MK-0429 (L-000845704) is an orally active, potent, selective and nonpeptide pan-integrin antagonist with IC 50 values of 1.6 nM, 2.8 nM, 0.1 nM, 0.7 nM, 0.5 nM and 12.2 nM for αvβ1 , αvβ3 , αvβ5 , αvβ6 , αvβ8 and α5β1 , respectively .
In Vivo
MK-0429 (100 or 300 mg/kg, p.o., twice daily b.i.d., 2 weeks) reduces metastatic tumor colony formation and area in the lungs. MK-0429 is safe and efficacious in significantly decreasing melanoma metastasis in the lungs . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: B6D2F1 hybrid female miceDosage: 100 or 300 mg/kg Administration: P.o., twice daily (b.i.d.), 2 weeks Result: MK-0429 at 100 and 300 mg/kg reduced the number of metastatic tumor colonies by 64 and 57%, respectively, and the high dose also reduced the tumor area by 60% as compared to the vehicle.
