1. Protein Tyrosine Kinase/RTK
    Autophagy
  2. VEGFR
    Autophagy

Brivanib (Synonyms: BMS-540215)

Cat. No.: HY-10337 Purity: 99.63%
Data Sheet SDS Handling Instructions

Brivanib is an ATP-competitive inhibitor against VEGFR2 with IC50 of 25 nM, abd has moderate potency against VEGFR-1 and FGFR-1, but > 240-fold against PDGFR-β.

For research use only. We do not sell to patients.
Brivanib Chemical Structure

Brivanib Chemical Structure

CAS No. : 649735-46-6

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $121 In-stock
5 mg $110 In-stock
10 mg $180 In-stock
50 mg $590 In-stock
100 mg $990 In-stock
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Other Forms of Brivanib:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Brivanib is an ATP-competitive inhibitor against VEGFR2 with IC50 of 25 nM, abd has moderate potency against VEGFR-1 and FGFR-1, but > 240-fold against PDGFR-β.

IC50 & Target

IC50: 25 nM (VEGFR2)

In Vitro

Brivanib 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[1]. Brivanib doses ≤20 µM paradoxically enhances FGF-induced LX-2 cell proliferation, whereas higher brivanib doses (≥30 µM) inhibits LX-2 cell proliferation. The inhibitory effect of brivanib on liver fibrosis is not through inhibition of TGF-β1-induced stellate cell activation, and is possibly through inhibition of PDGF-BB-induced stellate cell activation[3].

In Vivo

Brivanib displays antitumor activities in H3396 xenograft in athymic mice. At a dose of 60 and 90 mg/kg (p.o.), brivanib completely inhibits the tumor growth, with TGI of 85% and 97%, respectively[1]. Moreover, brivanib significantly suppresses tumor growth in Hepatocellular carcinoma (HCC) xenografts, which due to the decrease in phosphorylation of VEGFR2. The results show that the tumor weights in 06-0606 xenograft mice are 55% and 13%, compared with the controls at a dose of 50 mg/kg and 100 mg/kg. Brivanib is suggested to be efficient in treatment of HCC[2]. Brivanib (50 mg/kg, p.o.) attenuates liver fibrosis and stellate cell activation induced by BDL in mice. Brivanib inhibits growth factor and growth factor receptor mRNA expression in sham control animals but shows variable effects in bile duct ligated animals[3].

Clinical Trial
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References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.6999 mL 13.4996 mL 26.9993 mL
5 mM 0.5400 mL 2.6999 mL 5.3999 mL
10 mM 0.2700 mL 1.3500 mL 2.6999 mL
Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[3]

Viability is measured in LX-2 cells using the Cell Counting Kit-8 (CCK-8). Using 96-well plates with 2,000 cells per well, HSCs are incubated in 10% FBS-supplemented DMEM for 24 hours, followed by starvation in serum-free media. After 24 hours of starvation, brivanib is added at different doses. Two hours later, 5 ng/mL PDGF-BB is added. The cells are incubated for an additional 72 hours and cell viability is measured. Each experiment is performed in three replicates at least four times. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3]

Male mice 4-6 weeks of age are treated 3 times a week with a total of 12 intraperitoneal (i.p.) injections of 150 mL/kg TAA. At the onset of TAA treatment, placebo or brivanib (25 or 50 mg/kg) is administered orally on 5 consecutive days with weekend breaks. The animals are sacrificed 4 weeks after the start of the injections. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

370.38

Formula

C₁₉H₁₉FN₄O₃

CAS No.

649735-46-6

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 50 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Brivanib
Cat. No.:
HY-10337
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