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Brivanib

Cat. No. M1688
Brivanib Structure
Synonym:

BMS-540215

Size Price Availability Quantity
10mg USD 180 In stock
50mg USD 600 In stock
100mg USD 980 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Brivanib (BMS-540215) is an ATP-competitive inhibitor of human VEGFR -2, with an IC50 of 25 nmol/L and Ki of 26 nmol/L. Brivanib is currently in development for the treatment of hepatocellular and colon carcinomas. In vitro and in vivo studies were conducted to characterize the preclinical pharmacokinetics and disposition of brivanib and brivanib alaninate, and antitumor efficacy in mice bearing human xenografts.

Protocol
Cell Experiment
Cell lines VEGF or FGF stimulated HUVECs
Preparation method 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.
Concentrations ~ 10 μM
Incubation time 48 hours
Animal Experiment
Animal models H3396 xenografts in athymic mice
Formulation Dissolved in PEG400: Tween80 (75:25) (orally) or PEG400: water (3:2) (intravenously)
Dosages 60 mg/kg (orally) or 10 mg/kg (intravenously)
Administration oral or i.v.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 370.38
Formula C19H19FN4O3
CAS Number 649735-46-6
Purity >99%
Solubility DMSO
Storage at -20°C
Customer Product Validations & Biological Datas
Source AJR Am J Roentgenol (2014). Figure 3. Brivanib
Method DCE-MRI
Cell Lines HepG2 cells
Concentrations 0.01 mL/g
Incubation Time 14 d
Results In the brivanib-treated group, the Ktrans and ve values decreased statistically significantly between baseline and 7 days after treatment (p = 0.024 and p = 0.031, respectively), and between baseline and 14 days after treatment (p = 0.043 and p = 0.018), and did not show statistically significant changes between 7 days and 14 days (p = 0.302 and p = 1, respectively).
Rating
Source AJR Am J Roentgenol (2014). Figure 2. Brivanib
Method DCE-MRI
Cell Lines HepG2 cells
Concentrations 0.01 mL/g
Incubation Time 14 d
Results The mean MVD in the tumors that were treated with vehicle and brivanib was approximately 55.2 ± 9.5 vessels/field and 40.8 ± 17.3 vessels/field, respectively (Fig. 2).
Rating
References

Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor.
Bhide RS, et al. J Med Chem. 2006 Apr 6;49(7):2143-6. PMID: 16570908.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Brivanib, BMS-540215 supplier, VEGFR/PDGFR, inhibitors

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