规格 | 价格 | |
---|---|---|
500mg | ||
1g | ||
Other Sizes |
体外研究 (In Vitro) |
BGC0222 (72 h) 对 HT29、MIA PaCa-2 和 MCF-7 肿瘤细胞表现出优于伊立替康和 NKTR-102 的抗增殖活性,IC50 值分别为 1.83 μM、3.95 μM 和 0.68 μM[1]。BGC0222 (40 μM) 表现出良好的血管生成活性,血管长度可达 1930 mm(CAM 血管生成测定)[1]。
|
---|---|
体内研究 (In Vivo) |
BGC0222(20-60 mg/kg,静脉注射,每4天一次或每周一次,共3次)在HT-29、MIA PaCa-2、NCI-H446、U-87 MG和MDA-MB-231异种移植裸鼠中表现出明显的抗增殖活性,其RTV和T/C值均低于伊立替康[1]。BGC0222(30-90 mg/kg,静脉注射,每周一次,共28天)在Sprague-Dawley大鼠中表现出比伊立替康更好的安全性,其最大耐受剂量(MTD)分别为90 mg/kg和小于60 mg/kg[1]。BGC0222(20-80 mg/kg,单次静脉注射)在Sprague-Dawley大鼠体内缓慢而稳定地释放伊立替康[1]。
|
动物实验 |
Animal/Disease Models: HT-29, MIA PaCa-2, NCI-H446, U-87 MG and MDA-MB-231 xenograft female Balb/c nude mice (HT-29, 4 × 106; MIA PaCa-2, 5 × 106; NCI-H446, 8 × 106; U-87 MG,4 × 106; MDA-MB-231, 3 × 106)[1]
Doses: 20 mg/kg (MIA PaCa-2, NCI-H446, MDA-MB-231); 40 mg/kg (HT-29); 60 mg/kg (U-87 MG) Route of Administration: Intravenous injection (i.v.), every 4 days (HT-29 and MDA-MB-231) or once a week (MIA PaCa-2, NCI-H446 and U-87 MG), 3 times Experimental Results: Exhibited remarkable antiproliferation activity in the HT-29, MIA PaCa-2, NCI-H446, U-87 MG and MDA-MB-231 xenograft nude mice. Exhibited that T/C values of BGC0222 for days 12, 15, 18, 22, 25, 29 and 32 were determined to be 100%, 88.8%, 57.0%, 27.6%, 16.9%, 9.87% and 9.21%, while that of irinotecan were found to be 100%, 103%, 93.1%, 75.1%, 68.8%, 60.6%, 71.1% in the HT-29 xenograft nude mice, respectively. Showed that the RTV values of BGC0222 were much lower than that of irinotecan and NKTR-102 when the average tumor size reached approximately 100–300 mm3 (after day 12) in the HT-29 xenograft nude mice. |
参考文献 |
分子式 |
C1241H2276N64O552
|
---|---|
分子量 |
26927.36
|
运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 0.0371 mL | 0.1857 mL | 0.3714 mL | |
5 mM | 0.0074 mL | 0.0371 mL | 0.0743 mL | |
10 mM | 0.0037 mL | 0.0186 mL | 0.0371 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
计算结果:
工作液浓度: mg/mL;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。