MSX-122 is a novel small molecule and partial CXCR4 antagonist, with potent inhibition of CXCR4/CXCL12 actions (IC50 = 10 nM). MSX-122 blocks invasion and angiogenesis in vitro. MSX-122 attenuates colonic damage in mice with experimental colitis. MSX-122 blocks metastasis in an experimental animal model of breast cancer metastasis.
|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 mM|
Development of a unique small molecule modulator of CXCR4.
Liang Z, et al. PLoS One. 2012;7(4):e34038. PMID: 22485156.
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