製品番号: HY-50904

ニンテダニブ

(別名: Nintedanib; BIBF 1120)

74 Cited Publications

カスタマーレビュー

Based on 74 publication(s) in Google Scholar

Nintedanib (BIBF 1120) 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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

純度: 99.90%
CAS 番号: 656247-17-5
分子式: C₃₁H₃₃N₅O₄
分子量:539.62

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Nintedanib 構造式

CAS 番号: 656247-17-5

容量

価格（税別）

在庫状況

数量

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
化学情報
Publications (74)
溶剤 & 溶解度
- 体外
- 体内
プロトコル
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target^[1]

VEGFR1

34 nM (IC₅₀)

VEGFR2

13 nM (IC₅₀)

VEGFR3

13 nM (IC₅₀)

FGFR1

69 nM (IC₅₀)

FGFR2

37 nM (IC₅₀)

FGFR3

108 nM (IC₅₀)

PDGFRα

59 nM (IC₅₀)

PDGFRβ

65 nM (IC₅₀)

PDGFR アイソフォーム固有の製品をすべて表示 :

VEGFR アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	22.62 μM Compound: Nintedanib	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 28826084]
Calu-6	EC₅₀	>1 μM Compound: 3, BIBF1120	Antiangiogenic activity against human Calu6 cells assessed as inhibition of cell proliferation by [3H]thymidine incorporation assay Antiangiogenic activity against human Calu6 cells assessed as inhibition of cell proliferation by [3H]thymidine incorporation assay	[PMID: 19522465]
Calu-6	EC₅₀	>3500 nM Compound: BIBF 1120	Antiangiogenic activity in human Calu6 assessed as inhibition of cell proliferation by [3H]thymidine incorporation assay in presence of fetal calf serum Antiangiogenic activity in human Calu6 assessed as inhibition of cell proliferation by [3H]thymidine incorporation assay in presence of fetal calf serum	[PMID: 18559524]
FaDu	EC₅₀	>1 μM Compound: 3, BIBF1120	Antiangiogenic activity against human FADU cells assessed as inhibition of cell proliferation by [3H]thymidine incorporation assay Antiangiogenic activity against human FADU cells assessed as inhibition of cell proliferation by [3H]thymidine incorporation assay	[PMID: 19522465]
FaDu	EC₅₀	>4500 nM Compound: BIBF 1120	Antiangiogenic activity in human FADU assessed as inhibition of cell proliferation by [3H]thymidine incorporation assay in presence of fetal calf serum Antiangiogenic activity in human FADU assessed as inhibition of cell proliferation by [3H]thymidine incorporation assay in presence of fetal calf serum	[PMID: 18559524]
HeLa	EC₅₀	>1 μM Compound: 3, BIBF1120	Antiangiogenic activity against human HeLa cells assessed as inhibition of cell proliferation by [3H]thymidine incorporation assay Antiangiogenic activity against human HeLa cells assessed as inhibition of cell proliferation by [3H]thymidine incorporation assay	[PMID: 19522465]
HeLa	EC₅₀	>3500 nM Compound: BIBF 1120	Antiangiogenic activity in human HeLa assessed as inhibition of cell proliferation by [3H]thymidine incorporation assay in presence of fetal calf serum Antiangiogenic activity in human HeLa assessed as inhibition of cell proliferation by [3H]thymidine incorporation assay in presence of fetal calf serum	[PMID: 18559524]
HeLa	IC₅₀	51.65 μM Compound: Nintedanib	Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay	[PMID: 28190652]
HT-29	IC₅₀	0.83 μM Compound: Nintedanib	Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 28826084]
HT-29	IC₅₀	4.9 μM Compound: Nintedanib	Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 28190652]
HUVEC	EC₅₀	<10 nM Compound: BIBF 1120	Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced apoptosis by [3H]thymidine incorporation assay Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced apoptosis by [3H]thymidine incorporation assay	[PMID: 18559524]
