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Nintedanib
- BIBF-1120
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C31H33N5O4
- MW: 539.62
Description
Orally bioavailable, indolinone-derived, receptor tyrosine kinase (RTK) inhibitor with potential antiangiogenic and antineoplastic activities that simultaneously targets VEGFR1-3 (IC50 values 34 nM, 21 nM, and 13 nM, resp.), PDGFRα and β (IC50 values 59 and 65 nM), and FGFR1-3 (IC50 values 69 nM, 37 nM, and 108 nM, resp). In addition, BIBF1120 also inhibits members of the Src family of tyrosine kinases, including Src, Lck, Lyn, and FLT-3 (IC50 values 156 nM, 16 nM, 195 nM, and 26 nM, resp.).
More Information
| Parent CAS No. | 656247-17-5 |
|---|---|
| Chemical Name | (Z)-methyl 3-((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenylamino)(phenyl)methylene)-2-oxoindoline-6-carboxylate |
| SMILES | N1C2=C(C=CC(C(OC)=O)=C2)/C(=C(/NC2=CC=C(N(C)C(CN3CCN(C)CC3)=O)C=C2)C2=CC=CC=C2)/C1=O |
| MFCD | N.A. |
| InChi | 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- |
| InChiKey | XZXHXSATPCNXJR-ZIADKAODSA-N |
| CID | 135423438 |
| Short Description | RTK inhibitor |
References
- C Rolfo et al. BIBF 1120/ nintedanib : a new triple angiokinase inhibitor-directed therapy in patients with non-small cell lung cancer. Expert Opin Investig Drugs. 2013 Aug;22(8):1081-8.
- G Bousquet et al. Phase I study of BIBF 1120 with docetaxel and prednisone in metastatic chemo-naive hormone-refractory prostate cancer patients. Br J Cancer. 2011 Nov 22;105(11):1640-5.
- F Hilberg et al. BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. Cancer Res. 2008 Jun 15;68(12):4774-82.
- GJ Roth et al. Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120). J Med Chem. 2009 Jul 23;52(14):4466-80.
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