BIBF1120 Inhibitor CAS No. 656247-17-5

Cat. No.	Name	Size	Price
KI0195	BIBF1120	5 mg	$150
	BIBF1120	25 mg	$352.8
	BIBF1120	50 mg	$750
	BIBF1120	200 mg	$1836.8

Chemical Characteristic

Product Name	BIBF1120
Synonyms	Vargatef
CAS No.	656247-17-5
Molecular Weight	539.62
Formula	C₃₁H₃₃N₅O₄
Chemical Name	(Z)-methyl 3-((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenylamino)(phenyl)methylene)-2-oxoindoline-6-carboxylate
Smiles	N1C(=O)/C(=C(/c2ccccc2)\Nc2ccc(cc2)N(C(=O)CN2CCN(CC2)C)C)/c2ccc(cc12)C(=O)OC
Chemical Structure

Biological activities

BIBF1120 is a potent vascular endothelial growth factor receptor (VEGFR), platelet-derived growth factor receptors (PDGFR) and fibroblast growth factor receptors (FGFR) kinase inhibitor. BIBF1120 has IC50 values of 34, 21 and 13 nM for VEGFR-1, VEGFR-2 and VEGFR-3, respectively. BIBF1120 has IC50 values of 69, 37, 108 and 610 nM for FGFR-1, FGFR-2, FGFR-3 and FGFR-4, respectively. BIBF1120 inhibits PDGFR kinase activity of PDGFR-α and PDGFR-β types with IC50 values of 59 and 65 nM, respectively. BIBF1120 inhibits cell proliferation with EC50 <10 nM in VEGF-stimulated endothelial cells derived from umbilical veins (HUVEC) and skin microvessels (HSMEC). BIBF1120 inhibits proliferation of PDGF-BB??timulated bovine retinal pericytes (BRPs) with an EC50 value of 79 nM.^[1] BIBF1120 at a concentration of 10 nM completely inhibits the phosphorylation of VEGFR-2 and mitogen-activated protein kinase (MAPK) in HUVECs. BIBF1120 at a concentration of 10 nM partially inhibits tube formation in HUVECs stimulated with VEGF, whereas BIBF1120 at a concentration of 1 µM completely inhibits tube formation. The IC50 values of BIBF1120 for the HLE, HLF, HepG2, and Huh7 cell lines are 2.7, 2.7, 5.3 and 4.3 µM, respectively. In HepG2 xenografts model, a low (50 mg/kg/d) and high (100 mg/kg/d) dose of BIBF1120 significantly inhibits tumor growth with treated/control (T/C) values of 0.36 and 0.42, respectively. Besides, BIBF1120 administration (50 and 100 mg/kg/d) also significantly inhibits tumor angiogenesis. Body weight loss is not observed after the administration of BIBF1120 at either dose.^[2] In all tumor models, including human FaDu (squamous cell carcinoma of the head and neck) xenografts growing in nude mice and a syngeneic rat tumor model, BIBF1120 is highly active at well-tolerated doses (25-100 mg/kg daily p.o.), as measured by magnetic resonance imaging of tumor perfusion after 3 days, reducing vessel density and vessel integrity after 5 days, and inducing profound growth inhibition.^[1]

References

[1] Hilberg F, et al. BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. Cancer Res. 2008, 68(12): 4774-4782. [2] Kudo K, et al. Antitumor activity of BIBF 1120, a triple angiokinase inhibitor, and use of VEGFR2+pTyr+ peripheral blood leukocytes as a pharmacodynamic biomarker in vivo. Clin Cancer Res. 2011, 17(6): 1373-1381.

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