HUVEC	EC₅₀	290 nM Compound: BIBF 1120	Antiangiogenic activity in HUVEC assessed as inhibition of bFGF-induced cell proliferation by [3H]thymidine incorporation assay Antiangiogenic activity in HUVEC assessed as inhibition of bFGF-induced cell proliferation by [3H]thymidine incorporation assay	[PMID: 18559524]
HUVEC	EC₅₀	9 nM Compound: BIBF 1120	Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced cell proliferation by [3H]thymidine incorporation assay Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced cell proliferation by [3H]thymidine incorporation assay	[PMID: 18559524]
HUVEC	IC₅₀	10 nM Compound: 3, BIBF1120	Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced cell proliferation by [3H]thymidine incorporation assay Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced cell proliferation by [3H]thymidine incorporation assay	[PMID: 19522465]
MCF7	IC₅₀	8.28 μM Compound: Nintedanib	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 28826084]
NIH3T3	IC₅₀	2.41 μM Compound: Nintedanib	Antiproliferative activity against mouse NIH3T3 cells assessed as cell growth inhibition incubated for 24 to 72 hrs by CCK-8 assay Antiproliferative activity against mouse NIH3T3 cells assessed as cell growth inhibition incubated for 24 to 72 hrs by CCK-8 assay	[PMID: 36463728]
NRK-49F	IC₅₀	1.1 μM Compound: 2	Inhibition of TGF-beta-induced collagen accumulation in rat NRK-49F cells incubated for 2 days by PSR staining based microscopic analysis Inhibition of TGF-beta-induced collagen accumulation in rat NRK-49F cells incubated for 2 days by PSR staining based microscopic analysis	[PMID: 31699535]
NRK-49F	IC₅₀	1.1 μM Compound: Nintedanib	Inhibition of TGF-beta-induced collagen accumulation in rat NRK-49F cells incubated for 2 days by PSR staining based microscopic analysis Inhibition of TGF-beta-induced collagen accumulation in rat NRK-49F cells incubated for 2 days by PSR staining based microscopic analysis	[PMID: 32334267]
PC-3	IC₅₀	<30 μM Compound: Nintedanib	Cytotoxicity against human PC3 cells assessed as reduction in cell viability by CellTiter-Fluor assay Cytotoxicity against human PC3 cells assessed as reduction in cell viability by CellTiter-Fluor assay	[PMID: 30951312]
Sf9	IC₅₀	1.9 nM Compound: BIBF 1120	Inhibition of N-terminal GST-tagged human recombinant PDGFRalpha D842I mutant expressed in baculovirus-infected Sf9 cells using FAM-labeled peptide and ATP as substrate preincubated for 10 mins followed by substrate addition measured after 1 hr by mobilit Inhibition of N-terminal GST-tagged human recombinant PDGFRalpha D842I mutant expressed in baculovirus-infected Sf9 cells using FAM-labeled peptide and ATP as substrate preincubated for 10 mins followed by substrate addition measured after 1 hr by mobilit	[PMID: 32305182]
Sf9	IC₅₀	13 nM Compound: BIBF 1120	Inhibition of mouse GST-fused VEGFR2 expressed in Sf9 insect cells after 20 mins by scintillation counting Inhibition of mouse GST-fused VEGFR2 expressed in Sf9 insect cells after 20 mins by scintillation counting	[PMID: 18559524]
Sf9	IC₅₀	21 nM Compound: BIBF 1120	Inhibition of human GST-fused VEGFR2 expressed in Sf9 insect cells after 20 mins by scintillation counting Inhibition of human GST-fused VEGFR2 expressed in Sf9 insect cells after 20 mins by scintillation counting	[PMID: 18559524]
Sf9	IC₅₀	5 nM Compound: 3, BIBF1120	Inhibition of human VEGFR2 expressed in Sf9 cells Inhibition of human VEGFR2 expressed in Sf9 cells	[PMID: 19522465]
SK-OV-3	IC₅₀	28.76 μM Compound: Nintedanib	Antiproliferative activity against human SKOV3 cells after 72 hrs by MTT assay Antiproliferative activity against human SKOV3 cells after 72 hrs by MTT assay	[PMID: 28190652]

