NSC 207895 (XI-006)
(Synonyms: 4-(4-甲基-1-哌嗪基)-7-硝基-2,1,3-苯并二唑3-氧化物,XI-006) 目录号 : GC12701
An inhibitor of MDMX
Cas No.:58131-57-0
Sample solution is provided at 25 µL, 10mM.
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NSC 207895 is a small-molecule inhibitor of MDMX with GI50 value of 117nM [1].
NSC 207895 is a benzofuroxan derivative and is less toxic. NSC 207895 decreases the activity of MDMX promoter and subsequently decreases both the mRNA and protein levels of MDMX in MCF-7 cells. This inhibition of MDMX is accompanied with the activation of p53. NSC 207895 induces apoptosis in MCF-7 cells since it induces pro-apoptotic gene expression. It is found that the cleavage of PARP is significantly induced by NSC 207895 [2].
NSC 207895 is also found to be a DNA-damaging agent. It shows strong functional interactions with both DNA repair and replication fork complexes. NSC 207895 activates the DNA damage response (DDR) and leads a delay in cell cycle progression [3].
References:
[1] Hawes JJ, Nerva JD, Reilly KM. Novel dual-reporter preclinical screen for antiastrocytoma agents identifies cytostatic and cytotoxic compounds. J Biomol Screen. 2008 Sep;13(8):795-803.
[2] Wang H, Ma X, Ren S, Buolamwini JK, Yan C. A small-molecule inhibitor of MDMX activates p53 and induces apoptosis. Mol Cancer Ther. 2011 Jan;10(1):69-79.
[3] Kapitzky L, Beltrao P, Berens TJ, Gassner N, Zhou C, Wüster A, Wu J, Babu MM, Elledge SJ, Toczyski D, Lokey RS, Krogan NJ. Cross-species chemogenomic profiling reveals evolutionarily conserved drug mode of action. Mol Syst Biol. 2010 Dec 21;6:451.
| Cas No. | 58131-57-0 | SDF | |
| 别名 | 4-(4-甲基-1-哌嗪基)-7-硝基-2,1,3-苯并二唑3-氧化物,XI-006 | ||
| 化学名 | 4-(4-methylpiperazin-1-yl)-7-nitro-3-oxido-2,1,3-benzoxadiazol-3-ium | ||
| Canonical SMILES | CN1CCN(CC1)C2=CC=C(C3=NO[N+](=C23)[O-])[N+](=O)[O-] | ||
| 分子式 | C11H13N5O4 | 分子量 | 279.25 |
| 溶解度 | DMF: 15 mg/mL,DMF:PBS (pH 7.2) (1:4): 0.2mg/mL,DMSO: 2 mg/mL,Ethanol: 1 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 | 3.581 mL | 17.9051 mL | 35.8102 mL |
| 5 mM | 0.7162 mL | 3.581 mL | 7.162 mL |
| 10 mM | 0.3581 mL | 1.7905 mL | 3.581 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet