Plerixafor

CXCR4拮抗剂(IC50s=0.02-0.13µg/ml)；对CXCR4的选择性优于CXCR1-3和CXCR5-9(IC50s=>25µg/ml)；降低慢性感染HIV-1(IIIB)的Jurkat细胞上清液中的传染性病毒含量(EC50=~0.02µg/ml)；动员小鼠和人类造血干细胞和小鼠长期再增殖细胞进行移植；增加小鼠血液、脾脏和中枢神经系统中的T细胞运输；以1.25mg/kg每天两次的剂量减少小鼠肺转移模型中肺中4T1小鼠乳腺癌细胞的数量。An antagonist of CXCR4 (IC50s = 0.02-0.13 µg/ml); selective for CXCR4 over CXCR1-3 and CXCR5-9 (IC50s = >25 µg/ml); decreases infectious virus content in the supernatant of Jurkat cells chronically infected with HIV-1(IIIB) (EC50 = ~0.02 µg/ml); mobilizes murine and human hematopoietic stem and murine long-term repopulating cells for transplantation; increases T cell trafficking in mouse blood, spleen, and central nervous system; decreases the number of 4T1 murine mammary carcinoma cells in the lung in a mouse model of lung metastasis at 1.25 mg/kg twice per day.分子式C28H54N8分子量502.8C1(CN2CCNCCCNCCNCCC2)=CC=C(CN3CCNCCCNCCNCCC3)C=C1