体外実験

Nintedanib (BIBF 1120) binds to the ATP-binding site in the cleft between the amino and carboxy terminal lobes of the kinase domain. Nintedanib (BIBF 1120) inhibits proliferation of PDGF-BB stimulated BRPs with EC₅₀ of 79 nM in cell assays. Nintedanib (BIBF 1120) (100 nM) blocks activation of MAPK after stimulation with 5% serum plus PDGF-BB. Nintedanib (BIBF 1120) prevents PDGF-BB stimulated proliferation with an EC₅₀ of 69 nM in cultures of human vascular smooth muscle cells (HUASMC)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

体内実験

Nintedanib (BIBF 1120) (25-100 mg/kg daily p.o.) is highly active in all tumor models, including human tumor xenografts growing in nude mice and a syngeneic rat tumor model. This is evident in the magnetic resonance imaging of tumor perfusion after 3 days, reducing vessel density and vessel integrity after 5 days, and profound growth inhibition^[1]. Nintedanib (BIBF 1120) is orally available and displays encouraging efficacy in in vivo tumor models while being well tolerated^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

化学情報

CAS 番号 656247-17-5
性状 Solid
分子量 539.62
分子式 C₃₁H₃₃N₅O₄
Color Light yellow to yellow
SMILES

O=C1NC2=CC(C(OC)=O)=CC=C2/C1=C(NC3=CC=C(N(C(CN4CCN(C)CC4)=O)C)C=C3)\C5=CC=CC=C5
別名

Nintedanib; BIBF 1120
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (74)

All Cell Imaging/StainingIn Vivo Efficacy StudyCell Proliferation/Viability AssayHistological Imaging/StainingWB

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Journal Impact Factor

Nature

Inhibitors supercharge kinase turnover through native proteolytic circuits. [Abstract]

2026 Jan;649(8098):1032-1041. PMID: 41299171
Science

Antifibrotic drug finerenone restores fertility in premature ovarian insufficiency. [Abstract]

2026 Feb 5;391(6785):eadz4075. PMID: 41643022
Nat Mach Intell

2020 Jun.
Eur Respir J

Inhibition of AXL ameliorates pulmonary fibrosis via attenuation of M2 macrophage polarization. [Abstract]

2025 Jan 9:2400615. PMID: 39788632
Bioact Mater

Alveolar macrophage phagocytosis-evading inhaled microgels incorporating nintedanib-PLGA nanoparticles and pirfenidone-liposomes for improved treatment of pulmonary fibrosis. [Abstract]

2023 Nov 22:33:262-278. PMID: 38076650

Nintedanib purchased from MedChemExpress. Usage Cited in: Bioact Mater. 2023 Nov 22:33:262-278. [Abstract]

CLSM images of E-cadherin immunostaining in A549 cells after TGF-β (10 ng/mL) stimulation with Nintedanib (10 μM), PF (50 μM), n-PN (10 μM), and p-LP (50 μM) for 48 h were obtained.

Nintedanib purchased from MedChemExpress. Usage Cited in: Bioact Mater. 2023 Nov 22:33:262-278. [Abstract]

Cell growth inhibition of nintedanib (48 h), PF, n-PN, and p-LP at various concentrations in NIH/3T3 fibroblasts was assessed using an MTT assay.
Sci Transl Med

SARS-CoV-2 infection produces chronic pulmonary epithelial and immune cell dysfunction with fibrosis in mice. [Abstract]

2022 Sep 28;14(664):eabo5070. PMID: 35857635

Nintedanib purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2022 Sep 28;14(664):eabo5070. [Abstract]

Nintedanib (60 mg/kg). Mice were dosed once daily by oral gavage with either 100 μL of the suspension, and animals were monitored for weight loss.

