AZ 10417808
目录号 : GC13171
Caspase-3 inhibitor,selective non-peptide
Cas No.:331645-84-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
AZ 10417808 is a selective caspase-3 inhibitor with IC50 value of 14.9 uM [1].
The caspase-3 protein is a member of the cysteine-aspartic acid protease (caspase) family. Sequential activation of caspases plays a central role in the execution-phase of cell apoptosis [1].
AZ 10417808 (AQZ-1) is a potent small molecule nonpeptidic inhibitor of caspase-3, which block cellular and biochemical features of apoptosis [1].
AZ 10417808 was evaluated for its inhibitory activity against caspases 1, 2, 3, 6, 7, 8 and only caspases-3 was potently inhibited. AZ 10417808 completely blocked the staurosporine-induced intracellular DEVDase activity and this effect was dose-dependent. Of control cells ( 64 ± 7%) whereas cells treated with staurosporine plus 10 μM AZ 10417808 had 92 ± 2% viability, which indicated that the AZ 10417808 enhanced cell viability in SH-SY5Y cell culture apoptosis paradigm [1].
Reference:
[1]. Scott CW, Briner CS, Wilkins DE, et al. Novel small molecule inhibitors of caspase-3 block cellular and biochemical features of apoptosis. J Pharmacol Exp Ther, 2003, 304(1): 433-40.
| Cas No. | 331645-84-2 | SDF | |
| 化学名 | 2-(3,4-dichloroanilino)-6-nitro-4-oxo-N-prop-2-enyl-1H-quinazoline-8-carboxamide | ||
| Canonical SMILES | C=CCNC(=O)C1=C2C(=CC(=C1)[N+](=O)[O-])C(=O)N=C(N2)NC3=CC(=C(C=C3)Cl)Cl | ||
| 分子式 | C18H13Cl2N5O4 | 分子量 | 434.23 |
| 溶解度 | <10.86mg/ml in DMSO | 储存条件 | Store at RT |
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.3029 mL | 11.5146 mL | 23.0293 mL |
| 5 mM | 0.4606 mL | 2.3029 mL | 4.6059 mL |
| 10 mM | 0.2303 mL | 1.1515 mL | 2.3029 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。