(Rac)-SAR131675

SKU: orb1303891

Description

SAR131675 is a highly specific VEGFR-3 tyrosine kinase inhibitor with in vitro IC50 values of 20 nM and 45 nM for kinase activity and autophosphorylation, respectively. Its in vivo antitumor and antimetastatic effects are mediated through the inhibition of lymphangiogenesis and tumor-associated macrophage invasion.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1092539-44-0
• MW: 358.39
• Purity: 99.10% (May vary between batches)
• Formula: C₁₈H₂₂N₄O₄
• SMILES: CCn1c(N)c(C(=O)NC)c(=O)c2ccc(nc12)C#C[C@@](C)(O)COC
• Target: VEGFR
• Solubility: DMSO:Slightly soluble

Bioactivity

• Target IC50:
  VEGFR3:20 nmol/L|VEGFR3:45 nmol/L
• In Vitro:
  SAR131675 dose dependently inhibits the proliferation of primary human lymphatic cells, induced by the VEGFR-3 ligands VEGFC and VEGFD, with an IC50 of about 20 nM. SAR131675 dose dependently inhibits rh-VEGFR-3–TK activity with an IC50 of 23 nM. SAR131675 inhibits VEGR-3–TK activity with a Ki of about 12 nM. SAR131675 inhibits VEGFR-1–TK activity with an IC50 of > 3 μM and VEGFR-2–TK activity with an IC50 of 235 nM. SAR131675 inhibits VEGFR-1 autophosphorylation with an IC50 of about 1 μM and VEGFR-2 with an IC50 of about 280 nM. SAR131675 moderately inhibits VEGFR-2 and has very little effect on VEGFR-1, showing a good selectivity for VEGFR-3. SAR131675 inhibits VEGFA-induced VEGFR-2 phosphorylation in a dose-dependent manner, with an IC50 of 239 nM. SAR131675 potently inhibits lymphatic cell survival induced by VEGFC and VEGFD with IC50 of 14 nM and 17 nM, respectively. SAR131675 inhibits VEGFA-induced survival with an IC50 of 664 nM. SAR131675, significantly and dose dependently inhibits VEGFC-induced Erk phosphorylation, with an IC50 of about 30 nM.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, inhibit, (Rac) SAR131675, (Rac)SAR131675, (Rac)-SAR131675, (Rac)-SAR-131675, SAR131675, SAR-131675, SAR 131675, selective, potent, racemate, Vascular endothelial growth factor receptor, VEGFR3, VEGFR

Compound Identifiers

PubChem CID

71295845