OTX008
| 中文名称 | OTX008 |
|---|---|
| 中文同义词 | 化合物OTX008;2,2',2'',2'''-(1,3,5,7(1,3)-四苯环辛烷-12,32,52,72-四基四(氧基))四(N-(2-(二甲基氨基)乙基)乙酰胺);2,2',2'',2'''-(1,3,5,7(1,3)-四苯环辛烷-12,32,52,72-四基四(氧基))四(N-(2-(二甲基氨基)乙基)乙酰胺) |
| 英文名称 | OTX 008 |
| 英文同义词 | OTX008 (Calixarene 0118;OTX008 (Synonyms: Calixarene 0118;Calix[4]arene compound 0118;Calixarene 0118;PTX 008;Acetamide, 2,2',2'',2'''-[pentacyclo[19.3.1.13,7.19,13.115,19]octacosa-1(25),3,5,7(28),9,11,13(27),15,17,19(26),21,23-dodecaene-25,26,27,28-tetrayltetrakis(oxy)]tetrakis[N-[2-(dimethylamino)ethyl]-;2,2',2'',2'''-(1,3,5,7(1,3)-Tetrabenzenacyclooctaphane-12,32,52,72-tetrayltetrakis(oxy))tetrakis(N-(2-(dimethylamino)ethyl)acetamide);PTX 008,OTX 008,Galectin,Calixarene0118,PTX-008,inhibit,OTX008,Calixarene-0118,OTX-008,Inhibitor |
| CAS号 | 286936-40-1 |
| 分子式 | C52H72N8O8 |
| 分子量 | 937.18 |
| EINECS号 | |
| 相关类别 | 抑制剂 |
| Mol文件 | 286936-40-1.mol |
| 结构式 |  |
OTX008 性质
| 沸点 | 1143.4±65.0 °C(Predicted) |
|---|---|
| 密度 | 1.155±0.06 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | DMF：1mg/mL； DMSO：2mg/mL；乙醇：5mg/mL； PBS（pH 7.2）：0.5 mg/mL |
| 形态 | 结晶固体 |
| 酸度系数(pKa) | 13.84±0.46(Predicted) |
| 颜色 | 白色至米白色 |
| Target | Value |
|
galectin-1
() |
Growth inhibitory concentrations (GI 50 ) of OTX008 in a large panel of human solid tumour cell lines ranges from 3 to 500 μM. A significant correlation between OTX008 GI 50 values and Gal1 mRNA (LGALS1) and protein expression levels in the panel of cancer cells is observed. In SQ20B and A2780-1A9 cells, OTX008 inhibits Gal1 expression and ERK1/2 and AKT-dependent survival pathways, and induces G2/M cell cycle arrest through CDK1. OTX008 enhances the anti-proliferative effects of Semaphorin-3A (Sema3A) in SQ20B cells and reverses invasion induced by exogenous Gal1. OTX008 affects endothelial cell proliferation, motility, invasiveness, and cord formation. Tumor cell proliferation is also inhibited, with differences in sensitivity among cell lines (IC 50 from 1 to 190 μM).
OTX008 inhibits growth of A2780-1A9 xenografts. OTX008 treatment is associated with down-regulation of Gal1 and Ki67 in treated tumours, as well as decreased microvessel density and VEGFR2 expression. Finally, combination studies show OTX008 synergy with several cytotoxic and targeted therapies, principally when OTX008 is administered first.
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/08/19 | S6949 | OTX008 OTX008 | 286936-40-1 | 5mg | 1941.21元 |
| 2024/08/19 | S6949 | OTX008 OTX008 | 286936-40-1 | 25mg | 5872.45元 |