AZD4877
目录号 : GC73016AZD4877是Ispinesib的另一种同分异构体，也是一种激酶纺锤体蛋白（Eg5）抑制剂，IC50为2 nM。
Cas No.:758722-49-5
Sample solution is provided at 25 µL, 10mM.
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AZD4877 is another isostere to Ispinesib and also a kinesin spindle protein (Eg5) inhibitor with IC50 of 2 nM.AZD4877 arrests cell mitosis, leads to the formation of the monopolar spindle phenotype and induces apoptosis. AZD4877 inhibits circulating peripheral blood mononuclear cells (PBMCs) and has anti-cancer activity.
AZD4877 (10 nM, 24 or 48 hours) induces apoptosis in human bladder cancer cells and AZD4877-sensitive cells generally expressed high levels of p63[2].
AZD4877 (i.v., 6 mg/kg, 12 mg/kg; single dose) has a significant reduction in cell viability and increase in cleaved caspase 3 levels by 48 h post dose in a rat hollow fiber model[1]. AZD4877 (i.v., 6 mg/kg; single dose) shows a T1/2 of 3.5 h, and CL of 36 mL/min/kg in Hans Wistar rats[1].
References:
[1]. Theoclitou ME, et.al. Discovery of (+)-N-(3-aminopropyl)-N-[1-(5-benzyl-3-metl-4-oxo-[1,2]thiazolo[5,4-d]pyrimidin-6-yl)-2-metlpropyl]-4-metlbenzamide (AZD4877), a kinesin spindle protein inhibitor and potential anticancer agent. J Med Chem. 2011 Oct 13;54(19):6734-50.
[2]. Marquis L, et.al. p63 expression correlates with sensitivity to the Eg5 inhibitor ZD4877 in bladder cancer cells. Cancer Biol Ther. 2012 May;13(7):477-86.
[3]. Gerecitano JF, et.al. A Phase I trial of the kinesin spindle protein (Eg5) inhibitor AZD4877 in patients with solid and lymphoid malignancies. Invest New Drugs. 2013 Apr;31(2):355-62.
[4]. Shahin R, et.al. Kinesin spindle protein inhibitors in cancer: from high throughput screening to novel therapeutic strategies. Future Sci OA. 2022 Feb 21;8(3):FSO778.
[5]. Myers SM, et.al. Recent findings and future directions for interpolar mitotic kinesin inhibitors in cancer therapy. Future Med Chem. 2016;8(4):463-89.
| Cas No. | 758722-49-5 | SDF | |
| 分子式 | C28H33N5O2S | 分子量 | 503.66 |
| 溶解度 | 储存条件 | -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 | 1.9855 mL | 9.9273 mL | 19.8547 mL |
| 5 mM | 0.3971 mL | 1.9855 mL | 3.9709 mL |
| 10 mM | 0.1985 mL | 0.9927 mL | 1.9855 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