An internal standard for the quantification of BIBF 1120
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BIBF 1120-13C-d3

Item No. 25312

Technical Information
Formal Name
methyl (Z)-3-(((4-(N-methyl-2-(4-(methyl-13C-d3)piperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate
Synonyms
  • Nintedanib-13C-d3
Molecular Formula
C30[13C]H30D3N5O4
Formula Weight
Purity
≥99% deuterated forms (d1-d3)
A solid
DMSO: 25 mg/ml
SMILES
CN(C(CN1CCN([13C]([2H])([2H])[2H])CC1)=O)C(C=C2)=CC=C2N/C(C3=CC=CC=C3)=C4C(C=CC(C(OC)=O)=C5)=C5NC/4=O
InChi Code
InChI=1S/C31H33N5O4/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/h4-14,19,32H,15-18,20H2,1-3H3,(H,33,38)/b29-28-/i1+1D3
InChi Key
XZXHXSATPCNXJR-JMEGZYTGSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    BIBF 1120-13C-d3 is intended for use as an internal standard for the quantification of BIBF 1120 (Item Nos. 11022 | 31082) by GC- or LC-MS. 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).