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- 保存条件：
Powder: -20°C, 3 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
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MedChemExpress LLC
- CAS号：
2851841-61-5
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1 mg/5 mg/10 mg
| 规格： | 1 mg | 产品价格： | ￥1250.0 |
|---|---|---|---|
| 规格： | 5 mg | 产品价格： | ￥3123.0 |
| 规格： | 10 mg | 产品价格： | ￥4995.0 |
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Menin-MLL inhibitor-22
CAS No. : 2851841-61-5
MCE 国际站：Menin-MLL inhibitor-22
产品活性：Menin-MLL inhibitor-22 (compound C20) 是一种口服有效的针对 menin 和混合谱系白血病 (MLL) 相互作用的抑制剂 (IC50=7 nM)。Menin-MLL inhibitor-22 通过结合 menin 蛋白，抑制癌细胞生长 (MV4 细胞，IC50=0.3 μM)。Menin 是一种与多内分泌肿瘤 1 型 (MEN-1 综合征) 相关的肿瘤抑制因子。
研究领域：Epigenetics
作用靶点：Epigenetic Reader Domain
In Vitro: Menin-MLL inhibitor-22 (1 μM; 60 min) possesses good stability and low clearance rate in liver microsomes.
Menin-MLL inhibitor-22 (1 and 10 μM; 24 h) inhibits MLL-r Leukemia cells MV4;11 growth and (0.1-10 μM; 24 h) decreases the expression of the HOXA9 and MEIS1 induced by menin-MLL interaction.
Menin-MLL inhibitor-22 (1, and 10 μM; 7 d) increases the amount of CD11b, a differentiation marker of myeloid cells, indicating a reverse the differentiation arrest of MLL-r leukemia cells.
Menin-MLL inhibitor-22 (1, and 10 μM; 24 h) induces cell apoptosis and G0/G1 cell cycle arrest.
In Vivo: Menin-MLL inhibitor-22 (6 mg/kg and 30 mg/kg; p.o.; every second day for 16 days) shows potent antitumor activity in the MV4;11 subcutaneous xenograft models of MLL-rearranged leukemia.
Pharmacokinetic Properties in SD Rats
| Route | Dose (mg/kg) | Tmax (h) | T1/2 (h) | MRT (h) | Cmax (ng/mL) | AUC0-t (ng·h/mL) | AUC0-∞ (ng·h/mL) | Cltotal (mL/h/kg) | Vss (L/kg) | F (%) |
| i.v. | 5 | N/A | 17.5 | 7.1 | 1187 | 1700 | 2495 | 2056 | 49.3 | |
| p.o. | 15 | 7.3 | 15.5 | 12.0 | 56.7 | 863.7 | 1476 | 10730 | 23 | 16.9 |
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Panhandle PCR Approaches to Cloning MLL Genomic Breakpoint Junctions and Fusion Transcript Sequences
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