BIBF 1202VEGFR/PDGFR/FGFR inhibitor CAS# 894783-71-2 |
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Quality Control & MSDS
3D structure
Package In Stock
Number of papers citing our products
| Cas No. | 894783-71-2 | SDF | Download SDF |
| PubChem ID | 11606145 | Appearance | Powder |
| Formula | C30H31N5O4 | M.Wt | 525.6 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : ≥ 45 mg/mL (85.62 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | (3Z)-3-[[4-[methyl-[2-(4-methylpiperazin-1-yl)acetyl]amino]anilino]-phenylmethylidene]-2-oxo-1H-indole-6-carboxylic acid | ||
| SMILES | CN1CCN(CC1)CC(=O)N(C)C2=CC=C(C=C2)NC(=C3C4=C(C=C(C=C4)C(=O)O)NC3=O)C5=CC=CC=C5 | ||
| Standard InChIKey | KEHNCEDHZGQSNP-DQSJHHFOSA-N | ||
| Standard InChI | InChI=1S/C30H31N5O4/c1-33-14-16-35(17-15-33)19-26(36)34(2)23-11-9-22(10-12-23)31-28(20-6-4-3-5-7-20)27-24-13-8-21(30(38)39)18-25(24)32-29(27)37/h3-13,18,31H,14-17,19H2,1-2H3,(H,32,37)(H,38,39)/b28-27- | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | BIBF 1202 is the carboxylate metabolite of BIBF 1120 which inhibits VEGFR2 kinase with an IC50 of 62 nM.In Vitro:The major metabolic pathway for BIBF 1120 is methyl ester cleavage to BIBF 1202. Subsequently, the free carboxyl group of BIBF 1202 is glucuronidated to 1-O-acylglucuronide[2]. References: | |||||
BIBF 1202 Dilution Calculator
BIBF 1202 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.9026 mL | 9.5129 mL | 19.0259 mL | 38.0518 mL | 47.5647 mL |
| 5 mM | 0.3805 mL | 1.9026 mL | 3.8052 mL | 7.6104 mL | 9.5129 mL |
| 10 mM | 0.1903 mL | 0.9513 mL | 1.9026 mL | 3.8052 mL | 4.7565 mL |
| 50 mM | 0.0381 mL | 0.1903 mL | 0.3805 mL | 0.761 mL | 0.9513 mL |
| 100 mM | 0.019 mL | 0.0951 mL | 0.1903 mL | 0.3805 mL | 0.4756 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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IC50: 20–100 nmol/L for VEGFR, PDGFR and FGFR (BIBF 1120)
Inhibition of tumor angiogenesis through blockade of the vascular endothelial growth factor (VEGF) signaling pathway is a novel treatment modality in oncology. BIBF 1120 is an indolinone derivative blocking VEGFR, PDGFR and FGFR kinase activity in enzymatic assays. BIBF 1202 is the major in-vivo metabolite of BIBF 1120.
In vitro: BIBF 1120 inhibits mitogen-activated protein kinase and Akt signaling pathways mainly via interacting with VEGF, PDGFR and FGFR in three types of cell contributing to angiogenesis, endothelial cells, pericytes, and smooth muscle cells, leading to the inhibition of cell proliferation (EC50, 10–80 nmol/L) and apoptosis [1].
In vivo: In tumor models tested, including human tumor xenografts growing in nude mice and a syngeneic rat tumor model, BIBF 1120 is proven to be active at well-tolerated doses (25–100 mg/kg daily p.o.), as measured by MRI of tumor perfusion after 3 days, reducing vessel density and vessel integrity after 5 days, and inducing profound growth inhibition [1].
Clinical trials: Patients with locally advanced or metastatic relapsed NSCLC in whom first- or second-line platinum-based chemotherapy failed were randomly allocated to daily 250 mg BIBF 1120 b.i.d. or 150 mg BIBF 1120 b.i.d. Median PFS was 6.9 weeks, with no significant difference between treatment arms. Median overall survival (OS) was 21.9 weeks. BIBF 1120 displayed dose-linear pharmacokinetic characteristics. Continuous treatment with BIBF 1120 was well tolerated, and with no difference in efficacy between treatment arms [2].
References:
[1] Frank Hilberg, Gerald J. Roth, Martin Krssak, Susanna Kautschitsch, Wolfgang Sommergruber, Ulrike Tontsch-Grunt, Pilar Garin-Chesa, Gerd Bader, Andreas Zoephel, Jens Quant, Armin Heckel, and Wolfgang J. Rettig. BIBF 1120: Triple Angiokinase Inhibitor with Sustained Receptor Blockade and Good Antitumor Efficacy. Cancer Res 2008;68(12):4774–82
[2] Reck M, Kaiser R, Eschbach C, Stefanic M, Love J, Gatzemeier U, Stopfer P, von Pawel J. A phase II double-blind study to investigate efficacy and safety of two doses of the triple angiokinase inhibitor BIBF 1120 in patients with relapsed advanced non-small-cell lung cancer. Ann Oncol. 2011 Jun;22(6):1374-81.
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Simultaneous determination of nintedanib and its metabolite BIBF 1202 in different tissues of mice by UPLC-MS/MS and its application in drug tissue distribution study.[Pubmed:26342166]
J Chromatogr B Analyt Technol Biomed Life Sci. 2015 Oct 1;1002:239-44.
A sensitive and rapid ultra performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) method was developed to simultaneous determine nintedanib and BIBF 1202 in mice plasma and tissue using carbamazepine as the internal standard (IS). Sample preparation was accomplished through a protein precipitation procedure with acetonitrile. The analyte and IS were separated on an Acquity UPLC BEH C18 column (2.1mmx50mm, 1.7mum) with the mobile phase of acetonitrile and 0.1% formic acid in water with gradient elution at a flow rate of 0.40mL/min. The detection was performed on a triple quadrupole tandem mass spectrometer equipped with electrospray ionization (ESI) by multiple reactions monitoring (MRM) of the transitions at m/z 540.3-->113.1 for nintedanib, m/z 526.3-->113.1 for BIBF 1202 and m/z 237.1-->194.1 for IS, respectively. The linearity of this method was found to be within the concentration range of 1-1000ng/mL with a lower limit of quantification of 1.0ng/mL for each drug. Only 3.0min was needed for an analytical run. The inter-day and intra-day precision and accuracy of quality control (QC) samples, evaluated both in plasma and tissue homogenates, were all within 15%. The method was successfully applied to the pharmacokinetic and tissue distribution study of nintedanib and BIBF 1202 in mice after oral administration of nintedanib.
