2. Epigenetics
  3. Epigenetic Reader Domain
  4. Menin-MLL-IN-37

Menin-MLL-IN-37 是一种具有口服活性的 Menin-MLL 蛋白复合物抑制剂，其 IC50 为 820.50 nM。Menin-MLL-IN-37 可破坏 menin 与 MLL 蛋白之间的相互作用。Menin-MLL-IN-37 可诱导急性髓系白血病细胞分化，并选择性抑制 MLL 重排型及 DNMT3A/NPM1 突变型白血病细胞的增殖。Menin-MLL-IN-37 可用于急性髓系白血病 (AML) 的相关研究。

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Menin-MLL-IN-37

Menin-MLL-IN-37 Chemical Structure

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Customer Review

Menin-MLL-IN-37 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Menin-MLL-IN-37 is an orally active Menin-MLL protein complex inhibitor with an IC50 of 820.50 nM. Menin-MLL-IN-37 disrupts the interaction between menin and MLL proteins. Menin-MLL-IN-37 induces differentiation of acute myeloid leukemia cells and selectively inhibits the proliferation of MLL-rearranged and DNMT3A/NPM1-mutant leukemia cells. Menin-MLL-IN-37 can be used for the research of acute myeloid leukemia (AML)[1].

IC50 & Target[1]

Menin-MLL

820.50 nM (IC50)

体外研究
(In Vitro)

Menin-MLL-IN-37 (Compound A13) 可强效抑制 MLL 重排 (MV4-11、MOLM-13)、DNMT3A/NPM1 突变 (OCI-AML3) 及其他白血病细胞系 (THP-1, HL-60, K562) 的增殖，其 IC50 值分别为 0.379、0.838、0.763、1.618、1.179 和 2.653 μM[1]。
Menin-MLL-IN-37 (1-2 μM; 7 days) 可诱导 MV4-11 和 MOLM-13 白血病细胞分化，导致 CD11b 表面表达水平升高[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Menin-MLL-IN-37 相关抗体:

Cell Differentiation Assay[1]

Cell Line: MV4-11, MOLM-13 leukemia cell lines
Concentration: 1000 nM, 2000 nM
Incubation Time: 7 days
Result: Induced a significant increase in the percentage of CD11b-positive cells in MV4-11 cell line.
Induced a significant increase in the percentage of CD11b-positive cells in MOLM-13 cell line.
药代动力学
(Parmacokinetics)
Species Dose Route Tmax T1/2 Cmax AUC0-t AUC0-∞ MRT0-t Vz/F CL/F
Mice[1] 20 mg/kg i.g. 1.67 h 2.43 h 537.00 ng/mL 2241.09 ng·h/mL 2379.51 ng·h/mL 3.59 h 30499.24 mL/kg 147.32 mL/min/kg
体内研究
(In Vivo)

Menin-MLL-IN-37 (Compound A13) (20 mg/kg；灌胃；单剂量) 在小鼠中展现出良好的口服药代动力学特性 ，其吸收迅速且生物利用度高[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Mice[1]
Dosage: 20 mg/kg
Administration: I.g.; Blood samples were then collected at 0.25, 0.5, 1, 2, 4, 8, and 24 h post-dose
Result: Displayed favorable oral pharmacokinetic properties (Tmax=1.67 h, AUC=2241 ng h/mL), characterized by rapid absorption and high bioavailability, demonstrating its potential as a therapeutic agent
分子量

638.77

Formula

C29H37F3N6O3S2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Menin-MLL-IN-37 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Menin-MLL-IN-37Epigenetic Reader DomainMLL-rearranged leukemia cellsDNMT3A/NPM1-mutated leukemia cellsMOLM-13 cellsMV4-11 cellsOCI-AML3 cellsMLL proteinshuman menin proteinacute myeloid leukemia cellsMenin-MLL protein complexmeninInhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-181690
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