AZD-5991
目录号 : GC33247
An Mcl-1 inhibitor
Cas No.:2143061-81-6
Sample solution is provided at 25 µL, 10mM.
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AZD 5991 is an inhibitor of myeloid cell leukemia-1 (Mcl-1; IC50 = 0.72 nM).1 It is selective for Mcl-1 over Bcl-2, Bcl-xL, Bcl-W, and Bfl-1 (IC50s = 20, 36, 49, and 24 ?M, respectively). AZD 5991 decreases the viability of MV4-11 acute myeloid leukemia (AML) and MOLP-8 multiple myeloma (MM) cells with EC50 values of 24 and 33 nM, respectively. It disrupts formation of the Mcl-1-Bak complex and induces apoptosis in MOLP-8 cells when used at a concentration of 500 nM. AZD 5991 induces complete tumor regression in MV4-11 and MOLP-8 mouse xenograft models when administered at a single dose of 100 mg/kg.
1.Tron, A.E., Belmonte, M.A., Adam, A., et al.Discovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemiaNat. Commun.9(1)5341(2018)
Animal experiment: | Mice and Rats[1]In mice, drugs (e.g., AZD5991; 10-100 mg/kg) are dosed intravenously in a volume of 5 mL/kg except for Venetoclax that is dosed orally in a volume of 10 mL/kg. One million MV4-11, five million MOLP-8, ten million NCI-H929 or five million OCI-AML3 cells are injected subcutaneously in the right flank of mice in a volume of 0.1 mL. In rats, AZD5991 (10-100 mg/kg) is dosed intravenously in a volume of 10 mL/kg. Ten million MV4-11 cells are injected subcutaneously in the right flank of rats in a volume of 0.1 mL. Tumor volumes (measured by caliper), animal body weight, and tumor condition are recorded twice weekly for the duration of the study. The tumor volume is calculated[1]. |
References: [1]. Tron AE, et al. Discovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemia. Nat Commun. 2018 Dec 17;9(1):5341. | |
| Cas No. | 2143061-81-6 | SDF | |
| Canonical SMILES | O=C(O)C1=C(CCCOC2=C(C=CC=C3)C3=CC4=C2)C5=C(N1C)C(C6=C(C)N(C)N=C6CSCC7=NN(C)C(CS4)=C7)=C(Cl)C=C5 | ||
| 分子式 | C35H34ClN5O3S2 | 分子量 | 672.26 |
| 溶解度 | DMSO : 41.67 mg/mL (61.98 mM);Water : < 0.1 mg/mL (insoluble) | 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 | 1.4875 mL | 7.4376 mL | 14.8752 mL |
| 5 mM | 0.2975 mL | 1.4875 mL | 2.975 mL |
| 10 mM | 0.1488 mL | 0.7438 mL | 1.4875 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: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet