

  • MEK1

    MEK1, IC50:0.18 μM
描述 Mitogen-activated protein kinases/extracellular signal-regulated kinase (MAPK/ERK) pathway, also known as MEK pathway, is reported to be associated with the cell proliferation, differentiation, migration, senescence and apoptosis[3]. SL327 inhibits MEK1 and MEK2, with IC50 values of 0.18 μM and 0.22 μM, respectively[4]. In vivo, the study showed that the combination of SL327 with sunitinib malate induced significant additive suppression of doxorubicin-resistant anaplastic thyroid carcinoma (ATC) tumor growth[4]. SL327 attenuates phosphorylated MAPK levels in a dose-dependent manner in mice. Administration of 10, 30, or 50 mg/kg SL327 significantly attenuates p42 phospho-MAPK levels (F=20.90, P<0.0001; 10 mg/kg SL327 vs. vehicle, P<0.05, and 30 and 50 mg/kg SL327 vs. vehicle, P<0.001). Injection with 30 or 50 mg/kg SL327 also significantly reduces p44 phospho-MAPK levels (F=5.627, P<0.005; 30 mg/kg vs. vehicle, P<0.05, and 50 mg/kg SL327 vs. vehicle, P<0.01)[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.98mL

0.60mL

0.30mL

14.91mL

2.98mL

1.49mL

29.82mL

5.96mL

2.98mL
参考文献

[1]Scherle PA, Ma W, et al. Regulation of cyclooxygenase-2 induction in the mouse uterus during decidualization. An event of early pregnancy. J Biol Chem. 2000 Nov 24;275(47):37086-92.

[2]Atkins CM, Selcher JC, et al. The MAPK cascade is required for mammalian associative learning. Nat Neurosci. 1998 Nov;1(7):602-9.

[3]Sun Y, Liu WZ, Liu T, Feng X, Yang N, Zhou HF. Signaling pathway of MAPK/ERK in cell proliferation, differentiation, migration, senescence and apoptosis. J Recept Signal Transduct Res. 2015;35(6):600-4. doi: 10.3109/10799893.2015.1030412. Epub 2015 Jun 22. PMID: 26096166.

[4]Cheng Y, Tian H. Current Development Status of MEK Inhibitors. Molecules. 2017 Sep 26;22(10):1551. doi: 10.3390/molecules22101551. PMID: 28954413; PMCID: PMC6151813.

[5]Selcher JC, Atkins CM, Trzaskos JM, Paylor R, Sweatt JD. A necessity for MAP kinase activation in mammalian spatial learning. Learn Mem. 1999 Sep-Oct;6(5):478-90. doi: 10.1101/lm.6.5.478. PMID: 10541468; PMCID: PMC311312.