Nintedanib esylate
Based on 75 publication(s) in Google Scholar
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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.96%
- CAS. Nr.: 656247-18-6
- Formel: C33H39N5O7S
- Molecular Weight:649.76
-
Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Publications Citing Use of MedChemExpress (MCE) Nintedanib esylate
More- Nature. 2026 Jan;649(8098):1032-1041. [Abstract]
- Science. 2026 Feb 5;391(6785):eadz4075. [Abstract]
- Nat Mach Intell. 2020 Jun.
- Eur Respir J. 2025 Jun 5;65(6):2400615. [Abstract]
- Bioact Mater. 2023 Nov 22:33:262-278. [Abstract]
- Sci Transl Med. 2022 Sep 28;14(664):eabo5070. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Sci Adv. 2022 Jun 17;8(24):eabn4564. [Abstract]
- Biomaterials.
- Cell Death Dis. 2025 Apr 11;16(1):278. [Abstract]
- Small. 2024 Nov;20(45):e2403428. [Abstract]
- J Exp Med. 2025 Aug 4;222(8):e20241174. [Abstract]
- Phytomedicine. 2026 Sep:159:158568.
- Nano Today. 2024 Feb:54:102058. [Abstract]
- Acta Pharmacol Sin. 2021 Dec;42(12):2058-2068. [Abstract]
- Cell Chem Biol. 2022 Jul 21;29(7):1113-1125.e6. [Abstract]
- Free Radic Biol Med. 2021 Aug 1:171:135-142. [Abstract]
- Br J Cancer. 2025 Dec 13. [Abstract]
- Stem Cell Res Ther. 2020 Nov 25;11(1):496. [Abstract]
- Br J Cancer. 2020 Mar;122(7):986-994. [Abstract]
- Pharmaceutics. 2025 Dec 2;17(12):1553. [Abstract]
- J Ethnopharmacol. 2023 Oct 5:314:116633. [Abstract]
- J Agric Food Chem. 2025 Mar 20. [Abstract]
- Life Sci. 2022 Nov 1:308:120950. [Abstract]
- Eur J Pharmacol. 2024 Jun 5:972:176547. [Abstract]
- Int Immunopharmacol. 2026 Jun 13:185:116985. [Abstract]
- Int J Mol Sci. 2023 Jan 12;24(2):1475. [Abstract]
- Int Immunopharmacol. 2022 Dec;113(Pt B):109427. [Abstract]
- Int J Mol Sci. 2022 Jul 25;23(15):8193. [Abstract]
- Am J Respir Cell Mol Biol. 2026 Mar 11.
- Am J Respir Cell Mol Biol. 2021 Jul;65(1):54-69. [Abstract]
- Am J Respir Cell Mol Biol. 2020 Feb;62(2):178-190. [Abstract]
- Am J Respir Cell Mol Biol. 2019 Jul;61(1):74-85. [Abstract]
- Lung Cancer. 2023 Jun:180:107219. [Abstract]
- ACS Omega. 2022 May 17;7(21):17658-17669. [Abstract]
- Cancer Sci. 2026 Feb 27. [Abstract]
- Sci Rep. 2018 Jun 22;8(1):9540. [Abstract]
- J Mol Struct. 2016 Jul 5; 1115:171-179.
- J Cell Mol Med. 2026 Apr;30(7):e71101. [Abstract]
- Oncol Rep. 2016 Dec;36(6):3123-3130. [Abstract]
- J Pharmacol Exp Ther. 2019 Jun;369(3):511-522. [Abstract]
- J Photochem Photobiol B. 2016 Apr:157:70-6. [Abstract]
- J Nat Prod. 2019 May 24;82(5):1331-1337. [Abstract]
- Exp Eye Res. 2025 Apr:253:110285. [Abstract]
- FEBS Lett. 2024 Dec;598(24):3053-3070. [Abstract]
- Exp Eye Res. 2023 Apr:229:109431. [Abstract]
- J Cell Biochem. 2020 Mar;121(3):2343-2353. [Abstract]
- PLoS One. 2024 Nov 1;19(11):e0308647. [Abstract]
- European J Org Chem. Nov 2022
- PLoS One. 2019 Aug 6;14(8):e0218632. [Abstract]
- Fundam Clin Pharmacol. 2021 Oct;35(5):919-929. [Abstract]
- Drug Dev Ind Pharm. 2024 Jul;50(7):671-686. [Abstract]
- Virology. 2023 Aug:585:205-214. [Abstract]
- Eur J Drug Metab Pharmacokinet. 2021 Sep;46(5):625-635. [Abstract]
- J Ophthalmol. 2023 Apr 28:2023:7355039. [Abstract]
- Respir Investig. 2025 Jul 18;63(5):904-914. [Abstract]
- Oncol Lett. 2024 Jan 25;27(3):123. [Abstract]
- Int J Ophthalmol. 2022 Jun 18;15(6):914-923. [Abstract]
- Integr Biol (Camb). 2022 Mar 21;14(1):1-12. [Abstract]
- Folia Histochem Cytobiol. 2025;63(2):79-87. [Abstract]
- Curr Eye Res. 2022 Dec;47(12):1578-1589. [Abstract]
- bioRxiv. 2026 Feb 2:2026.01.29.702646. [Abstract]
- bioRxiv. 2026 Feb 20.
