Efaproxiral sodium 是血红蛋白 (Hb) 合成变构调节剂,能够减少血红蛋白氧 (O2) 的结合亲和力。
产品描述
Efaproxiral Sodium , a synthetic allosteric modifier of hemoglobin, is utilized for brain metastases originating from breast cancer.
体外活性
Efaproxiral, a synthetic allosteric modi?er of hemoglobinoxygen binding af?nity, has been shown to bind reversibly to hemoglobin, stabilizing the deoxyhemoglobin tetramer conformation to reduce its af?nity for oxygen. [1]
体内活性
Efaproxiral plus oxygen breathing reduces the radiobiological hypoxic fraction of EMT6 tumors from the value of 24% found in both air-breathing and oxygen-breathing mice to 9% and improves the response of the tumors to radiation. Carboplatin (100 mg/kg) slowes tumor growth in air-breathing mice, producing a growth delay of 3.3 days. Efaproxiral plus oxygen increases the growth delay to 5.7 days; this is 2.4 days (71%) greater than that for carboplatin alone and 2.1 days (57%) greater than that for carboplatin plus oxygen breathing. Efaproxiral plus oxygen breathing, therefore, improves the tumor growth delay obtained with 100 mg/kg carboplatin to or beyond that obtained with the highly toxic dose of 150 mg/kg carboplatin, but does so without increasing the toxicity beyond that seen with 100 mg/kg carboplatin in air-breathing mice.[1] Efaproxiral significantly increases tumor oxygenation by 8.4 to 43.4 mmHg within 5 days in C3H mice with RIF-1 tumors, with maximum increases at 22-31 min after treatment. Efaproxiral plus oxygen plus Radiation produces tumor growth inhibition throughout the treatment duration in C3H mice with RIF-1 tumors, and inhibition is significantly different from radiation plus oxygen from day 3 to day 5. [2]
Cas No.
170787-99-2
分子式
C20H22NNaO4
分子量
363.389
别名
RSR13 sodium;乙丙昔罗钠
储存和溶解度
H2O:67 mg/mL (184.4 mM)
Ethanol:68 mg/mL (187.1 mM)
DMSO:68 mg/mL (187.1 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years