CS-1273

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 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

CS-1273 用途与合成方法

EG00229 是一种神经纤维蛋白 1 受体 (NRP1) 拮抗剂。EG00229 选择性抑制 VEGF-A 与 NRP1 b1 域的结合, IC50 为 3μM,但对 VEGFA 与 VEGFR-1 和 VEGFR-2 的结合没有影响。

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

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/04/30HY-10799EG002291 mg636元
2024/04/30HY-10799CS-1273
EG00229
1210945-69-95mg1400元

CS-1273 上下游产品信息

"CS-1273"相关产品信息
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