MZP-55
目录号 : GC33363
MZP-55是基于PROTAC技术的一种选择性的BRD3/4降解剂，对Brd4BD2的Kd值为8nM。
Cas No.:2010159-48-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: | MV4;11 or HL60 cells are incubated with MZP-55 at the desired concentration for 48 h on a clear-bottom 384-well plate. Cells are kept in RPMI medium supplemented with 10% FBS, l-glutamine, penicillin, and streptomycin. Initial cell density is 3 × 105 per mL. Cells are treated with various concentrations of MZP-55 or 0.05% DMSO. After treatment, cell viability is measured with cell viability assay kit. Signal is recorded. Data are analyzed with Graphpad Prism software to obtain EC50 values of each MZP-55[1]. |
References: [1]. Chan KH, et al. Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds. J Med Chem. 2018 Jan 25;61(2):504-513. | |
MZP-55 is a selective degrader of BRD3/4 based on PROTAC technology, with a Kd of 8 nM for Brd4BD2.
MZP-55 is a selective degrader of BRD3/4 based on PROTAC technology, with a Kd of 8 nM for Brd4BD2. MZP-55 binds to VHL-EloC-EloB protein (VCB) with a Kd of 105 ± 24 nM. MZP-55 shows an inhibitory activity against MV4;11 and HL60 cells, with pEC50s of 7.31 ± 0.03 and 6.57 ± 0.02, respectively[1].
[1]. Chan KH, et al. Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds. J Med Chem. 2018 Jan 25;61(2):504-513.
| Cas No. | 2010159-48-3 | SDF | |
| Canonical SMILES | CC(N=CS1)=C1C2=CC=C(CNC([C@@H]3C[C@@H](O)CN3C([C@H](C(C)(C)C)NC(COCCOCCOCCOCCNC(C(C=C4)=CC=C4C5=CC6=C(C=C5)N(C(C)=O)[C@@H](C)C[C@H]6NC7=CC=C(Cl)C=C7)=O)=O)=O)=O)C=C2 | ||
| 分子式 | C57H70ClN7O10S | 分子量 | 1080.72 |
| 溶解度 | DMSO: 50 mg/mL (46.27 mM) | 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 | 0.9253 mL | 4.6265 mL | 9.2531 mL |
| 5 mM | 0.1851 mL | 0.9253 mL | 1.8506 mL |
| 10 mM | 0.0925 mL | 0.4627 mL | 0.9253 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。