ML390
目录号 : GC14415
A DHODH inhibitor
Cas No.:2029049-79-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
IC50: 0.56 μM
ML390 is a human DHODH inhibitor.
Homeobox (Hox) transcription factors are reported to be involved in the hematopoietic differentiation. Recently studies have showed that the inhibitors of dihydroorotate dehydrogenase (DHODH) can induce the differentiation in multiple AML models in vitro and in vivo. More importantly, DHODH inhibitors have been found to be effective at prolonging survival in animal models of leukemia.
In vitro: In the screening study, ML390 was identified as the most potent compound against the engineered ERHOX-GFP cell line. Moreover, the addition of uridine to the cell culture media could abrogate the differentiation effects of ML390, demonstrating further evidences that ML390’ effects were due to their inhibition of DHODH-catalyzed pyrimidine synthesis. In addition, ML390 was found to be not able to inhibit DHODH in the P. falciparum parasite, which is the causative agent of malaria. Furthermore, the X-ray structure indicated that the binding of ML390 to the enzyme might be increased by modifying ML390 with a ring in its central portion to lock the molecule into its binding conformation with the amide substituents [1].
In vivo: So far, there is no animal in vivo data reported.
Clinical trial: Up to now, ML390 is still in the preclinical development stage.
Reference:
[1] Timothy A Lewis et al. Development of ML390: A Human DHODH Inhibitor That Induces Differentiation in Acute Myeloid Leukemia. ACS Med Chem Lett 2016 Dec 28;7(12):1112-1117. Epub 2016 Sep 28.
| Cas No. | 2029049-79-2 | SDF | |
| 化学名 | (R)-N-(3-oxo-3-((1,2,3,4-tetrahydronaphthalen-1-yl)amino)propyl)-4-(trifluoromethoxy)benzamide | ||
| Canonical SMILES | O=C(NCCC(N[C@@H]1CCCC2=C1C=CC=C2)=O)C3=CC=C(OC(F)(F)F)C=C3 | ||
| 分子式 | C21H21F3N2O3 | 分子量 | 406.4 |
| 溶解度 | ≥ 40.6mg/mL in DMSO | 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 | 2.4606 mL | 12.3031 mL | 24.6063 mL |
| 5 mM | 0.4921 mL | 2.4606 mL | 4.9213 mL |
| 10 mM | 0.2461 mL | 1.2303 mL | 2.4606 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。