生物活性
MALT1 inhibitor（MI-2）是一种 MALT1 抑制剂 (IC50=5.84 μM)，MALT1 inhibitor（MI-2）直接与 MALT1 结合，不可逆地抑制蛋白酶功能。MALT1 inhibitor (ABM-3912) decreases NF-κB activity induced by MALT1. MALT1 inhibitor (ABM-3912) inhibits cell proliferation and MALT1-mediated cleavage activity. MALT1 inhibitor (ABM-3912) concentrates within human ABC-DLBCL cells and irreversibly inhibited cleavage of MALT1 substrates. MALT1 inhibitor (ABM-3912) displayes selective activity against ABC-DLBCL cell lines in vitro and xenotransplanted ABC-DLBCL tumors in vivo.
化学数据
| 分子量 | 455.72 |
| 分子式 | C19H17Cl3N4O3 |
| CAS号 | 1047953-91-2 |
| 纯度 | 99.92% |
| 溶解性（25°C） | DMSO ≥ 35 mg/mL |
| 储存和运输条件 | 固体粉末： -20°C 冷藏长期储存
常温运输及临时存放 |
实验操作 来自于公开的文献，仅供相同实验参考（如实验材料、目的不同，请参考其他文献）
| 细胞实验 |
|---|
| 细胞系 | MLL-AF9 and E2A-HLF transduced murine BMC |
| 方法 | Plating the MLL-AF9 and E2A-HLF transduced murine BMC in 12-well plates at the concentration of 5×103cells/mL with 1 mL methylcellulose medium M3234 containing 20% IMDM medium, 1% penicillin/streptomycin, IL-3 and 0.25% DMSO or compounds.After 6 days staining colonies with 100 μL iodonitrotetrazolium chloride at final concentration of 1 mg/mL, incubating at 37°C for 30 min and counting . To replate for the 2nd round, counting colonies at day 6 without staining and washing cells out by 1×PBS buffer and resuspending in IMDM medium which contains 15% FBS, 1% penicillin/streptomycin and IL-3.Plateing 5×103 cells in 12-well plates with 1ml methycellulose medium M3234 containing 20% IMDM medium, 1% penicillin/streptomycin, IL-3 and 0.25% DMSO or compounds. 6 days later staining and counting colonies . |
| 浓度 | ~20 μM |
| 处理时间 | 12 days |
不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 |
| 重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| 体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km系数 | 3 | 6 | 12 | 8 | 5 | 20 |
| 动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
| 动物 A的Km系数 |
例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。
储备液配制
以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.1943 mL | 10.9716 mL | 21.9433 mL |
| 5 mM | 0.4389 mL | 2.1943 mL | 4.3887 mL |
| 10 mM | 0.2194 mL | 1.0972 mL | 2.1943 mL |
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