CS-1273

生物活性靶点体外研究体内研究 CS-1273 试剂级价格

CS-1273

CAS号:1210945-69-9
英文名:EG00229
中文名:CS-1273
CBNumber:CB02627791
分子式:C19H20F3N7O7S3
分子量:611.59
MOL File:1210945-69-9.mol

CS-1273化学性质

储存条件 :Store at -20°C
溶解度 :Soluble in DMSO
形态 :Powder
颜色 :Light yellow to yellow

CS-1273性质、用途与生产工艺

生物活性 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。
靶点

IC50: 8 μM ( ¹²⁵ I-VEGF-A binding to PAE/NRP1); 3 μM (bt-VEGF-A binding to purified NRP1 b1 domain).

体外研究

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.

体内研究

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.