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Nintedanib

Catalog No. T1777 CAS 656247-17-5

Synonyms: BIBF 1120, Intedanib

Nintedanib (Intedanib) is a triple vascular kinase inhibitor that inhibits VEGFR1, VEGFR2, and VEGFR3 (IC50=34/13/13 nM), FGFR1, FGFR2, and FGFR3 (IC50=69/37/108 nM), PDGFRα, and PDGFRβ (IC50=59/65 nM). Nintedanib has antitumor activity and inhibits tumor growth by inhibiting angiogenesis.

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Nintedanib, CAS 656247-17-5

Pack Size	Availability	Price/USD
5 mg	In stock	$ 38.00
10 mg	In stock	$ 54.00
50 mg	In stock	$ 64.00
100 mg	In stock	$ 93.00
200 mg	In stock	$ 144.00
1 mL * 10 mM (in DMSO)	In stock	$ 50.00

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Purity: 99.92%

Purity: 99.72%

Purity: 99.65%

Purity: 99.36%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Nintedanib (Intedanib) is a triple vascular kinase inhibitor that inhibits VEGFR1, VEGFR2, and VEGFR3 (IC50=34/13/13 nM), FGFR1, FGFR2, and FGFR3 (IC50=69/37/108 nM), PDGFRα, and PDGFRβ (IC50=59/65 nM). Nintedanib has antitumor activity and inhibits tumor growth by inhibiting angiogenesis.
Targets&IC50	PDGFRα:59 nM (cell free), FGFR1:69 nM (cell free), FGFR2:37 nM (cell free), VEGFR1:34 nM (cell free), VEGFR3:13 nM (cell free), VEGFR2:13 nM (cell free)
In vitro	METHODS: Human nasopharyngeal carcinoma cells CNE-2, HNE-1 and HONE-1 were treated with Nintedanib (0.078-10 µM) for 72 h, and cell viability was measured by CCK8 assay. RESULTS: Nintedanib significantly inhibited the growth of CNE-2, HNE-1 and HONE-1 cell lines in a dose-dependent manner with IC50 values of 4.16 µM, 5.62 µM and 6.32 µM, respectively. [1] METHODS: Human endothelial cells HUVEC, smooth muscle cells HUASMC and bovine pericytes were treated with Nintedanib (0.03-1 µM) for 2 h, and the expression levels of target proteins were detected by Western Blot. RESULTS: Nintedanib inhibited ligand-dependent phosphorylation of MAPK and Akt in HUVEC, HUASMC and bovine pericytes. [2]
In vivo	METHODS: To test the antitumor activity in vivo, Nintedanib (10-100 mg/kg) was administered by gavage to athymic NMRI-nu/nu mice bearing the human head and neck small cell carcinoma tumor FaDu or the human renal carcinoma tumor Caki-1 once daily for 23-35 days. RESULTS: Nintedanib inhibited tumor growth in FaDu and Caki-1. [2] METHODS: To test the antitumor activity in vivo, Nintedanib (40 mg/kg) and TFTD (150 mg/kg) were administered intraperitoneally to BALB/c nu/nu mice bearing tumors of DLD-1, DLD-1/5-FU, HT-29, or HCT116 twice daily for two weeks. RESULTS: At day 15, Nintedanib and TFTD monotherapy resulted in a significant reduction in tumor growth in vivo. The combination therapy exhibited greater anti-tumor activity than the two monotherapies. [3]
Kinase Assay	The cytoplasmic tyrosine kinase domain of VEGFR-2 (residues 797–1355 according to sequence deposited in databank SWISS-PROT P35968) was cloned into pFastBac fused to GST and extracted as described in supplementary methods. Enzyme activity was assayed using standard conditions using a random polymer (Glu/Tyr 4:1) and in the presence of 100 μmol/L ATP (for details, see supplementary methods). For all other kinase assays, the entire cytoplasmic domains of the receptors (from the end of the transmembrane to the COOH terminus) were cloned into pFastBac vector containing GST and assayed under standard conditions [1].
Cell Research	HUVEC, HUASMC, and BRP were cultured as described above. Two hours before the addition of ligands, BIBF 1120 was added to the cultures. Cell lysates were generated according to standard protocols. Western blotting was done using standard SDS-PAGE methods, loading 50 to 75 μg of protein per lane, with detection by enhanced chemiluminescence. Total and phosphorylated mitogen-activated protein kinase (MAPK) was analyzed using monoclonal antibodies M3807 and M8159. Total Akt was detected using the polyclonal antibody and phosphorylated Akt (Ser473) was analyzed with the monoclonal antibody. Cleaved caspase-3 was detected with the monoclonal antibody [1].
Animal Research	Five-week-old to 6-wk-old athymic NMRI-nu/nu female mice (21–31 g) were purchased from Harlan. After acclimatization, mice were inoculated with 1 to 5 × 10^6 (in 100 μL) FaDu, Caki-1, SKOV-3, H460, HT-29, or PAC-120 cells s.c. into the right flank of the animal. F344 Fischer rats after acclimatization were injected with 5 × 10^6 (in 100 μL) GS-9L cells s.c. into the right flank of the animal. For pharmacokinetic analysis, blood was isolated at indicated time points from the retroorbital plexus of mice and plasma was analyzed using high-performance liquid chromatography-mass spectrometry methodology [1].

Synonyms	BIBF 1120, Intedanib
Molecular Weight	539.62
Formula	C31H33N5O4
CAS No.	656247-17-5

Storage

keep away from direct sunlight

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 3 mg/mL (5.55 mM)

DMSO: 6 mg/mL (11.11 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Xue C, et al. Efficacy of BIBF 1120 or BIBF 1120 plus chemotherapy on nasopharyngeal carcinoma in vitro and in vivo. Drug Des Devel Ther. 2016 Mar 15;10:1173-80. 2. Hilberg F, et al. BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. Cancer Res. 2008 Jun 15;68(12):4774-82. 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.

Citations

1. Dong X, Wang L, Wang D, et al.Proteomic study on nintedanib in gastric cancer cells.PeerJ.2024, 12: e16771.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Kinase Inhibitor Library Anti-Cancer Active Compound Library Membrane Protein-targeted Compound Library Anti-Cancer Approved Drug Library Tyrosine Kinase Inhibitor Library Drug Repurposing Compound Library EMA Approved Drug Library Inhibitor Library Anti-Cancer Clinical Compound Library

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N-Desethylsunitinib hydrochloride SU11274 Riddelline (Z)-Guggulsterone JK-P3 RAF265 SU5205 TAK-593

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Keywords

Nintedanib 656247-17-5 Angiogenesis Tyrosine Kinase/Adaptors VEGFR FGFR PDGFR FLT Src BIBF 1120 Inhibitor Platelet-derived growth factor receptor Fibroblast growth factor receptor Vascular endothelial growth factor receptor Intedanib BIBF1120 inhibit BIBF-1120 inhibitor

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