Nintedanib purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2022 Sep 28;14(664):eabo5070. [Abstract]

Nintedanib (60 mg/kg). Mice were dosed once daily by oral gavage with either 100 μL of the suspension, and histopathological analysis of lungs was performed.
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Sci Adv

Female reproductive life span is extended by targeted removal of fibrotic collagen from the mouse ovary. [Abstract]

2022 Jun 17;8(24):eabn4564. PMID: 35714185
Biomaterials
Cell Death Dis

Inhibition of Rho GEFs attenuates pulmonary fibrosis through suppressing myofibroblast activation and reprogramming profibrotic macrophages. [Abstract]

2025 Apr 11;16(1):278. PMID: 40216763
Small

Self-Oxygenated Hydrogel Enhances Immune Cell Response and Infiltration Via Triggering Dual DNA Damage to Activate cGAS-STING and Inhibiting CAFs. [Abstract]

2024 Jul 25:e2403428. PMID: 39051518
J Exp Med

A multimorphic variant in ThPOK causes an inborn error of immunity with T cell defects and fibrosis. [Abstract]

2025 Aug 4;222(8):e20241174. PMID: 40392549
Nano Today

Reprogramming the pancreatic cancer stroma and immune landscape by a silicasome nanocarrier delivering nintedanib, a protein tyrosine kinase inhibitor. [Abstract]

2024 Feb:54:102058. PMID: 38681872
Acta Pharmacol Sin

Roxithromycin attenuates bleomycin-induced pulmonary fibrosis by targeting senescent cells. [Abstract]

2021 Dec;42(12):2058-2068. PMID: 33654217
Cell Chem Biol

Identifying enhancers of innate immune signaling as broad-spectrum antivirals active against emerging viruses. [Abstract]

2022 Jul 21;29(7):1113-1125.e6. PMID: 35728599
Free Radic Biol Med

3-Carbamoyl-proxyl nitroxide radicals attenuate bleomycin-induced pulmonary fibrosis in mice. [Abstract]

2021 Aug 1:171:135-142. PMID: 33989760
Br J Cancer

Fibroblast growth factor signals drive the metastatic behavior in small cell lung cancer. [Abstract]

2025 Dec 13. PMID: 41390896
Stem Cell Res Ther

Bone marrow mesenchymal stem cell-derived exosomes promote rotator cuff tendon-bone healing by promoting angiogenesis and regulating M1 macrophages in rats. [Abstract]

2020 Nov 25;11(1):496. PMID: 33239091
Br J Cancer

Nintedanib inhibits intrahepatic cholangiocarcinoma aggressiveness via suppression of cytokines extracted from activated cancer-associated fibroblasts. [Abstract]

2020 Mar;122(7):986-994. PMID: 32015511
Pharmaceutics

Development and Validation of LC-MS/MS Method for Nintedanib and BIBF 1202 Monitoring in Plasma of Patients with Progressive Pulmonary Fibrosis Associated with Systemic Sclerosis. [Abstract]

2025 Dec 2;17(12):1553. PMID: 41471068
J Ethnopharmacol

Fu-Zheng-Tong-Luo formula promotes autophagy and alleviates idiopathic pulmonary fibrosis by controlling the Janus kinase 2/signal transducer and activator of transcription 3 pathway. [Abstract]

2023 Oct 5:314:116633. PMID: 37207878
J Agric Food Chem

A Novel Polysaccharide from the Flowers of Lilium lancifolium Alleviates Pulmonary Fibrosis In Vivo and In Vitro. [Abstract]

2025 Mar 20. PMID: 40114341
Life Sci

Verbascoside and isoverbascoside ameliorate transforming growth factor β1-induced collagen expression by lung fibroblasts through Smad/non-Smad signaling pathways. [Abstract]

2022 Nov 1:308:120950. PMID: 36100079
Eur J Pharmacol

Pirfenidone and nintedanib attenuates pulmonary artery endothelial and smooth muscle cells transformations induced by IL-11. [Abstract]

2024 Jun 5:972:176547. PMID: 38561103
Int Immunopharmacol

Cucurbitacin B attenuates bleomycin-induced pulmonary fibrosis by inhibiting M2 macrophage polarization via PI3K/AKT/mTOR signaling. [Abstract]

