MI-3
(Synonyms: Menin-MLL inhibitor 3;Thieno[2,3-d]pyrimidine, 4-[4-(4,5-dihydro-5,5-dimethyl-2-thiazolyl)-1-piperazinyl]-6-(1-methylethyl)-) 目录号 : GC12199
An inhibitor of menin-MLL fusion protein interactions
Cas No.:1271738-59-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
MI-3 is an inhibitor of Menin-Mixed linage leukemia (MML) protein interaction with IC50 value of 648 ± 25 nM [1].
MLL protein is a histone methyltransferase that positively regulates gene transcription. However, MLL gene is a common target for chromosomal translocations found in some leukemia. Fusion of MLL gene with one of over 50 different partner genes forms chimeric oncogenes encoding MLL fusion proteins. Translocations will disrupt the regulatory ability of MLL protein on HOX gene, resulting in enhanced cell proliferation and blocked hematopoietic differentiation. Menin is a tumor suppressor protein which directly controls cell growth in endocrine organs. Importantly, menin is also a highly specific partner of MLL. The regulatory function of MLL and MLL fusion protein is facilitated by the association of menin. Therefore, the interaction between MLL fusion protein and menin is critical for the pathology of leukemia [1].
In HEK293 cells expressing menin and MLL-AF9 fusion protein, treatment of MI-3 resulted in significant disruption of menin-MLL-AF9 complex without affecting expression level of menin and MLL-AF9 complex [1]. In mouse bone marrow cells (BMC) transduced with MLL-AF9 and MLL-ENL, MI-3 was observed to effectively inhibit menin-MLL interaction-induced cell proliferation, transformation and hematopoietic differentiation [1].
In human MLL leukemia cell lines harboring different translocations, MI-3 treatment showed an effective and dose-dependent growth inhibition of several cell lines with different MLL translocations [1].
Reference:
[1] Grembecka J et al. , Menin-MLL inhibitors reverse oncogenic activity of MLL fusion proteins in leukemia. Nature Chemical Biology. 2012, 8(3): 277-284.
| Cas No. | 1271738-59-0 | SDF | |
| 别名 | Menin-MLL inhibitor 3;Thieno[2,3-d]pyrimidine, 4-[4-(4,5-dihydro-5,5-dimethyl-2-thiazolyl)-1-piperazinyl]-6-(1-methylethyl)- | ||
| 化学名 | 4-(4-(5,5-dimethyl-4,5-dihydrothiazol-2-yl)piperazin-1-yl)-6-isopropylthieno[2,3-d]pyrimidine | ||
| Canonical SMILES | CC(C1=CC2=C(N3CCN(C(S4)=NCC4(C)C)CC3)N=CN=C2S1)C | ||
| 分子式 | C18H25N5S2 | 分子量 | 375.55 |
| 溶解度 | DMSO: slightly soluble,Ethanol: slightly soluble | 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 | 2.6628 mL | 13.3138 mL | 26.6276 mL |
| 5 mM | 0.5326 mL | 2.6628 mL | 5.3255 mL |
| 10 mM | 0.2663 mL | 1.3314 mL | 2.6628 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。