Brivanib

SKU: orb1689660

Description

Brivanib (BMS-540215) is a potent, ATP-competitive VEGFR2 inhibitor (IC50=25 nM) with additional activity against VEGFR-1 and FGFR-1, but significantly less potency against PDGFR-β. This investigational compound has been evaluated in Phase 3 clinical trials for oncology research, supporting its use in both in vitro and in vivo studies of angiogenesis and tumor growth.

Research Area

Cardiovascular Research, Cell Biology, Signal Transduction

Key Properties

• CAS Number: 649735-46-6
• MW: 370.38
• Purity: 98.87%
• Formula: C₁₉H₁₉FN₄O₃
• SMILES: C[C@@H](O)COc1cn2ncnc(Oc3ccc4[nH]c(C)cc4c3F)c2c1C
• Target: Autophagy,FGFR,VEGFR,EGFR
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.4 mM);H2O:<1 mg/mL;Ethanol:3 mg/mL (8.1 mM);DMSO:69 mg/mL (186.3 mM)

Bioactivity

• Target IC50:
  VEGFR2:25 nM
• In Vivo:
  Brivanib exhibits antitumor activity in H3396 xenografts in athymic mice, completely inhibiting tumor growth at 60 and 90 mg/kg (p.o.) with TGIs of 85% and 97%, respectively . It also significantly suppresses tumor growth in Hepatocellular carcinoma (HCC) xenografts by decreasing VEGFR2 phosphorylation, resulting in tumor weights of 55% and 13% compared to controls at doses of 50 mg/kg and 100 mg/kg. Brivanib shows potential for efficient treatment of HCC .
• In Vitro:
  Brivanib also inhibits VEGFR1 and FGFR-1 with IC50 of 0.38 μM and 0.148 μM. Brivanib is not sensitive to PDGFRβ, EGFR, LCK, PKCα or JAK-3 with IC50 all above 1900 nM. Brivanib could inhibit the proliferation of VEGF-stimulated HUVECs with IC50 of 40 nM, compared to 276 nM in FGF-stimulated HUVECs. On the other hand, Brivanib exhibits low activity to tumor cell lines.
• Cell Research:
  The cells are stimulated by VEGF or FGF at a concentration of 8 or 80 ng/mL. These cells are seeded in 96 well plates at a density of 2 × 103 and incubated for 24 hours. Brivanib at various dilutions are added to the cells for another 48 hours. Then 0.5 μCi of [3H] thymidine is added for 24 hours. After that the incorporated tritium is quantified using a β-counter. (Only for Reference)

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

Autophagy, BMS 540215, BMS540215, BMS-540215, Brivanib, Inhibitor, EGFR, FGFR1, Flk1, inhibit, VEGFR2, VEGFR, VEGFR1, Vascular endothelial growth factor receptor

Compound Identifiers

PubChem CID

11234052