Nintedanib esylate
Nintedanib esylate (BIBF 1120 esylate) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
Product Specifications
CAS Number
656247-18-6
Product Name Alternative
BIBF 1120 (esylate)
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
FGFR; PDGFR; VEGFR
Type
Reference compound
Related Pathways
Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/BIBF-1120-esylate.html
Purity
99.96
Solubility
DMSO : 66.67 mg/mL (ultrasonic) |Ethanol : 3.08 mg/mL (ultrasonic) |H2O : 16.67 mg/mL (ultrasonic)
Smiles
O=C(C1=CC(NC/2=O)=C(C=C1)C2=C(NC3=CC=C(N(C)C(CN4CCN(C)CC4)=O)C=C3)/C5=CC=CC=C5)OC.CCS(=O)(O)=O
Molecular Formula
C33H39N5O7S
Molecular Weight
649.76
Precautions
H302, H315, H319, H335
References & Citations
[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]Roth GJ, 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, 52 (14), 4466-4480.|[3]Suzuki N, et al. Effect of a novel oral chemotherapeutic agent containing a combination of trifluridine, tipiracil and the novel triple angiokinase inhibitor nintedanib, on human colorectal cancer xenografts. Oncol Rep. 2016 Dec;36 (6) :3123-3130.
Shipping Conditions
Room Temperature
Storage Conditions
4°C (Powder, sealed storage, away from moisture)
Scientific Category
Reference compound1
Clinical Information
Launched
Isoform
PDGFRα; PDGFRβ; VEGFR1/Flt-1; VEGFR2/KDR/Flk-1; VEGFR3/Flt-4
Citation 01
Am J Respir Cell Mol Biol. 2020 Feb;62 (2) :178-190.|Nano Today. 2024 Feb:54:102058.|Preprints. 2025 Apr 08.|ACS Omega. 2022 May 17;7 (21) :17658-17669.|Acta Pharmacol Sin. 2021 Dec;42 (12) :2058-2068.|Am J Respir Cell Mol Biol. 2019 Jul;61 (1) :74-85.|Am J Respir Cell Mol Biol. 2021 Jul;65 (1) :54-69.|Bioact Mater. 2023 Nov 22:33:262-278.|bioRxiv. 2024 Apr 21.|bioRxiv. 2024 Sep 13:2024.01.10.575008.|bioRxiv. 2025 Aug 09.|bioRxiv. 2025 March 19.|bioRxiv. 2025 Oct 24.|Br J Cancer. 2020 Mar;122 (7) :986-994.|Cell Chem Biol. 2022 Jul 21;29 (7) :1113-1125.e6.|Cell Death Dis. 2025 Apr 11;16 (1) :278.|Curr Eye Res. 2022 Dec;47 (12) :1578-1589.|Drug Dev Ind Pharm. 2024 Aug 7:1-16.|Eur J Drug Metab Pharmacokinet. 2021 Sep;46 (5) :625-635.|Eur J Pharmacol. 2024 Jun 5:972:176547.|Eur Respir J. 2025 Jan 9:2400615.|European J Org Chem. Nov 2022|Exp Eye Res. 2023 Apr:229:109431.|Exp Eye Res. 2025 Feb 12:110285.|FEBS Lett. 2024 Dec;598 (24) :3053-3070.|Folia Histochem Cytobiol. 2025;63 (2) :79-87.|Free Radic Biol Med. 2021 Aug 1:171:135-142.|Fundam Clin Pharmacol. 2021 Oct;35 (5) :919-929.|Harvard Medical School LINCS LIBRARY|Int Immunopharmacol. 2022 Dec;113 (Pt B) :109427.|Int J Mol Sci. 2022 Jul 25;23 (15) :8193.|Int J Mol Sci. 2023 Jan 12;24 (2) :1475.|Int J Ophthalmol. 2022 Jun 18;15 (6) :914-923.|Integr Biol (Camb) . 2022 Mar 21;14 (1) :1-12.|J Agric Food Chem. 2025 Apr 2;73 (13) :7774-7787.|J Cell Biochem. 2020 Mar;121 (3) :2343-2353.|J Ethnopharmacol. 2023 Oct 5:314:116633.|J Exp Med. 2025 Aug 4;222 (8) :e20241174.|J Mol Struct. 2016 Jul 5; 1115:171-179.|J Nat Prod. 2019 May 24;82 (5) :1331-1337.|J Ophthalmol. 2023 Apr 28:2023:7355039.|J Pharmacol Exp Ther. 2019 Jun;369 (3) :511-522.|J Photochem Photobiol B. 2016 Apr:157:70-6.|Life Sci. 2022 Nov 1:308:120950.|Lung Cancer. 2023 Jun:180:107219.|medRxiv. 2024 Jun 28.|Nat Mach Intell. 2020 Jun.|Nature. 2025 Nov 26.|Oncol Lett. 2024 Jan 25;27 (3) :123.|Oncol Rep. 2016 Dec;36 (6) :3123-3130.|Patent. US20220257531A1.|PLoS One. 2019 Aug 6;14 (8) :e0218632.|PLoS One. 2024 Nov 1;19 (11) :e0308647.|Research Square Print. September 14th, 2022.|Respir Investig. 2025 Jul 18;63 (5) :904-914.|Sci Adv. 2022 Jun 17;8 (24) :eabn4564.|Sci Rep. 2018 Jun 22;8 (1) :9540. |Sci Transl Med. 2018 Jul 18;10 (450) :eaaq1093.|Sci Transl Med. 2022 Sep 28;14 (664) :eabo5070.|Small. 2024 Jul 25:e2403428.|SSRN. 2023 May 8.|SSRN. 2025 Aug 27.|Stem Cell Res Ther. 2020 Nov 25;11 (1) :496.|University of Pittsburgh. 2025.|Virology. 2023 Aug:585:205-214.
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