CS-1273
中文名称 | CS-1273 |
---|---|
中文同义词 | 化合物 T11153;EG 00229 三氟乙酸盐 |
英文名称 | EG00229 |
英文同义词 | EG00229;EG00229 TFA;EG 00229 Trifluoroacetate;CS-1273;EG00229,EG-00229;EG 00229 (trifluoroacetate salt) |
CAS号 | 1210945-69-9 |
分子式 | C19H20F3N7O7S3 |
分子量 | 611.59 |
EINECS号 | |
相关类别 | |
Mol文件 | 1210945-69-9.mol |
结构式 | ![]() |
CS-1273 性质
储存条件 | Store at -20°C |
---|---|
溶解度 | 溶于二甲基亚砜 |
形态 | 粉末 |
颜色 | 浅黄至黄色 |
IC50: 8 μM ( 125 I-VEGF-A binding to PAE/NRP1); 3 μM (bt-VEGF-A binding to purified NRP1 b1 domain).
EG00229 (Compound 2; 0-100 μM; 48 hours; A549 cells) treatment causes a significant reduction in cell viability over a 48 hours incubation.
EG00229 (Compound 2) demonstrates inhibition of VEGF-A binding to NRP1 and attenuates VEGFR2 phosphorylation in endothelial cells. Inhibition of migration of endothelial cells is also observed in HUVECs.
EG00229 (Compound 2) selectively inhibits radiolabeled
125
I-VEGF-A binding to porcine aortic endothelial (PAE)/NRP1, but not VEGFR2-expressing cells, with an
IC
50
of 8 μM. EG00229 also inhibits VEGF-A binding to lung carcinoma A549 and prostate carcinoma DU145 cells, which express NRP1, but not VEGFR1 and VEGFR2, with similar potency. Binding of VEGF-A to human umbilical vein endothelial cells (HUVECs), which express VEGFR2, VEGFR1, and NRP1, is also inhibited by EG00229 with an
IC
50
of 23 μM.
Cell Viability Assay
Cell Line: | A549 cells |
Concentration: | 0 µM, 10 μM, 30 μM, 100 μM |
Incubation Time: | 48 hours |
Result: | Caused a significant reduction in cell viability. |
EG00229 (0-10 mg/kg; intraperitoneal injection; three times per week; for 4 weeks; NSG mice) treatment substantially reduces tumor growth and visible vascularization.
Animal Model: | 6-week old female NOD scid IL2 receptor gamma chain knockout mice (NSG mice) with ECS cells |
Dosage: | 0 mg/kg, 10 mg/kg |
Administration: | Intraperitoneal injection; three times per week; for 4 weeks |
Result: | Reduces tumor growth and visible vascularization. |
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
---|---|---|---|---|---|
2024/04/30 | HY-10799 | EG00229 | 1 mg | 636元 | |
2024/04/30 | HY-10799 | CS-1273 EG00229 | 1210945-69-9 | 5mg | 1400元 |