BrivanibAn ATP-competitive inhibitor against VEGFR-2, Flk-1, VEGFR-1 and FGFR-1

Brivanib (CAS 649735-46-6)

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Synonym: (2R)-1-[4-(4-Fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4 ]triazin-6-yloxy]propanol
Application: An ATP-competitive inhibitor against VEGFR-2, Flk-1, VEGFR-1 and FGFR-1
CAS Number: 649735-46-6
Molecular Weight: 370.38
Molecular Formula: C19H19FN4O3
* Refer to Certificate of Analysis for lot specific data (including water content).
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Brivanib is an ATP-competitive inhibitor against human Flk-1 (VEGFR-2) and mouse Flk-1 with IC50 of 25 nM and 89 nM, respectively. Brivanib also inhibits Flt-1 (VEGFR-1) and Flg (FGFR-1) with IC50 of 0.38 and 0.148 μM. Brivanib displays antitumor activities in H3396 xenograft. This compound completely inhibits the tumor growth, with TGI of 85% and 97%, respectively.

Physical State :
Solid
Solubility :
Soluble in DMSO (74 mg/ml at 25 °C), water (<1 mg/ml at 25 °C), and ethanol (3 mg/ml at 25 °C).
Storage :
Store at -20° C
Melting Point :
227.09 °C (Predicted)
Boiling Point :
531.02 °C (Predicted)
Density :
~1.4 g/cm3 (Predicted)
Refractive Index :
n20D 1.66 (Predicted)
IC50 :
Flk-1: IC50 = 25 nM (human); Flk-1: IC50 = 89 nM (mouse); Flg: IC50 = 148 nM (human); Flt-1: IC50 = 380 nM (human); mTORC2: IC50 >1.9 µM (human)
Ki Data :
Flk-1: Ki= 26 nM (human); Vascular endothelial growth factor receptor 2: Ki= 28 nM (mouse); Flt-1: Ki= 60 nM (human)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
11234052
MDL Number :
MFCD13194684
SMILES :
CC1=CC2=C(N1)C=CC(=C2F)OC3=NC=NN4C3=C(C(=C4)OC[C@@H](C)O)C

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Certificate of Analysis

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