Brivanib alaninate |
(S)-((R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[1,2-f][1,2,4]triazin-6-yloxy)propan-2-yl) 2-aminopropanoate |
(CAS 649735-63-7) |
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Description: |
Brivanib alaninate(BMS582664) 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].
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Product No. |
KT20013 |
Product Name |
Brivanib alaninate |
Synonyms |
BMS-582664; BMS 582664; BMS582664 |
Formal Name |
(S)-((R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[1,2-f][1,2,4]triazin-6-yloxy)propan-2-yl) 2-aminopropanoate |
CAS Number |
649735-63-7 |
Molecular Formula |
C22H24FN5O4 |
Formula Weight |
441.46 |
Formulation |
A crystalline solid |
Purity |
98%min |
Stability |
1 year |
Storage |
-20°C |
Shipping |
USD45 for Europe and USA. No shipping charge once amount reach USD500. |
Quality Control |
HNMR,CNMR,LCMS,HPLC,IR,etc. |
Price & Availability |
In Stock. Price Negotiated. |
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