WZ811 is a highly potent competitive antagonist of CXCR4. WZ811 shows subnanomolar potency (EC50 = 0.3 nM) in an affinity binding assay. WZ811 inhibits CXCR4/stromal cell-derived factor-1 (SDF-1)-mediated modulation of cyclic adenosine monophophate (cAMP) levels (EC50 = 1.2 nM). In addition, WZ811 efficiently inhibits SDF-1 induced Matrigel invasion (EC50 = 5.2 nM).
|Source||PLoS One (2017). Figure 2. WZ 811|
|Cell Lines||U87.CD4.CXCR4 cells|
|Results||100 μMof CTCE-9908, WZ811 and Me6TREN did not affect the calcium flux evoked by CXCL12 (IC50s >100,000 nM)|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO 10 mg/mL|
Dipyrimidine amines: a novel class of chemokine receptor type 4 antagonists with high specificity.
Zhu A, et al. J Med Chem. 2010 Dec 23;53(24):8556-68. PMID: 21105715.
Discovery of small molecule CXCR4 antagonists.
Zhan W, et al. J Med Chem. 2007 Nov 15;50(23):5655-64. PMID: 17958344.
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