MK-0429 is a potent and selective inhibitor of the αvβ3 integrin, which showed therapeutic effects on bone turnover disease in men with hormone-refractory prostate cancer (HRPC) and bone metastases. MK-0429 was safe and efficacious in significantly decreasing melanoma metastasis in the lungs. MK-0429 may be useful for the prevention of metastatic melanoma.

CAS 227963-15-7 MFCD27963157

化学结构图

227963-15-7
SMILES: COc1ccc([C@H](CC(=O)O)N2CCN(CCCc3ccc4c(n3)NCCC4)C2=O)cn1

化学属性

Mol. Weight439.51
Appearance white solid powder
SolubilitySoluble in DMSO, not in water

别名和识别编码

Chemical NameMK-0429 is a potent and selective inhibitor of the αvβ3 integrin, which showed therapeutic effects on bone turnover disease in men with hormone-refractory prostate cancer (HRPC) and bone metastases. MK-0429 was safe and efficacious in significantly decreasing melanoma metastasis in the lungs. MK-0429 may be useful for the prevention of metastatic melanoma.
FormulaC23H29N5O4
Synonym MK-0429; MK 0429; MK0429; L-000845704; L 000845704; L000845704.
IUPAC Name(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
InChIKeyHGFOOLONGOBCMP-IBGZPJMESA-N
InChIInChI=1S/C23H29N5O4/c1-32-20-9-7-17(15-25-20)19(14-21(29)30)28-13-12-27(23(28)31)11-3-5-18-8-6-16-4-2-10-24-22(16)26-18/h6-9,15,19H,2-5,10-14H2,1H3,(H,24,26)(H,29,30)/t19-/m0/s1
Canonical SMILESO=C(O)C[C@@H](C1=CC=C(OC)N=C1)N2CCN(CCCC3=NC4=C(CCCN4)C=C3)C2=O
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产品应用

  • MK-0429 is a potent and selective inhibitor of the αvβ3 integrin, which showed therapeutic effects on bone turnover disease in men with hormone-refractory prostate cancer (HRPC) and bone metastases. MK-0429 was safe and efficacious in significantly decreasing melanoma metastasis in the lungs. MK-0429 may be useful for the prevention of metastatic melanoma.

相关文献及参考

  • [2]. Pickarski M, et al. Orally active αvβ3 integrin inhibitor MK-0429 reduces melanoma metastasis. Oncol Rep. 2015 Jun;33(6):2737-45.
  • [3]. Xiaoyan Zhou, et al. An integrin antagonist (MK-0429) decreases proteinuria and renal fibrosis in the ZSF1 rat diabetic nephropathy model. Pharmacol Res Perspect. 2017 Oct;5(5):e00354.
  • [1]. Hutchinson JH, et al. Nonpeptide alphavbeta3 antagonists. 8. In vitro and in vivo evaluation of a potent alphavbeta3 antagonist for the prevention and treatment of osteoporosis. J Med Chem. 2003 Oct 23;46(22):4790-8.
  • [1]. Hutchinson JH, et al. Nonpeptide alphavbeta3 antagonists. 8. In vitro and in vivo evaluation of a potent alphavbeta3 antagonist for the prevention and treatment of osteoporosis. J Med Chem. 2003 Oct 23;46(22):4790-8.
  • [2]. Pickarski M, et al. Orally active αvβ3 integrin inhibitor MK-0429 reduces melanoma metastasis. Oncol Rep. 2015 Jun;33(6):2737-45.
  • [3]. Xiaoyan Zhou, et al. An integrin antagon

安全信息

Storage condition Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

系列性分类


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