CS-1273
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- CAS号:
- 1210945-69-9
- 英文名:
- EG00229
- 英文别名:
- CS-1273;EG00229;EG00229 TFA;EG00229,EG-00229;EG 00229 Trifluoroacetate;EG 00229 (trifluoroacetate salt)
- 中文名:
- CS-1273
- 中文别名:
- 化合物 T11153;EG 00229 三氟乙酸盐
- CBNumber:
- CB02627791
- 分子式:
- C19H20F3N7O7S3
- 分子量:
- 611.59
- MOL File:
- 1210945-69-9.mol
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CS-1273化学性质
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储存条件:
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Store at -20°C
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溶解度:
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Soluble in DMSO
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形态:
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Powder
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CS-1273性质、用途与生产工艺
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
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Cell Line:
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A549 cells
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Concentration:
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0 µM, 10 μM, 30 μM, 100 μM
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Incubation Time:
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48 hours
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Result:
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Caused a significant reduction in cell viability.
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EG00229 (0-10 mg/kg; intraperitoneal injection; three times per week; for 4 weeks; NSG mice) treatment substantially reduces tumor growth and visible vascularization.
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Animal Model:
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6-week old female NOD scid IL2 receptor gamma chain knockout mice (NSG mice) with ECS cells
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Dosage:
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0 mg/kg, 10 mg/kg
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Administration:
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Intraperitoneal injection; three times per week; for 4 weeks
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Result:
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Reduces tumor growth and visible vascularization.
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CS-1273
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/01/25 | HY-10799 | EG00229 | | 1 mg | 636元 |
| 2024/01/25 | HY-10799 | CS-1273
EG00229 | 1210945-69-9 | 5mg | 1400元 |
1210945-69-9, CS-1273 相关搜索:
- 酶
- C19H20F3N7O7S3
- EG 00229 三氟乙酸盐
- 化合物 T11153
- 1210945-69-9
- EG 00229 (trifluoroacetate salt)
- EG00229,EG-00229
- CS-1273
- EG 00229 Trifluoroacetate
- EG00229 TFA
- EG00229