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NSC139021  (Synonyms: ERGi-USU)

目录号: HY-112158 纯度: 99.86%
COA 产品使用指南

NSC139021 (ERGi-USU) 是ERG阳性癌细胞生长的高度选择性抑制剂,抑制不同细胞系的 IC50 值为 30 到400 nM。

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NSC139021 Chemical Structure

NSC139021 Chemical Structure

CAS No. : 1147-56-4

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规格 价格 是否有货 数量
Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ¥550
In-stock
100 mg ¥500
In-stock
200 mg   询价  
500 mg   询价  

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Customer Review

MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

NSC139021 (ERGi-USU) is a highly selective inhibitor for the growth of ERG-positive cancer cells with IC50s ranging from 30 to 400 nM.

IC50 & Target

IC50: 30 to 400 nM (ERG-positive cancer cells)[1]

体外研究
(In Vitro)

NSC139021 selectively inhibits growth of ERGpositive cancer cell lines with minimal effect on normal prostate or endothelial cells or ERG-negative tumor cell lines. The IC50 of NSC139021 for cell growth inhibition of responsive cell lines range between 30 nM to 400 nM. Combination of NSC139021 with enzalutamide shows additive effects in inhibiting growth of VCaP cells. A screen of kinases reveal that NSC139021 directly bound the ribosomal biogenesis regulator atypical kinase RIOK2 and induces ribosomal stress signature[1].

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

体内研究
(In Vivo)

NSC139021 treatment inhibits growth of ERG-positive VCaP tumor xenografts with no apparent toxicity. Significant (P<0.05, P<0.005) inhibition of tumor growth is noted at day 26 in treatment groups indicating 44% (100 mg/kg) and 65% (150 mg/kg) reduction of tumor burden. At 100 mg/kg and 150 mg/kg, no apparent toxicity including weight loss, lethargy, diarrhea, loss of appetite, respiratory distress, or overall drug related toxicity is observed. [1].

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

分子量

255.30

Formula

C13H9N3OS

CAS 号
性状

固体

颜色

Pink to red

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
In Vitro: 

DMSO 中的溶解度 : ≥ 62 mg/mL (242.85 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.9170 mL 19.5848 mL 39.1696 mL
5 mM 0.7834 mL 3.9170 mL 7.8339 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

In Vivo:

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: 15% Cremophor EL    85% Saline

    Solubility: 15.53 mg/mL (60.83 mM); 悬浊液; 超声助溶

  • 方案 二

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

    Solubility: ≥ 2.5 mg/mL (9.79 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    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。
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

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: 99.86%

参考文献
Cell Assay
[1]

To assess cell growth, To evaluate the ERG selectivity of the NSC139021, a panel of the following cell lines are assessed: ERG positive tumor cell lines (prostate cancer: VCaP; colon cancer: COLO320; leukemia: KG-1, MOLT-4; ERG negative prostate cancer cell lines (LNCaP, LAPC4, MDA PCa2b); normal prostate epithelium derived cell lines (BPH-1, RWPE-1); and primary endothelium derived cells (HUVEC). Monolayer of adherent cells are grown in their respective medium for 48 h followed by treatment with indicated dosage and time for the small molecule inhibitor NSC139021. Medium is replaced every 24 h containing the same concentration of the small molecule compound. Cells are counted by using trypan blue exclusion method. Cell morphology is documented by photography in all indicated time points. IC50 is calculated using GraphPad Prism 6 software[1].

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

Animal Administration
[1]

Mice[1]

The VCaP prostate cancer cells are injected into lower right dorsal flank of the male athymic nude mice (6-8 weeks old and weighing 27 to 30g). when tumors are palpable, mice are randomly separated into 2 experimental groups and into one control group of 6 mice in each group. In the treatment groups mice are injected intraperitoneally (I.P) with 100 mg/kg of NSC139021 or 150 mg/kg of NSC139021 while the control group are injected with vehicle (1:1[v/v], DMSO/PEG300) only. Growth in tumor volume is recorded weekly by using digital calipers and tumor volumes are calculated[1].

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

参考文献

NSC139021 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 3.9170 mL 19.5848 mL 39.1696 mL 97.9240 mL
5 mM 0.7834 mL 3.9170 mL 7.8339 mL 19.5848 mL
10 mM 0.3917 mL 1.9585 mL 3.9170 mL 9.7924 mL
15 mM 0.2611 mL 1.3057 mL 2.6113 mL 6.5283 mL
20 mM 0.1958 mL 0.9792 mL 1.9585 mL 4.8962 mL
25 mM 0.1567 mL 0.7834 mL 1.5668 mL 3.9170 mL
30 mM 0.1306 mL 0.6528 mL 1.3057 mL 3.2641 mL
40 mM 0.0979 mL 0.4896 mL 0.9792 mL 2.4481 mL
50 mM 0.0783 mL 0.3917 mL 0.7834 mL 1.9585 mL
60 mM 0.0653 mL 0.3264 mL 0.6528 mL 1.6321 mL
80 mM 0.0490 mL 0.2448 mL 0.4896 mL 1.2241 mL
100 mM 0.0392 mL 0.1958 mL 0.3917 mL 0.9792 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.

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产品名称:
NSC139021
目录号:
HY-112158
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