NSC139021 (ERGi-USU)
(Synonyms: 1-(2-噻唑基偶氮)-2-萘酚,ERGi-USU) 目录号 : GC34106
An ERG inhibitor
Cas No.:1147-56-4
Sample solution is provided at 25 µL, 10mM.
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ERGi-USU is an inhibitor of the oncoprotein ETS-related gene (ERG; IC50 = 315 nM).1 It inhibits proliferation of ERG-expressing VCaP prostate, COLO 320 colon, and KG-1 and MOLT-4 leukemia cancer cells (IC50s = 30-400 nM) but not LNCaP, LAPC4, and MDA PCa 2b prostate cancer and human umbilical vein endothelial cells (HUVECs), which do not express ERG (IC50s = >10 ?M for all). ERGi-USU (100 and 150 mg/kg) reduces tumor growth in a VCaP mouse xenograft model.
1.Mohamed, A.A., Xavier, C.P., Sukumar, G., et al.Identification of a small molecule that selectively inhibits ERG-positive cancer cell growthCancer Res.78(13)3659-3671(2018)
Cell experiment: | 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]. |
Animal experiment: | 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]. |
References: [1]. Mohamed AA, et al. Identification of a small molecule that selectively inhibits ERG-positive cancer cell growth. Cancer Res. 2018 Apr 30. pii: canres.2949.2017. | |
| Cas No. | 1147-56-4 | SDF | |
| 别名 | 1-(2-噻唑基偶氮)-2-萘酚,ERGi-USU | ||
| Canonical SMILES | OC1=C(/N=N/C2=NC=CS2)C3=CC=CC=C3C=C1 | ||
| 分子式 | C13H9N3OS | 分子量 | 255.3 |
| 溶解度 | DMSO : ≥ 62 mg/mL (242.85 mM) | 储存条件 | Store 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 | 3.917 mL | 19.5848 mL | 39.1696 mL |
| 5 mM | 0.7834 mL | 3.917 mL | 7.8339 mL |
| 10 mM | 0.3917 mL | 1.9585 mL | 3.917 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。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet