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BIBF 1202

Names

[ CAS No. ]:
894783-71-2

[ Name ]:
BIBF 1202

[Synonym ]:
1H-Indole-6-carboxylic acid, 2,3-dihydro-3-[[[4-[methyl[(4-methyl-1-piperazinyl)acetyl]amino]phenyl]amino]phenylmethylene]-2-oxo-, (3Z)-
BIBF 1202

Biological Activity

[Description]:

BIBF 1202 is the carboxylate metabolite of BIBF 1120 which inhibits VEGFR2 kinase with an IC50 of 62 nM.

[Related Catalog]:

Research Areas >> Cancer

[Target]

IC50: 62 nM (VEGFR2)[1]


[In Vitro]

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].

[References]

[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.


[Related Small Molecules]

Nintedanib (BIBF 1120) | SU5416 | Apatinib Mesylate | PD173074 | Foretinib (GSK1363089) | SU 5402 | Linifanib (ABT-869) | Cediranib | Lucitanib | RAF265 (CHIR-265) | LY2784544 | SU14813 | Dovitinib (TKI-258, CHIR-258) | SAR131675 | Vatalanib (PTK787) 2HCl

Chemical & Physical Properties

[ Molecular Formula ]:
C30H31N5O4

[ Molecular Weight ]:
525.59800

[ Exact Mass ]:
525.23800

[ PSA ]:
105.22000

[ LogP ]:
3.61430

[ Storage condition ]:
2-8℃

Related Compounds