SH-4-54
目录号 : GC14658A STAT3 inhibitor
Cas No.:1456632-40-8
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
SH-4-54 is a potent inhibitor of STAT3 with KD values of 300 and 464 nM for STAT3 and STAT5, respectively [1].
STAT3 is a transcription factor that belongs to the STAT transcription factor family. STAT3 signaling plays an important role in the survival and proliferation of brain tumor stem cells (BTSCs) and glioblastoma (GBM) [1].
SH-4-54 is a potent STAT inhibitor. SH-4-54 inhibited interactions between STAT3 and phosphopeptide with Ki value of 10-30 μM. SH-4-54 exhibited selectivity for STAT3 against STAT1 by >10-fold. SH-4-54 inhibited pSTAT3 (Y705) in a concentration-dependent way with no effect on pSTAT3 (S727), suggesting that SH-4-54 bound to the STAT3 SH2 domain. Also, SH-4-54 reduced pSTAT3 levels and inhibited the downstream targets Cyclin D1 and Bcl-xL, which were involved in cell growth and survival [1].
In mice, intraperitoneal injection of SH-4-54 (10 mg/kg) caused a concentration of 700 nM after 30 min in the brain. In NOD-SCID mice xenografted with 105 BT73 glioma cells, SH-4-54 (10 mg/kg) reduced tumor cells and pSTAT3 expression. Also, SH-4-54 inhibited proliferation and induced apoptosis [1].
Reference:
[1]. Haftchenary S, Luchman HA, Jouk AO, et al. Potent Targeting of the STAT3 Protein in Brain Cancer Stem Cells: A Promising Route for Treating Glioblastoma. ACS Med Chem Lett, 2013, 4(11): 1102-1107.
Cas No. | 1456632-40-8 | SDF | |
Canonical SMILES | FC(C(S(=O)(N(C)CC(N(C1=CC=C(C(O)=O)C=C1)CC2=CC=C(C=C2)C3CCCCC3)=O)=O)=C(C(F)=C4F)F)=C4F | ||
分子式 | C29H27F5N2O5S | 分子量 | 610.59 |
溶解度 | ≥ 20.25mg/mL in DMSO | 储存条件 | Desiccate at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 1.6378 mL | 8.1888 mL | 16.3776 mL |
5 mM | 0.3276 mL | 1.6378 mL | 3.2755 mL |
10 mM | 0.1638 mL | 0.8189 mL | 1.6378 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。