2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
生物活性
Description
In Vivo
In Vitro
化合物的使用
Kinase Assay
Cell Assay
Animal Administration
参考文献
A potent and selective antagonist of CXCR4 with IC50 of 13 nM in a CXCR4 125I-SDF inhibition binding assay; displays no significant activity (IC50>10 uM) for a series of other closely GPCRs (CCR1, CCR2b, CCR4, CCR5, CXCR1, and CXCR2); inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with IC50 of 2 nM and 26 nM, respectively, with noncytotoxic to cells (>23 uM); exhibits good PK profiles and excellent oral bioavailability; also inhibits CXCR4/SDF-1-mediated events in ALL cancer cells and transplant models.HIV InfectionPhase 3 Clinical
