生物活性
Fumitremorgin C (FTC) is a fungal toxin of the diketopiperazines family of compounds. In mammalian cells, FTC is tremorgenic and causes cell cycle arrest. Fumitremorgin C has been shown to reverse resistance to doxorubicin, mitoxantrane, and topotecan in non-Pgp (P-glycoprotein), non-MRP (multidrug resistance protein) multidrug-resistance (MDR) cells. This reversal of resistance is associated with an increase in drug accumulation. Fumitremorgin C is a specific, selective, and potent inhibitor at micromolar concentrations of the breast cancer resistant protein (BCRP/ABCG2), an ABC transporter associated with chemotherapy resistance. FTC, in combination with mitoxantrone, can be used for the detection of ABCG2 functional activity in several cell lines.
化学数据
| 分子量 |
379.45 |
| 分子式 |
C22H25N3O3 |
| CAS号 |
118974-02-0 |
| 纯度 |
>98% |
| 溶解性（25°C） |
acetonitrile: soluble 5 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 |
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
以下数据基于半岛bd体育手机客户端 分子量，对于特殊半岛bd体育手机客户端 ，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 |
2.6354 mL |
13.177 mL |
26.3539 mL |
| 5 mM |
0.5271 mL |
2.6354 mL |
5.2708 mL |
| 10 mM |
0.2635 mL |
1.3177 mL |
2.6354 mL |
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