2026 Jun 13:185:116985. PMID: 42287958
Int J Mol Sci

Nintedanib-αVβ6 Integrin Ligand Conjugates Reduce TGF β-Induced EMT in Human Non-Small Cell Lung Cancer. [Abstract]

2023 Jan 12;24(2):1475. PMID: 36674990
Int Immunopharmacol

Entrectinib ameliorates bleomycin-induced pulmonary fibrosis in mice by inhibiting TGF-β1 signaling pathway. [Abstract]

2022 Dec;113(Pt B):109427. PMID: 36375321
Int J Mol Sci

Nintedanib Inhibits Endothelial Mesenchymal Transition in Bleomycin-Induced Pulmonary Fibrosis via Focal Adhesion Kinase Activity Reduction. [Abstract]

2022 Jul 25;23(15):8193. PMID: 35897764
Am J Respir Cell Mol Biol

2026 Mar 11.
Am J Respir Cell Mol Biol

Kindlin-2 Acts as a Key Mediator of Lung Fibroblast Activation and Pulmonary Fibrosis Progression. [Abstract]

2021 Jul;65(1):54-69. PMID: 33761308
Am J Respir Cell Mol Biol

Bleomycin Induces Drug Efflux in Lungs. A Pitfall for Pharmacological Studies of Pulmonary Fibrosis. [Abstract]

2020 Feb;62(2):178-190. PMID: 31419911
Am J Respir Cell Mol Biol

Defining the Activated Fibroblast Population in Lung Fibrosis Using Single-Cell Sequencing. [Abstract]

2019 Jul;61(1):74-85. PMID: 30848683
Lung Cancer

Combination therapy with anti-programmed cell death 1 antibody plus angiokinase inhibitor exerts synergistic antitumor effect against malignant mesothelioma via tumor microenvironment modulation. [Abstract]

2023 Jun:180:107219. PMID: 37146474
ACS Omega

Nintedanib-Containing Dual Conjugates Targeting αVβ6 Integrin and Tyrosine Kinase Receptors as Potential Antifibrotic Agents. [Abstract]

2022 May 17;7(21):17658-17669. PMID: 35664627
Cancer Sci

TGF-β Inhibitor Potentiates Osimertinib-Induced Anti-Tumor Immunity in Egfr-Mutant Lung Cancer. [Abstract]

2026 Feb 27. PMID: 41757675
Sci Rep

Nintedanib inhibits growth of human prostate carcinoma cells by modulating both cell cycle and angiogenesis regulators. [Abstract]

2018 Jun 22;8(1):9540. PMID: 29934570

Nintedanib purchased from MedChemExpress. Usage Cited in: Sci Rep. 2018 Jun 22;8(1):9540. [Abstract]

Western blot based detection of cell cycle associated molecules viz., Cyclins A, D1 and E, and CDKs 2, 4 and 6 in PC3, and LNCaP cells after 72 hours of Nintedanib treatment.
J Mol Struct

2016 Jul 5; 1115:171-179.
J Cell Mol Med

Inactivation of CDK12 Enhances Mitochondrial Efficiency to Suppress DNA Damage. [Abstract]

2026 Apr;30(7):e71101. PMID: 41896195
Oncol Rep

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. [Abstract]

2016 Dec;36(6):3123-3130. PMID: 27805254

Nintedanib purchased from MedChemExpress. Usage Cited in: Oncol Rep. 2016 Dec;36(6):3123-3130. [Abstract]

The mice are treated with TFTD alone (150 mg/kg, orally twice daily from days 1 to 14, open column), or a combination of TFTD and Nintedanib (closed column). The HT-29 and HCT116 tumors are collected at 24 h following the final administration of the drugs (day 15). The values indicate the mean ± SD (n=6).
J Pharmacol Exp Ther

AK106-001616, a Potent and Selective Inhibitor of Cytosolic Phospholipase A2: In Vivo Efficacy for Inflammation, Neuropathic Pain, and Pulmonary Fibrosis. [Abstract]

2019 Jun;369(3):511-522. PMID: 30971478
J Photochem Photobiol B

Interplay of multiple interaction forces: Binding of tyrosine kinase inhibitor nintedanib with human serum albumin. [Abstract]

