A VEGFR, FGFR, and PDGFR inhibitor
Related Products
Active Metabolite(s)
27176BIBF 1202
Alternative(s)
11022BIBF 1120
Labeled Version(s)
25312BIBF 1120-13C-d3
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BIBF 1120 (esylate)

Item No. 31082

Technical Information
Formal Name
(3Z)-2,3-dihydro-3-[[[4-[methyl[2-(4-methyl-1-piperazinyl)acetyl]amino]phenyl]amino]phenylmethylene]-2-oxo-1H-indole-6-carboxylic acid, methyl ester, monoethanesulfonate
CAS Number
656247-18-6
Synonyms
  • Nintedanib
Molecular Formula
C31H33N5O4 • C2H6O3S
Formula Weight
Purity
≥98%
A solid
DMF: 3 mg/mlDMSO: 5 mg/mlDMSO:PBS (pH 7.2) (1:5): 0.16 mg/ml
λmax
287, 392 nm
SMILES
O=C1NC2=CC(C(OC)=O)=CC=C2/C1=C(C3=CC=CC=C3)/NC4=CC=C(N(C(CN5CCN(C)CC5)=O)C)C=C4.O=S(O)(CC)=O
InChi Code
InChI=1S/C31H33N5O4.C2H6O3S/c1-34-15-17-36(18-16-34)20-27(37)35(2)24-12-10-23(11-13-24)32-29(21-7-5-4-6-8-21)28-25-14-9-22(31(39)40-3)19-26(25)33-30(28)38;1-2-6(3,4)5/h4-14,19,32H,15-18,20H2,1-3H3,(H,33,38);2H2,1H3,(H,3,4,5)/b29-28-;
InChi Key
MMMVNAGRWOJNMW-FJBFXRHMSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    BIBF 1120 is an inhibitor of the receptor tyrosine kinases VEGFR, FGFR, and PDGFR (IC50s = 13-34, 37-610, 59, and 65 nM for VEGFR1-3, FGFR1-4, PDGFRα, and PDGFRβ, respectively).1 It is selective for VEGFR, FGFR, and PDGFR over a panel of 33 kinases but does inhibit FLT3, LCK, LYN, and Src (IC50s = 16-156 nM). BIBF 1120 inhibits growth factor-dependent proliferation of human umbilical vascular endothelial cells (HUVECs), human microvascular skin endothelial cells (HSMECs), human umbilical artery smooth muscle cells (HUASMCs), and bovine retinal pericytes (BRPs; EC50s = 7-290 nM). In vivo, BIBF 1120 (100 mg/kg) reduces tumor microvessel density and the number of PDGFRβ-expressing perivascular cells in a FaDu head and neck small cell carcinoma mouse xenograft model. It also inhibits tumor growth in a Caki-1 renal cancer mouse xenograft model. Formulations containing BIBF 1120 have been used in the treatment of idiopathic pulmonary fibrosis and non-small cell lung cancer (NSCLC).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hilberg, F., Roth, G.J., Krssak, M., et alBIBF 1120: Triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. Cancer Res. 68(12), 4774-4782 (2008).