Nintedanib esylate

$66$408

Products Details

Product Description

– 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.

Web ID

– HY-11106

Storage Temperature

– 4°C (Powder, sealed storage, away from moisture)

Shipping

– Room Temperature

Applications

– Cancer-Kinase/protease

Molecular Formula

– C33H39N5O7S

Citations

– Am J Respir Cell Mol Biol. 2020 Feb;62(2):178-190. |Nano Today. 2024 Feb, 54, 102058.|ACS Omega. 2022, 7, 21, 17658-17669.|Acta Pharmacol Sin. 2021 Mar 2.|Am J Respir Cell Mol Biol. 2019 Jul;61(1):74-85. |Am J Respir Cell Mol Biol. 2021 Mar 24.|Bioact Mater. 2024 Mar, 33, Pages 262-278.|Br J Cancer. 2020 Mar;122(7):986-994.|Cell Chem Biol. 2022 Jun 9;S2451-9456(22)00201-X.|Curr Eye Res. 2022 Oct 19;1-12.|Eur J Drug Metab Pharmacokinet. 2021 Jul 18;1-11.|European J Org Chem. Nov 2022|Exp Eye Res. 2023 Mar 2;109431.|Free Radic Biol Med. 2021 May 11;S0891-5849(21)00291-4.|Fundam Clin Pharmacol. 2021 Feb 1.|Harvard Medical School LINCS LIBRARY|Int Immunopharmacol. 2022, 113: 109427.|Int J Mol Sci. 2022 Jul 25;23(15):8193.|Int J Mol Sci. 2023, 24(2), 1475.|Int J Ophthalmol. 2022 Jun 18;15(6):914-923.|Integr Biol (Camb). 2022 Feb 19;zyac001.|J Cell Biochem. 2020 Mar;121(3):2343-2353.|J Ethnopharmacol. 2023 May 17;116633.|J Nat Prod. 2019 May 24;82(5):1331-1337.|J Ophthalmol. 2023 Apr 28.|J Pharmacol Exp Ther. 2019 Jun;369(3):511-522.|J Photochem Photobiol B. 2016 Feb 5;157:70-76. |Journal of Molecular Structure. 2016 Jul 5; 1115:171-179.|Life Sci. 2022 Sep 10;120950.|Lung Cancer. 2023 Jun, 180, 107219.|Nature Machine Intelligence. 2020 Jun.|Oncol Rep. 2016 Dec;36(6):3123-3130.|Patent. US20220257531A1.|PLoS One. 2019 Aug 6;14(8):e0218632.|Research Square Print. September 14th, 2022.|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. 7 Jul 2022.|SSRN. 2023 May 8.|Stem Cell Res Ther. 2020 Nov 25;11(1):496.|Virology. 2023 Jun 21.

References

– [1]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.|[2]Hilberg F, et al. BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. Cancer Res, 2008, 68(12), 4774-4782.|[3]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.

CAS Number

– 656247-18-6

Molecular Weight

– 649.76

Compound Purity

– 99.95

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

Clinical Information

– Launched

Research Area

– Cancer

Solubility

– DMSO : 66.67 mg/mL (ultrasonic)|Ethanol : 3.08 mg/mL (ultrasonic)|H2O : 16.67 mg/mL (ultrasonic)

Target

– FGFR;PDGFR;VEGFR

Isoform

– FGFR1;FGFR2;FGFR3;PDGFRα;PDGFRβ;VEGFR1/Flt-1;VEGFR2/KDR/Flk-1;VEGFR3/Flt-4

Pathway

– Protein Tyrosine Kinase/RTK

Product type

– Reference compound

Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.

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