2016 Apr:157:70-6. PMID: 26894847
J Nat Prod

Clavukoellians A-F, Highly Rearranged Nardosinane Sesquiterpenoids with Antiangiogenic Activity from Clavularia koellikeri. [Abstract]

2019 May 24;82(5):1331-1337. PMID: 30994348
Exp Eye Res

Nintedanib and ranibizumab attenuates pathological neovascularization in a rat model of oxygen induced retinopathy. [Abstract]

2025 Feb 12:110285. PMID: 39952427
FEBS Lett

Platycodin D reduces PD-L1 levels by inhibiting LXR-β activity and combines with nintedanib to enhance the tumor-killing effect of T cells. [Abstract]

2024 Dec;598(24):3053-3070. PMID: 39428320
Exp Eye Res

The anti-scar effect of tyrosine-kinase inhibitor nintedanib in experimental glaucoma filtration surgery in rabbits. [Abstract]

2023 Apr:229:109431. PMID: 36870440
J Cell Biochem

Vascular endothelial growth factor enhances tendon-bone healing by activating Yes-associated protein for angiogenesis induction and rotator cuff reconstruction in rats. [Abstract]

2020 Mar;121(3):2343-2353. PMID: 31633245
PLoS One

A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]

2024 Nov 1;19(11):e0308647. PMID: 39485774
European J Org Chem

Nov 2022
PLoS One

Inhibitory effect of nintedanib on VEGF secretion in retinal pigment epithelial cells induced by exposure to a necrotic cell lysate. [Abstract]

2019 Aug 6;14(8):e0218632. PMID: 31386668
Fundam Clin Pharmacol

Inhibition of organic cation transporter 3 activity by tyrosine kinase inhibitors. [Abstract]

2021 Oct;35(5):919-929. PMID: 33523504
Drug Dev Ind Pharm

Nintedanib and miR-29b co-loaded lipoplexes in idiopathic pulmonary fibrosis: formulation, characterization, and in vitro evaluation. [Abstract]

2024 Aug 7:1-16. PMID: 39099436
Virology

Structure-based virtual screening of ROCK1 inhibitors for the discovery of Enterovirus-A71 antivirals. [Abstract]

2023 Aug:585:205-214. PMID: 37384967
Eur J Drug Metab Pharmacokinet

Differential Inhibition of Equilibrative Nucleoside Transporter 1 (ENT1) Activity by Tyrosine Kinase Inhibitors. [Abstract]

2021 Sep;46(5):625-635. PMID: 34275128
J Ophthalmol

BIBF1120 Protects against Diabetic Retinopathy through Neovascularization-Related Molecules and the MAPK Signaling Pathway. [Abstract]

2023 Apr 28:2023:7355039. PMID: 37152616
Respir Investig

Induced pluripotent stem cell-derived conditioned medium, as well as nintedanib, ameliorates bleomycin-induced pulmonary fibrosis via suppressing endothelial-mesenchymal transition. [Abstract]

2025 Jul 18;63(5):904-914. PMID: 40683174
Oncol Lett

Single‑agent nintedanib suppresses metastatic osteosarcoma growth by inhibiting tumor vascular formation. [Abstract]

2024 Jan 25;27(3):123. PMID: 38348384
Int J Ophthalmol

Evaluation of nintedanib as a new postoperative antiscarring agent in experimental extraocular muscle surgery. [Abstract]

2022 Jun 18;15(6):914-923. PMID: 35814898
Integr Biol (Camb)

Contracting scars from fibrin drops. [Abstract]

2022 Mar 21;14(1):1-12. PMID: 35184163
Folia Histochem Cytobiol

Nintedanib alleviates hyperoxia-induced lung injury via targeting NF-κB signalling pathway in rat model of bronchopulmonary dysplasia. [Abstract]

2025;63(2):79-87. PMID: 40421818
Curr Eye Res

Effect of Nintedanib Nanothermoreversible Hydrogel on Neovascularization in an Ocular Alkali Burn Rat Model. [Abstract]

