CXCL-CXCR1/2-IN-1
目录号 : GC74037CXCL-CXCR1/2-IN-1是一种口服活性ELR+CXCL-CXCR1/2通路抑制剂,CXCR2的EC50为42.7nM。
Cas No.:2415653-55-1
Sample solution is provided at 25 µL, 10mM.
CXCL-CXCR1/2-IN-1 is an orally active ELR+CXCL-CXCR1/2 pathway inhibitor with an EC50 of 42.7 nM for CXCR2. CXCL-CXCR1/2-IN-1 shows anticancer and antiangiogenic effects.
In renal cell carcinoma (RCC) cell lines (A498, RCC4, 786, and Sunitinib-resistant RCC cell line 786-R) and neck squamous cell carcinoma (HNSCC) cell lines (CAL33, CAL27, Cisplatin- and radiotherapy-resistant cell lines CAL33RR and CAL27RR), CXCL-CXCR1/2-IN-1 (compound 10) shows IC50 values of 2 μM, 2 μM, 2.5 μM, 2 μM, 3 μM, 4 μM, 4 μM, 2.5 μM, and 2.5 μM against A498, RCC4, 786, 786-R, CAL33, CAL27, CAL33RR, and CAL27RR, respectively[1].CXCL-CXCR1/2-IN-1 inhibits the migration of A498 cancer cells in vitro[1]. CXCL-CXCR1/2-IN-1 (1-2.5 μM; 24-48 h) shows a reduction in the phosphorylation of ERK and AKT in A498 cells. CXCL-CXCR1/2-IN-1 also exhibits the capability to inhibit the secretion of CXCL1, CXCL5, and CXCL8, which are representative proangiogenic ELR+CXCL cytokines[1].
CXCL-CXCR1/2-IN-1 (1 μM; 48 h) reduces metastasis area in zebrafish embryos injected with A498 cells[1].CXCL-CXCR1/2-IN-1 (100 mg/kg; oral gavage; twice a day; for 28 days) inhibits tumor growth in mice[1].
References:
[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.
Cas No. | 2415653-55-1 | SDF | |
分子式 | C14H8Cl2N4O3S | 分子量 | 383.21 |
溶解度 | DMSO : 4.17 mg/mL (10.88 mM; ultrasonic and warming and heat to 60°C) | 储存条件 | -20°C |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
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1 mg | 5 mg | 10 mg | |
1 mM | 2.6095 mL | 13.0477 mL | 26.0954 mL |
5 mM | 0.5219 mL | 2.6095 mL | 5.2191 mL |
10 mM | 0.261 mL | 1.3048 mL | 2.6095 mL |
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给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
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1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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