ZM336372
目录号 : GC13286
An activator of the Raf-1 signalling pathway
Cas No.:208260-29-1
Sample solution is provided at 25 µL, 10mM.
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ZM336372 is a potent inhibitor of C-Raf with IC50 value of 70 nM [1]. It is also reported that ZM336372 inhibits SAPK2b/p38β2 with IC50 value of 2 μM.
C-Raf is a member of the Raf kinase family of serine/threonine-specific protein kinases and plays an important role in the ERK1/2 pathway. It has been reported that abnormal expression of C-Raf correlates with human diseases and also involves in a variety of cancers.
ZM336372 is a potent C-Raf inhibitor and has a different selectivity with the reported C-Raf inhibitor PD98059. When tested with primary neurons, ZM3363372 treatment decreased low potassium-induced apoptosis percent by inhibiting C-Raf activation [2]. In tumor spheroids pretreated with H2O2 and ZM336372 for 24 hours totally abolished the ROS-induced eNOS up-regulation via mediating ERK1/2 signaling pathway [3].
References:
1. Hall-Jackson, C.A., et al., Paradoxical activation of Raf by a novel Raf inhibitor. Chem Biol, 1999. 6(8): p. 559-68.
2. Burgess, S. and V. Echeverria, Raf inhibitors as therapeutic agents against neurodegenerative diseases. CNS Neurol Disord Drug Targets, 2010. 9(1): p. 120-7.
3. Wartenberg, M., et al., Reactive oxygen species-mediated regulation of eNOS and iNOS expression in multicellular prostate tumor spheroids. Int J Cancer, 2003. 104(3): p. 274-82.
Cell experiment: | Proliferation of H727 and BON cells after treatment with ZM336372 is measured using a 3,4-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide. Cells are trypsinized and plated in triplicate to 24-well plates and allowed to adhere overnight. Then, cells are treated with either 100 μM ZM336372 or DMSO (2%) and incubated. Media are changed every 2 days with new treatment. At each time point, cell growth rates are analyzed after the addition of 3,4-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide reagent to the cultured cells. Absorbance is determined using spectrophotometer at a wavelength of 540 nm[2]. |
References: [1]. Hall-Jackson CA, et al. Paradoxical activation of Raf by a novel Raf inhibitor. Chem Biol. 1999 Aug;6(8):559-68. | |
| Cas No. | 208260-29-1 | SDF | |
| 化学名 | 3-(dimethylamino)-N-[3-[(4-hydroxybenzoyl)amino]-4-methylphenyl]benzamide | ||
| Canonical SMILES | CC1=C(C=C(C=C1)NC(=O)C2=CC(=CC=C2)N(C)C)NC(=O)C3=CC=C(C=C3)O | ||
| 分子式 | C23H23N3O3 | 分子量 | 389.4 |
| 溶解度 | ≥ 19.45mg/mL in DMSO | 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 | 2.5681 mL | 12.8403 mL | 25.6805 mL |
| 5 mM | 0.5136 mL | 2.5681 mL | 5.1361 mL |
| 10 mM | 0.2568 mL | 1.284 mL | 2.5681 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