2022 Dec;47(12):1578-1589. PMID: 36259508
bioRxiv

Modeling cell-cell interactions to advance drug discovery in Idiopathic Pulmonary Fibrosis. [Abstract]

2026 Feb 2:2026.01.29.702646. PMID: 41676623
bioRxiv

2026 Feb 20.
bioRxiv

2025 Oct 24.
bioRxiv

2025 Aug 09.
SSRN

2025 Aug 27.
University of Pittsburgh

2025.
Preprints

2025 Apr 08.
bioRxiv

2025 March 19.
medRxiv

2024 Jun 28.
bioRxiv

SON-dependent nuclear speckle rehabilitation alleviates proteinopathies. [Abstract]

2025 Apr 28:2024.04.18.590103. PMID: 38659924
bioRxiv

Aberrant activation of wound healing programs within the metastatic niche facilitates lung colonization by osteosarcoma cells. [Abstract]

2024 Sep 13:2024.01.10.575008. PMID: 38260361
SSRN

2023 May 8.
Research Square Print

September 14th, 2022.
Patent

US20220257531A1.

溶剤 & 溶解度

体外:

DMSO : 5 mg/mL (9.27 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8532 mL

9.2658 mL

18.5316 mL

5 mM

0.3706 mL

1.8532 mL

3.7063 mL

10 mM

---

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

体内:

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 10 mg/mL (18.53 mM); Suspended solution; Need ultrasonic

Protocol 2

Add each solvent one by one: 1% CMC/0.5% Tween-80 in Saline water

Solubility: 10 mg/mL (18.53 mM); Suspended solution; Need ultrasonic

プロトコル

Kinase Assay^[2]

Enzyme activity is assayed in the presence or absence of serial dilutions of BIBF1120 performed in 25% DMSO. Each microtiter plate contains internal controls such as blank, maximum reaction, and historical reference compound. All incubations are conducted at room temperature on a rotation shaker. 10 μL of each BIBF1120 dilution is added to 10 μL of diluted kinase (0.8 μg/mL VEGFR2, 10 mM Tris pH 7.5, 2 mM EDTA, and 2 mg/mL BSA) and preincubated for 1 hour. The reaction is started by addition of 30 μL of substrate mix containing 62.4 mM Tris pH 7.5, 2.7 mM DTT, 5.3 mM MnCl₂, 13.3 mM Mg-acetate, 0.42 mM ATP, 0.83 mg/mL Poly-Glu-Tyr(4:1), and 1.7 μg/mL Poly-Glu-Tyr(4:1)-biotin and incubated for 1 hour. The reaction is stopped by addition of 50 μL of 250 mM EDTA, 20 mM HEPES, pH 7.4. 90 μL of the reaction mix is transferred to a streptavidin plate and incubated for 1-2 hours. After three washes with PBS the EU-labeled antibody, PY20 is added (recommended dilution 1:2000 of 0.5 mg/mL labeled antibody in DELFIA assay buffer). Excessive detection antibody is removed by three ishes of DELFIA washing buffer. Then 10 minutes before measurement on the multilabel reader, each well is incubated with 100 μL of DELFIA enhancement solution.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[1]

Five-week-old to 6-wk-old athymic NMRI-nu/nu female mice (21-31 g) are used for the assay. After acclimatization, mice are inoculated with 1 to 5×10⁶ (in 100 μL) FaDu, Caki-1, SKOV-3, H460, HT-29, or PAC-120 cells s.c. into the right flank of the animal. After acclimatization, F344 Fischer rats are injected with 5×10⁶ (in 100 μL) GS-9L cells s.c. into the right flank of the animal. For pharmacokinetic analysis, blood is isolated at indicated time points from the retroorbital plexus of mice and plasma is analyzed using high performance liquid chromatography-mass spectrometry methodology.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

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COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[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. [Content Brief]

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8532 mL	9.2658 mL	18.5316 mL	46.3289 mL
DMSO	5 mM	0.3706 mL	1.8532 mL	3.7063 mL	9.2658 mL

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