NSC 617145是一种靶向Werner综合征解旋酶（WRN）的抑制剂，IC50值为230nM。
Cas No.:203115-63-3
Sample solution is provided at 25 µL, 10mM.
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NSC 617145 is targeted inhibitor of werner syndrome helicase (WRN) helicase, with an IC50 value of 230nM [1]. NSC 617145 can induce synthetic lethality via a genetic-based and/or chemically induced mechanism and render human cells deficient in the Fanconi Anemia (FA) pathway hypersensitive to the DNA cross-linking agent mitomycin C (MMC) in a WRN-dependent manner[2]. NSC 617145 has been widely used as an anti-cancer agent and has been applied in various cancer cell models to induce DNA damage[3].
In vitro, NSC 617145 treatment for 48 hours significantly inhibited the proliferation of PC3 cells, K562 cells, and HeLa cells, with IC50 values of 184.6 ± 36.3, 20.3 ± 11.5, and 237.0 ± 120.2nM, respectively[4]. Treatment with 250nM NSC 617145 for 4 days significantly reduced the number of LMY1 cells and induced cell apoptosis[5]. NSC 617145 treatment for 48 hours exhibited significant cytotoxicity in normal human liver LX2 cells and normal human renal epithelial HK2 cells, with the IC50 values of 1.81 ± 0.27μM and 5.64 ± 0.96μM, respectively[6].
References:
[1] Aggarwal M, Banerjee T, Sommers J A, et al. Werner syndrome helicase has a critical role in DNA damage responses in the absence of a functional fanconi anemia pathway[J]. Cancer research, 2013, 73(17): 5497-5507.
[2] Datta A, Brosh Jr R M. New insights into DNA helicases as druggable targets for cancer therapy[J]. Frontiers in molecular biosciences, 2018, 5: 59.
[3] Aggarwal M, Banerjee T, Sommers J A, et al. Targeting an Achilles’ heel of cancer with a WRN helicase inhibitor[J]. Cell cycle, 2013, 12(20): 3329-3335.
[4] Li H, Yu J, Yu G, et al. Design and synthesis of N-aryl-2-trifluoromethyl-quinazoline-4-amine derivatives as potential Werner-dependent antiproliferative agents[J]. Molecular Diversity, 2025, 29(1): 195-214.
[5] Moles R, Bai X T, Chaib-Mezrag H, et al. WRN-targeted therapy using inhibitors NSC 19630 and NSC 617145 induce apoptosis in HTLV-1-transformed adult T-cell leukemia cells[J]. Journal of hematology & oncology, 2016, 9(1): 121.
[6] Yu J, Yu G, Cheng S, et al. Quinazoline Derivative kzl052 Suppresses Prostate Cancer by Targeting WRN Helicase to Stabilize DNA Replication Forks[J]. International Journal of Molecular Sciences, 2025, 26(13): 6093.
NSC 617145是一种靶向Werner综合征解旋酶（WRN）的抑制剂，IC50值为230nM[1]。NSC 617145可通过基于遗传和/或化学诱导的机制诱发合成致死效应，并以WRN依赖性方式使范可尼贫血（FA）通路缺陷的人体细胞对DNA交联剂丝裂霉素C（MMC）超敏[2]。NSC 617145作为抗癌剂广泛应用于多种癌细胞模型，可诱导DNA损伤[3]。
在体外，NSC 617145处理48小时可显著抑制PC3、K562和HeLa细胞增殖，IC50值分别为184.6 ± 36.3nM、20.3 ± 11.5nM和237.0 ± 120.2nM[4]。250nM的NSC 617145处理LMY1细胞4天显著减少细胞数量并诱导凋亡[5]。NSC 617145处理正常人肝LX2细胞和肾上皮HK2细胞48小时表现出显著细胞毒性，IC50值分别为1.81 ± 0.27μM和5.64 ± 0.96μM [6]。
| Cell experiment [1]: | |
Cell lines | LMY1 cells |
Preparation Method | LMY1 cells were cultured in RPMI-1640 medium supplemented with penicillin, streptomycin and 10% fetal bovine serum (FBS). The cells were treated with NSC 617145 (0.02, 0.2, 2, and 20μM) or DMSO as a control. After 96 hours, the inhibition of cell growth was measured by cell counting. |
Reaction Conditions | 0.02, 0.2, 2, and 20μM; 96h |
Applications | NSC 617145 treatment significantly inhibited the cell proliferation of LMY1 cells. |
References: | |
| Cas No. | 203115-63-3 | SDF | |
| 化学名 | 1,1'-(2,2-dimethyl-1,3-propanediyl)bis[3,4-dichloro-1H-pyrrole-2,5-dione | ||
| Canonical SMILES | CC(CN(C(C(Cl)=C1Cl)=O)C1=O)(C)CN2C(C(Cl)=C(Cl)C2=O)=O | ||
| 分子式 | C13H10Cl4N2O4 | 分子量 | 400 |
| 溶解度 | 1mg/mL in DMSO, 2mg/mL in DMF | 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 | 2.5 mL | 12.5 mL | 25 mL |
| 5 mM | 500 μL | 2.5 mL | 5 mL |
| 10 mM | 250 μL | 1.25 mL | 2.5 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
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- Purity: >98.00% Appearance: A solid
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