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Brivanib alaninate（BMS-582664） CAS NO.649735-46-6
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- Min.Order: 100 Gram
- Payment Terms: L/C
- Available Specifications:
≥98.0%(100-500)Gram≥98.0%(1000-5000)Gram
- Product Details
Keywords
- Brivanib alaninate
- BMS-582664，1-[[4-[(4-Fluoro-2-methyl-1H-indol-5-yl)oxy]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]oxy]-2-propanol;Brivanib;Tyrosine Kinase Inhibitor;(R)-1-(4-(4-Fluoro-2-methyl-1H-indol-5-yloxy)-5-me
- 649735-46-6
Quick Details
- ProName: Brivanib alaninate（BMS-582664）
- CasNo: 649735-46-6
- Molecular Formula: C19H19FN4O3
- Appearance: off white powder
- Application: CAS：649735-46-6； 1-[[4-[(4-Fluoro-2-m...
- DeliveryTime: 2 months
- PackAge: 10g,100g,500g
- Port: shang hai
- ProductionCapacity: 100 Metric Ton/Week
- Purity: 98%
- Storage: Dry seal
- Transportation: shipping
- LimitNum: 100 Gram
Superiority
We are committed to provide excellence in researching, manufacturing and drug discovery process.
Our research team of scientists consists of western-trained Ph.D.s with experience and capabilities in drug R&D methodologies and medicinal chemistry.
Details
Brivanib(BMS540215) is an ATP-competitive inhibitor against VEGFR2 with IC50 of 25 nM, moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β.
IC50 value: 25 nM
Target: VEGFR2
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 [1].
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].