- bioRxiv. 2025 Oct 24.
- bioRxiv. 2025 Aug 09.
- SSRN. 2025 Aug 27.
- University of Pittsburgh. 2025.
- bioRxiv. 2025 Apr 28:2024.04.18.590103. [Abstract]
- Preprints. 2025 Apr 08.
- bioRxiv. 2025 March 19.
- medRxiv. 2024 Jun 28.
- bioRxiv. 2024 Sep 13:2024.01.10.575008. [Abstract]
- SSRN. 2023 May 8.
- Research Square Print. September 14th, 2022.
- Patent. US20220257531A1.
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Cell Imaging/Staining
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Cell Proliferation/Viability Assay
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WB
Alle VEGFR Isoform-spezifische Produkte anzeigen
More
Biologische Aktivität
Beschreibung
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) |
In Vitro
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. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 656247-18-6
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Appearance Solid
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Molecular Weight 649.76
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Formel C33H39N5O7S
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Color Light yellow to green yellow
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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
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Synonyms
BIBF 1120 esylate
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (75)
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Journal Impact Factor
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Most Recent
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Nature
2026 Jan;649(8098):1032-1041. PMID: 41299171 -
Science
2026 Feb 5;391(6785):eadz4075. PMID: 41643022 -
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Eur Respir J
Inhibition of AXL ameliorates pulmonary fibrosis via attenuation of M2 macrophage polarization. [Abstract]2025 Jun 5;65(6):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 esylate 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 esylate 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.
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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 esylate 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 esylate 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.
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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 -
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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 Nov;20(45):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 -
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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 -
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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 esylate 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.
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J Cell Mol Med
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 esylate 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).
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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 Apr:253:110285. 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 -
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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
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 Jul;50(7):671-686. 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)
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 -
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bioRxiv
2025 Apr 28:2024.04.18.590103. PMID: 38659924 -
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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 -
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Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 66.67 mg/mL (102.61 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 16.67 mg/mL (25.66 mM; Need ultrasonic)
Ethanol : 3.08 mg/mL (4.74 mM; Need ultrasonic)
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (3.85 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Reinheit & Dokumentation
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Data Sheet (283 KB)
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SDS (623 KB)
- English - EN (623 KB)
- Français - FR (623 KB)
- Deutsch - DE (623 KB)
- Norwegian - NO (623 KB)
- Español - ES (623 KB)
- Swedish - SV (623 KB)
- Italian - IT (623 KB)
- Korean - KR (623 KB)
- Portuguese - PT (623 KB)
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Handling Instructions (2659 KB)
Verweise
[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]. 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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| Ethanol / H2O / DMSO | 1 mM | 1.5390 mL | 7.6951 mL | 15.3903 mL | 38.4757 mL |
| H2O / DMSO | 5 mM | 0.3078 mL | 1.5390 mL | 3.0781 mL | 7.6951 mL |
| 10 mM | 0.1539 mL | 0.7695 mL | 1.5390 mL | 3.8476 mL | |
| 15 mM | 0.1026 mL | 0.5130 mL | 1.0260 mL | 2.5650 mL | |
| 20 mM | 0.0770 mL | 0.3848 mL | 0.7695 mL | 1.9238 mL | |
| 25 mM | 0.0616 mL | 0.3078 mL | 0.6156 mL | 1.5390 mL | |
| DMSO | 30 mM | 0.0513 mL | 0.2565 mL | 0.5130 mL | 1.2825 mL |
| 40 mM | 0.0385 mL | 0.1924 mL | 0.3848 mL | 0.9619 mL | |
| 50 mM | 0.0308 mL | 0.1539 mL | 0.3078 mL | 0.7695 mL | |
| 60 mM | 0.0257 mL | 0.1283 mL | 0.2565 mL | 0.6413 mL | |
| 80 mM | 0.0192 mL | 0.0962 mL | 0.1924 mL | 0.4809 mL | |
| 100 mM | 0.0154 mL | 0.0770 mL | 0.1539 mL | 0.3848 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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