MK-0429

Research use only, not for human use.

MK-0429 is a potent, selective, orally-active nonpeptide αvβ3 integrin inhibitor with IC50 of 0.08 nM in SPAV3 assay.

MK-0429 is a potent, selective, orally-active nonpeptide αvβ3 integrin inhibitor with IC50 of 0.08 nM in SPAV3 assay; displays approximately 100-fold selectivity for αvβ3 over αvβ5 (IC50=10 nM), and no significant activity for the fibrinogen receptor αIIBβ3 (IC50>30 uM); shows activity in different animal models of bone turnover and has potentiation for the prevention and treatment of osteoporosis; also reduces melanoma metastasis both in vitro and in vivo.Prostate Cancer Phase 1 Discontinued.

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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. Animal Model:B6D2F1 hybrid female mice Dosage: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.

MK0429

Cell Cycle/DNA Damage

Integrin

Integrin

Cancer

Prostate Cancer

227963-15-7

439.51

C23H29N5O4

>98% (HPLC)

DMSO : 250 mg/mL 568.82 mM

O=C(O)C[C@@H](C1=CC=C(OC)N=C1)N2CCN(CCCC3=NC4=C(CCCN4)C=C3)C2=O

(S)-3-(6-methoxypyridin-3-yl)-3-(2-oxo-3-(3-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)propyl)imidazolidin-1-yl)propanoic acid

(-20℃)

With Ice Pack

≥ 2 years