For research use only. Not for therapeutic Use.
BIBF 1202 is the carboxylate metabolite of BIBF 1120 which inhibits VEGFR2 kinase with an IC50 of 62 nM.
The major metabolic pathway for BIBF 1120 is methyl ester cleavage to BIBF 1202. Subsequently, the free carboxyl group of BIBF 1202 is glucuronidated to 1-O-acylglucuronide[2].
| Catalog Number | I005355 |
| CAS Number | 894783-71-2 |
| Synonyms | 2-hydroxy-3-[N-[4-[methyl-[2-(4-methylpiperazin-1-yl)acetyl]amino]phenyl]-C-phenylcarbonimidoyl]-1H-indole-6-carboxylic acid |
| Molecular Formula | C30H31N5O4 |
| Purity | ≥95% |
| InChI | InChI=1S/C30H31N5O4/c1-33-14-16-35(17-15-33)19-26(36)34(2)23-11-9-22(10-12-23)31-28(20-6-4-3-5-7-20)27-24-13-8-21(30(38)39)18-25(24)32-29(27)37/h3-13,18,32,37H,14-17,19H2,1-2H3,(H,38,39) |
| InChIKey | SDJMWYVJAVLZEG-UHFFFAOYSA-N |
| SMILES | CN1CCN(CC1)CC(=O)N(C)C2=CC=C(C=C2)N=C(C3=CC=CC=C3)C4=C(NC5=C4C=CC(=C5)C(=O)O)O |
| Reference | [1]. Hilberg F, et al. BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumorefficacy. Cancer Res. 2008 Jun 15;68(12):4774-82. [2]. Stopfer P, et al. Pharmacokinetics and metabolism of BIBF 1120 after oral dosing to healthy male volunteers. Xenobiotica. 2011 Apr;41(4):297-311. |
