CAS NO: | 173436-66-3 |
A cell-permeable compound that targets β-catenin via direct affinity interaction within the C-terminal two thirds (a.a. 301-670) of the Armadillo repeat region (a.a. 136–686), inducing β-catenin ubiquitination and proteasomal degradation (Eff. conc. 1.25-5 μM in DLD-1, SW480 and LS174T cultures). MSAB selectively inhibits against Wnt sginaling-dependent proliferation of cancer cells (IC50 <6 μM), while exhibiting little efficacy in Wnt-independent cultures (<10% inhibition at 10 μM). Likewise, daily intraperitoneal injection (10-20 mg/kg/day) is efficacious in suppressing the expansion of established tumors from HCT116, HT115, and H23 xenografts in mice, while exhibiting little efficacy against the Wnt-independent H460 tumor growth.
分子量 | 305.35 |
分子式 | C15H15NO4S |
CAS号 | 173436-66-3 |
纯度 | >98% |
溶解性(25°C) | DMSO: 25 mg/mL clear |
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 |
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。
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 | 3.2749 mL | 16.3747 mL | 32.7493 mL |
5 mM | 0.655 mL | 3.2749 mL | 6.5499 mL |
10 mM | 0.3275 mL | 1.6375 mL | 3.2749 mL |