NSC59984
目录号 : GC16179
A p53 reactivator
Cas No.:803647-40-7
Sample solution is provided at 25 µL, 10mM.
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NSC59984 is a promising lead compound for anti-cancer therapy that acts by targeting GOF mutant p53 and stimulates p73 to restore the p53 signaling pathway.Thep53 is a tumour-suppressor protein which exerts antiproliferative effects, including growth arrestand apoptosis.
In vitro: In SW480 and DLD-1 cells, NSC59984 treatment for 3 hours dose-dependently increased the mRNA levels of p21, Noxa and Puma. NSC59984 was also found to increase p53-responsive reporter activity in both SW480 in a dose-dependent manner. The EC50 values of NSC59984 against a panel of cancer cell lines were different, varying from 8.38 to 110.49 µM. After incubation with 12 µM NSC59984 for 8 hours, the level ofγH2AX, a marker of genotoxicity due to DNA double-strand breaks, increased in HCT116 cells. NSC59984 induced cell death in apanel of cancer cells but displayed little or no cytotoxicity towards normal cells.Noxa mRNA slightly increased in response to 25 μM of NSC59984 in HCT116 and 12 μM of NSC59984 in p53-null HCT116 cells [1].
In vivo: In nude mice bearing colon-tumor xenografts, NSC59984 (i.p. injection, 45mg/kg) did not cause an obvious change in mouse body weights and no overt toxic effects. NSC59984 treatment significantly repressed the DLD-1 xenograft tumor growth. Tumor weight measured at day 15 reduced by 34% in DLD-1 xenograft tumors. In p73 knock-down DLD-1 xenograft tumors, NSC59984 didn’t suppress tumor growth. In p73 knock-down DLD-1 xenograft tumors, NSC59984 treatment reduced tumor weight by 18% [1].
Reference:
[1].Zhang S, Zhou L, Hong B, et al. Small-molecule NSC59984 restores p53 pathway signaling and antitumor effects against colorectal cancer via p73 activation and degradation of mutant p53[J]. Cancer research, 2015, 75(18): 3842-3852
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| Cas No. | 803647-40-7 | SDF | |
| 化学名 | (E)-1-(4-methylpiperazin-1-yl)-3-(5-nitrofuran-2-yl)prop-2-en-1-one | ||
| Canonical SMILES | CN1CCN(C(/C=C/C2=CC=C([N+]([O-])=O)O2)=O)CC1 | ||
| 分子式 | C12H15N3O4 | 分子量 | 265.27 |
| 溶解度 | DMF: 25 mg/ml,DMSO: 10 mg/ml,Ethanol: 5 mg/ml | 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 | 3.7697 mL | 18.8487 mL | 37.6974 mL |
| 5 mM | 0.7539 mL | 3.7697 mL | 7.5395 mL |
| 10 mM | 0.377 mL | 1.8849 mL | 3.7697 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: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet