2. PI3K/Akt/mTOR Apoptosis
  3. PI3K Apoptosis
  4. HS-173

HS-173 是一种新颖的 PI3K 抑制剂，常用于癌症研究。

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HS-173 Chemical Structure

HS-173 Chemical Structure

CAS No. : 1276110-06-5

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规格 价格 是否有货 数量
1 mg ￥300
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5 mg ￥680
In-stock
10 mg ￥1100
In-stock
25 mg ￥2200
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50 mg ￥3450
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100 mg ￥5188
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500 mg   询价  

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Customer Review

HS-173 相关抗体

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查看 PI3K 亚型特异性产品:

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

HS-173 is a novel PI3K inhibitor, that is used for cancer treatment.

IC50 & Target[4]

PI3Kα

0.8 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
0.26 μM
Compound: HS-173
Antiproliferative activity against human A549 cells after 72 hrs by SRB assay
Antiproliferative activity against human A549 cells after 72 hrs by SRB assay
[PMID: 28800461]
HCT-116 IC50
0.25 μM
Compound: HS-173
Cytotoxicity against human HCT116 cells harboring PIK3CA mutant assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
Cytotoxicity against human HCT116 cells harboring PIK3CA mutant assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
[PMID: 32069401]
HCT-116 IC50
0.54 μM
Compound: HS-173
Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay
Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay
[PMID: 28800461]
MCF7 IC50
7.8 μM
Compound: 19c
Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay
Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay
[PMID: 21388141]
MDA-MB-231 IC50
0.76 μM
Compound: HS-173
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay
[PMID: 28800461]
SK-BR-3 IC50
1.5 μM
Compound: 19c
Cytotoxicity against human SK-BR-3 cells after 48 hrs by MTT assay
Cytotoxicity against human SK-BR-3 cells after 48 hrs by MTT assay
[PMID: 21388141]
SK-HEP1 IC50
1.09 μM
Compound: HS-173
Antiproliferative activity against human SKHEP1 cells after 72 hrs by SRB assay
Antiproliferative activity against human SKHEP1 cells after 72 hrs by SRB assay
[PMID: 28800461]
SNU-638 IC50
0.68 μM
Compound: HS-173
Antiproliferative activity against human SNU638 cells after 72 hrs by SRB assay
Antiproliferative activity against human SNU638 cells after 72 hrs by SRB assay
[PMID: 28800461]
T47D IC50
0.6 μM
Compound: 19c
Cytotoxicity against human T47D cells after 48 hrs by MTT assay
Cytotoxicity against human T47D cells after 48 hrs by MTT assay
[PMID: 21388141]
体外研究
(In Vitro)

HS-173 (0.1-10 μM) 以剂量和时间依赖性方式降低细胞活力。HS-173 通过剂量依赖性地抑制胰腺癌细胞中的集落形成显示出显著的药物反应。HS-173 抑制胰腺癌细胞中 TGF-β 诱导的细胞迁移和侵袭。HS-173 抑制 TGF-β 诱导的上皮间质转化 (EMT)[1]。HS-173 处理以剂量和时间依赖性方式降低两种肝星状细胞系的细胞活力。HS-173 在 G2/M 期诱导细胞周期停滞。HS-173 处理增加了裂解的 caspase-3 的表达并降低了 HSC-T6 细胞中 Bcl-2 的表达。HS-173 抑制 HSCs 中促纤维化介质和 ECM 降解调节剂的表达[2]。索拉非尼和 HS-173 的组合协同抑制胰腺癌细胞系中的细胞增殖。Sorafenib (HY-10201) 和 HS-173 的组合抑制 RAF/MAPK 和 PI3K/AKT 信号通路中的关键酶[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

HS-173 相关抗体:
体内研究
(In Vivo)

HS-173 (10 mg/kg，腹腔注射) 显著增加 TUNEL 的表达，裂解 caspase-3，同时降低肿瘤组织中 PCNA 的表达。HS-173 处理可降低肿瘤组织中的 p-AKT 和 p-Smad2。HS-173 (10 和 30 mg/kg) 显著降低肺和肝的转移负担[1]。HS-173 (10 和 20 mg/kg) 抑制 CCl4 诱导的肝纤维化动物模型小鼠的 ECM 积累和 PI3K/Akt 信号传导。在 CCl4 诱导的肝纤维化小鼠中，HS-173 明显抑制 p-Akt 和 p-P70S6K 的表达，同时降低胶原蛋白 I 和波形蛋白的表达[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

422.46

Formula

C21H18N4O4S
CAS 号
性状

固体

颜色

White to gray

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 50 mg/mL (118.35 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 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
查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验：

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (5.92 mM); 悬浊液; 超声助溶

    此方案可获得 2.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (5.92 mM); 悬浊液; 超声助溶

    此方案可获得 2.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

    2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.04%

COA (286 KB) LCMS (120 KB)

产品使用指南 (1538 KB)
参考文献
Cell Assay
[1]

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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

HS-173 相关分类

完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3671 mL 11.8354 mL 23.6709 mL 59.1772 mL
5 mM 0.4734 mL 2.3671 mL 4.7342 mL 11.8354 mL
10 mM 0.2367 mL 1.1835 mL 2.3671 mL 5.9177 mL
15 mM 0.1578 mL 0.7890 mL 1.5781 mL 3.9451 mL
20 mM 0.1184 mL 0.5918 mL 1.1835 mL 2.9589 mL
25 mM 0.0947 mL 0.4734 mL 0.9468 mL 2.3671 mL
30 mM 0.0789 mL 0.3945 mL 0.7890 mL 1.9726 mL
40 mM 0.0592 mL 0.2959 mL 0.5918 mL 1.4794 mL
50 mM 0.0473 mL 0.2367 mL 0.4734 mL 1.1835 mL
60 mM 0.0395 mL 0.1973 mL 0.3945 mL 0.9863 mL
80 mM 0.0296 mL 0.1479 mL 0.2959 mL 0.7397 mL
100 mM 0.0237 mL 0.1184 mL 0.2367 mL 0.5918 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

HS-1731276110-06-5HS173HS 173PI3KApoptosisPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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