Enzomenib
(Synonyms: DSP-5336) 目录号 : GC92678Enzomenib is an inhibitor of the protein-protein interaction between menin and mixed-lineage leukemia 1 (MLL1).
Cas No.:2412555-70-3
Sample solution is provided at 25 µL, 10mM.
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Enzomenib is an inhibitor of the protein-protein interaction between menin and mixed-lineage leukemia 1 (MLL1). It binds to menin (Kd = 6 nM) and inhibits the menin-MLL1 interaction with an IC50 value of 1.4 nM. Enzomenib selectively inhibits the growth of MV4-11, MOLM-13, KOPN-8, and OCI-AML-3 leukemia cells (IC50s = 10, 15, 31, and 15 nM, respectively), which contain MLL rearrangement (MLL-r) or NPM1 mutations, over HL-60, MOLT-4, and Reh leukemia cells (IC50s = >10 µM for all), which do not have MLL-r or NPM1 mutations. In vivo, enzomenib (25 and 50 mg/kg) has antitumor activity in a mouse xenograft model using MV4-11 cells, which express an MLL-AF4 gene fusion.
| Cas No. | 2412555-70-3 | SDF | |
| 别名 | DSP-5336 | ||
| 化学名 | 5-fluoro-2-[[4-[7-[[(1S,3S,4R)-5-methylene-2-azabicyclo[2.2.2]oct-3-yl]carbonyl]-2,7-diazaspiro[3.5]non-2-yl]-5-pyrimidinyl]oxy]-N,N-bis(1-methylethyl)-benzamide | ||
| Canonical SMILES | O=C([C@@H]1[C@@]2([H])C(C[C@@](CC2)([H])N1)=C)N3CCC4(CC3)CN(C4)C5=NC=NC=C5OC6=C(C(N(C(C)C)C(C)C)=O)C=C(F)C=C6 | ||
| 分子式 | C33H43FN6O3 | 分子量 | 590.744403 |
| 溶解度 | Acetonitrile: Slightly Soluble: 0.1-1 mg/ml; DMSO: Slightly Soluble: 0.1-1 mg/ml | 储存条件 | -20°C |
| 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 | 1.6928 mL | 8.4639 mL | 16.9278 mL |
| 5 mM | 338.6 μL | 1.6928 mL | 3.3856 mL |
| 10 mM | 169.3 μL | 846.4 μL | 1.6928 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