HS-173
目录号 : GC16713
A PI3K inhibitor
Cas No.:1276110-06-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: | Cell viability is performed using an MTT assay. In brief, cells are seeded at a density of 5000-7000 cells/well in a 96-well plates following to 24 h incubation. On the following day the media are removed and the cells are treated with either vehicle as a negative control or various concentrations of HS-173 (0.5-10 μM) following an incubation for 24, 48, or 72 h. After incubation of respective time 10% of an MTT solution (2 mg/mL) is added to each well and the cells are incubated for another 4 h at 37°C. The formazan crystals that formed are dissolved in DMSO (100 or 300 μL/well) with constant shaking for 5 min. The absorbance of the plate is then read with a microplate reader at 540 nm. Three replicate wells are evaluated for each analysis. |
Animal experiment: | Male BALB/c mice (4 week old, weighing 18-20 g) are fed with standard rat chow and tap water ad libitum, and are maintained with a 12 h dark/light cycle at 21°C. After one week of adaptation period, Panc-1 cells (5×106 cells/mice) are inoculated in the right flank of the mouse. After reaching an average tumor volume of 50 mm3, mice are randomly divided into two groups with five mice in each group; the control group is treated with vehicle and the experimental group is treated with HS-173 (10 mg/kg) intraperitoneally thrice a week for 26 days. The body weight and tumor size are measured thrice a week. At the end of the experiment, mice are sacrificed and primary tumor is harvested. Tumors are weighed, photographed, and divided into two parts for Western blot and IHC analysis. For IHC analysis, tissues are immediately fixed in 4% PFA for overnight and for Western blotting analysis, tissues are snap-frozen in liquid nitrogen. |
References: [1]. Rumman M, et al. HS-173, a novel PI3K inhibitor suppresses EMT and metastasis in pancreatic cancer. Oncotarget. 2016 Oct 25 | |
Phosphatidylinositol 3-kinase (PI3K) was first identified over 20 years ago as a lipid kinase associated with viral oncoproteins. PI3K signaling pathway regulates various cellular processes such as growth, cell cycle progression, apoptosis, migration, metabolism, and cytoskeleton rearrangement. HS-173 is a novel PI3K inhibitor.
In vitro: HS-173 inhibited the PI3K signaling pathway, and showed anti-proliferative effects on cancer cells. Also, HS-173 induced cell cycle arrest at the G2/M phase and apoptosis. In addition, HS-173 decreased the expression HIF-1a and VEGF which play an important role in angiogenesis. This effect was confirmed by the suppression of tube formation and migration assay in vitro [1].
In vivo: HS-173 diminished blood vessel formation in the Matrigel plug assay in mice. These results suggest that HS-173 has potent anti-angiogenic activity in vivo [1].
Clinical trials: Currenlty no clinical data are available.
Reference:
[1] Lee H, Jung KH, Jeong Y, Hong S, Hong SS. HS-173, a novel phosphatidylinositol 3-kinase (PI3K) inhibitor, has anti-tumor activity through promoting apoptosis and inhibiting angiogenesis. Cancer Lett. 2013 Jan 1;328(1):152-9.
| Cas No. | 1276110-06-5 | SDF | |
| Canonical SMILES | O=S(NC1=CN=CC(C(C=C2)=CN3C2=NC=C3C(OCC)=O)=C1)(C4=CC=CC=C4)=O | ||
| 分子式 | C21H18N4O4S | 分子量 | 422.46 |
| 溶解度 | ≥ 21.1mg/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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3671 mL | 11.8354 mL | 23.6709 mL |
| 5 mM | 0.4734 mL | 2.3671 mL | 4.7342 mL |
| 10 mM | 0.2367 mL | 1.1835 mL | 2.3671 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。