Bioactivity | CXCL-CXCR1/2-IN-1 is an orally active ELR+CXCL-CXCR1/2 pathway inhibitor with an EC50 of 42.7 nM for CXCR2[1]. CXCL-CXCR1/2-IN-1 shows anticancer and antiangiogenic effects[1]. |
Invitro | CXCL-CXCR1/2-IN-1(1-2.5 μM;24-48 小时)显示 A498 细胞中 ERK 和 AKT 磷酸化减少。CXCL-CXCR1/2-IN-1 还具有抑制 CXCL1、CXCL5 和 CXCL8 分泌的能力,这些细胞因子是代表性的促血管生成 ELR+CXCL 细胞因子[1]。 在肾细胞癌 (RCC) 细胞系(A498、RCC4、786 和舒尼替尼耐药 RCC 细胞系 786-R)和颈部鳞状细胞癌 (HNSCC) 细胞系(CAL33、CAL27、顺铂和放疗耐药细胞系,CAL33RR 和 CAL27RR),CXCL-CXCR1/2-IN-1 (compound 10) 对 A498、RCC4、786、786-R、CAL33、CAL27、CAL33RR 和 CAL27RR 细胞的的 IC50 值分别为 2 μM、2 μM、2.5 μM、2 μM、3 μM、4 μM、4 μM、2.5 μM 和 2.5 μM[1]。 CXCL-CXCR1/2-IN-1 抑制 A498 癌细胞的体外迁移[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> CXCL-CXCR1/2-IN-1 相关抗体: Western Blot Analysis[1] Cell Line: |
In Vivo | CXCL-CXCR1/2-IN-1(1 μM;48 小时)可减少注射 A498 细胞的斑马鱼胚胎的转移面积[1]。 CXCL-CXCR1/2-IN-1(100 mg/kg;口服灌胃;每天两次;持续 28 天)抑制小鼠肿瘤生长[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
CAS | 2415653-55-1 |
Formula | C14H8Cl2N4O3S |
Molar Mass | 383.21 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Oleksandr Grytsai, et al. A Potent Solution for Tumor Growth and Angiogenesis Suppression via an ELR+CXCL-CXCR1/2 Pathway Inhibitor. ACS Med. Chem. Lett. April 3, 2024. |