MK-0429

CAS No. 227963-15-7

MK-0429( MK0429 )

Catalog No. M13624 CAS No. 227963-15-7

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

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
50MG 1674 In Stock
100MG 2502 In Stock
200MG Get Quote In Stock
500MG Get Quote In Stock
1G Get Quote In Stock

Biological Information

  • Product Name
    MK-0429
  • Note
    Research use only, not for human use.
  • Brief Description
    MK-0429 is a potent, selective, orally-active nonpeptide αvβ3 integrin inhibitor with IC50 of 0.08 nM in SPAV3 assay.
  • Description
    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.
  • In Vitro
    ——
  • 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. 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.
  • Synonyms
    MK0429
  • Pathway
    Cell Cycle/DNA Damage
  • Target
    Integrin
  • Recptor
    Integrin
  • Research Area
    Cancer
  • Indication
    Prostate Cancer

Chemical Information

  • CAS Number
    227963-15-7
  • Formula Weight
    439.51
  • Molecular Formula
    C23H29N5O4
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO : 250 mg/mL 568.82 mM
  • SMILES
    O=C(O)C[C@@H](C1=CC=C(OC)N=C1)N2CCN(CCCC3=NC4=C(CCCN4)C=C3)C2=O
  • Chemical 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

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Hutchinson JH, et al. J Med Chem. 2003 Oct 23;46(22):4790-8. 2. Pickarski M, et al. Oncol Rep. 2015 Jun;33(6):2737-45. 3. Zhou X, et al. Pharmacol Res Perspect. 2017 Oct;5(5).
molnova catalog
related products
  • Echistatin, α1 isofo...

    Potent irreversible αVβ3 integrin antagonist (Ki = 0.27 nM). Disrupts attachment of osteoclasts to bone and inhibits bone reabsorption (IC50 = 0.1 nM). Prevents ADP-induced platelet aggregation via inhibition of glycoprotein IIb/IIIa (GpIIb/IIIa, αIIbβ3) receptors (IC50 = 30 nM) in vitro.

  • Abrilumab

    Abrilumab (MEDI-7183) is a fully human monoclonal antibody against α4β7 that inhibits the α4β7 integrin and can be used to study inflammatory bowel disease and ulcerative colitis.

  • Lifitegrast

    A potent LFA-1/ICAM-1 antagonist with IC50 of 9 nM in HuT78 cells; exhibits good in vitro safety profile and low potency on CYP3A4, CYP2C9 and hERG.