MSX-122 是一种口服可用的部分 CXCR4 拮抗剂,抑制 CXCR4/CXCL12 相互作用的 IC50 约为 10 nM。MSX-122 具有抗炎和抗转移活性。
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产品名称 | CXCR1 ↓ ↑ | CXCR2 ↓ ↑ | CXCR4 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Reparixin | ✔ | 99%+ | |||||||||||||||||
SB225002 |
+++
CXCR2, IC50: 22 nM |
99%+ | |||||||||||||||||
Plerixafor |
++
CXCR4, IC50: 44 nM |
99% | |||||||||||||||||
AMD 3465 6HBr | ✔ | 98% | |||||||||||||||||
WZ811 |
++++
CXCR4, EC50: 0.3 nM |
98% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | MSX-122, a partial antagonist of CXCR4, impedes the CXCR4/CXCL12 interaction with an IC50 of approximately 10 nM. It does not affect cAMP reduction mediated by the ligands CCR3/CCL5 and CCR5/CCL5. At 100 nM, MSX-122 strongly inhibits the invasion of 78% of MDA-MB-231 cells but does not affect T-tropic HIV infection or show activity in calcium flux assays[1]. |
体内研究 | MSX-122 (10 mg/kg, i.p.) reduces inflammation caused by carrageenan and lung fibrosis from bleomycin in mice. At 4 mg/kg, i.p., daily, MSX-122 inhibits metastasis in a breast cancer metastasis animal model, and at 10 mg/kg i.p., daily, it significantly reduces hepatic micrometastases[1]. |
体外研究 | MSX-122, a partial antagonist of CXCR4, impedes the CXCR4/CXCL12 interaction with an IC50 of approximately 10 nM. It does not affect cAMP reduction mediated by the ligands CCR3/CCL5 and CCR5/CCL5. At 100 nM, MSX-122 strongly inhibits the invasion of 78% of MDA-MB-231 cells but does not affect T-tropic HIV infection or show activity in calcium flux assays[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.42mL 0.68mL 0.34mL |
17.10mL 3.42mL 1.71mL |
34.21mL 6.84mL 3.42mL |
CAS号 | 897657-95-3 |
分子式 | C16H16N6 |
分子量 | 292.338 |
别名 | Q-122 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Sealed in dry,2-8°C |
溶解度 |
DMSO: 3 mg/mL(10.26 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |