ZINC69391
目录号 : GC66020
ZINC69391 是一种特异的 Rac1 抑制剂，通过在 Rac1 表面掩蔽 Trp56 残基来干扰 Rac1-GEF 的相互作用。ZINC69391 干扰 Rac1 与 Dock180 的相互作用，降低 Rac1-GTP水平。ZINC69391 诱导细胞凋亡，具有抗增殖和抗转移作用。
Cas No.:303094-67-9
Sample solution is provided at 25 µL, 10mM.
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ZINC69391, a specific Rac1 inhibitor, interferes with Rac1-GEF interaction by masking Trp56 residue on Rac1 surface. ZINC69391 interferes with the interaction of Rac1 with Dock180 and reduces Rac1-GTP levels. ZINC69391 induces apoptosis, and shows antiproliferative and antimetastatic effects[1][2][3].
ZINC69391 inhibits growth of U937, HL-60, KG1A and Jurkat cells with IC50s ranging from 41 to 54 μM[1].
ZINC69391 (50-100 μM; 24 hours) augments the enzymatic activity of caspase 3 in a concentration dependent manner[1].
ZINC69391 (0-125 μM; 72h) reduces cell proliferation of human glioma cells[2].
ZINC69391 (50-100 μM; 48 hours) triggers cell cycle arrest[2].
ZINC69391 (50 μM; 24 hours) triggers apoptosis on human acute leukemic cells[1].
Cell Proliferation Assay[2]
| Cell Line: | U-87 MG, LN229 cells |
| Concentration: | 0-125μM |
| Incubation Time: | 72 hours |
| Result: | Reduced cell proliferation in a concentration-dependent manner. |
Cell Cycle Analysis[2]
| Cell Line: | LN229 cells |
| Concentration: | 50, 100 μM |
| Incubation Time: | 48 hours |
| Result: | Resulted in a significant increased percentage of cells in the sub-G0/G1 phase in a concentration dependent manner. |
Apoptosis Analysis[1]
| Cell Line: | HL-60, U937 and KG1A cell lines |
| Concentration: | 50 μM |
| Incubation Time: | 24 hours |
| Result: | Led to a significant increase in apoptotic cells. |
ZINC69391 (25 mg/kg; i.p; daily for 21 days) impairs metastatic lung colonization in a syngeneic animal model[3].
| Animal Model: | Specific pathogen-free female BALB/c inbred mice (bearing F3II cells)[3] |
| Dosage: | 25 mg/kg body weight |
| Administration: | I.p; daily for 21 days |
| Result: | Significantly reduced by about 60% the formation of total metastatic lung colonies. |
| Cas No. | 303094-67-9 | SDF | Download SDF |
| 分子式 | C14H14F3N5 | 分子量 | 309.29 |
| 溶解度 | DMSO : 25 mg/mL (80.83 mM; ultrasonic and warming and heat to 60°C) | 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 | 3.2332 mL | 16.1661 mL | 32.3321 mL |
| 5 mM | 0.6466 mL | 3.2332 mL | 6.4664 mL |
| 10 mM | 0.3233 mL | 1.6166 mL | 3.2332 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: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet