Pazopanib (GW-786034)VEGFR/PDGFR/FGFR inhibitor CAS# 444731-52-6 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 444731-52-6 | SDF | Download SDF |
| PubChem ID | 10113978 | Appearance | Powder |
| Formula | C21H23N7O2S | M.Wt | 437.52 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | GW786034 | ||
| Solubility | DMSO : ≥ 43 mg/mL (98.28 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 5-[[4-[(2,3-dimethylindazol-6-yl)-methylamino]pyrimidin-2-yl]amino]-2-methylbenzenesulfonamide | ||
| SMILES | CC1=C(C=C(C=C1)NC2=NC=CC(=N2)N(C)C3=CC4=NN(C(=C4C=C3)C)C)S(=O)(=O)N | ||
| Standard InChIKey | CUIHSIWYWATEQL-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C21H23N7O2S/c1-13-5-6-15(11-19(13)31(22,29)30)24-21-23-10-9-20(25-21)27(3)16-7-8-17-14(2)28(4)26-18(17)12-16/h5-12H,1-4H3,(H2,22,29,30)(H,23,24,25) | ||
| 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 | Pazopanib is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM, respectively. | ||||||
| Targets | VEGFR1 | VEGFR2 | VEGFR3 | PDGFR | FGFR | ||
| IC50 | 10 nM | 30 nM | 47 nM | 84 nM | 74 nM | ||
| Cell experiment: [1] | |
| Cell lines | Primary human brain microvascular endothelial cells (HBMEC) |
| Preparation method | The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
| Reacting condition | IC50: 2 μM, 48 hours |
| Applications | The IC50 for pazopanib for anchorage-dependent growth was 2 μM and 1 μM after 48 h and 72 h, respectively. Pazopanib abrogated the phosphorylation of VEGFR2 with disruption of downstream PLCγ1. It also disrupted the Ras-Raf-ERK pathway through decreased phosphorylated MEK1/2 and ERK1/2 and affected the phosphorylation of 70S6K. Our findings confirmed that pazopanib targeted endothelial cells, affecting cell growth, VEGFR-induced signaling, and tube formation. |
| Animal experiment: [2] | |
| Animal models | Immune-deficient beige-nude-xid (BNX) mice injected with MM.1S cells |
| Dosage form | Oral administration, 30 mg/kg and 100 mg/kg, daily for five weeks |
| Application | Tumor growth in treated mice was significantly delayed (30 mg/kg) or almost totally inhibited (100 mg/kg) compared with the control group. However, tumors rapidly regrew after cessation of treatment at day 30. Using Kaplan–Meier and log-rank analysis, the mean overall survival (OS) was 20 days in the control cohort versus 41 days and 51 days in groups treated with 30 mg/kg and 100 mg/kg pazopanib, respectively. Statistically significant prolongation in mean OS compared with control mice was observed in animals treated with 30 mg/kg and 100 mg/kg. Importantly, treatment with either the vehicle alone or pazopanib did not affect body weight. |
| Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
| References: [1] Gril B, Palmieri D, Qian Y, et al. Pazopanib reveals a role for tumor cell B-Raf in the prevention of HER2+ breast cancer brain metastasis. Clinical Cancer Research, 2011, 17(1): 142-153. [2] Podar K, Tonon G, Sattler M, et al. The small-molecule VEGF receptor inhibitor pazopanib (GW786034B) targets both tumor and endothelial cells in multiple myeloma. Proceedings of the National Academy of Sciences, 2006, 103(51): 19478-19483. | |
Pazopanib (GW-786034) Dilution Calculator
Pazopanib (GW-786034) Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.2856 mL | 11.428 mL | 22.8561 mL | 45.7122 mL | 57.1402 mL |
| 5 mM | 0.4571 mL | 2.2856 mL | 4.5712 mL | 9.1424 mL | 11.428 mL |
| 10 mM | 0.2286 mL | 1.1428 mL | 2.2856 mL | 4.5712 mL | 5.714 mL |
| 50 mM | 0.0457 mL | 0.2286 mL | 0.4571 mL | 0.9142 mL | 1.1428 mL |
| 100 mM | 0.0229 mL | 0.1143 mL | 0.2286 mL | 0.4571 mL | 0.5714 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. | |||||
Abstract
Due to recent approval for the treatment of STS, a retrospective analysis of pazopanib in STS has been conducted.
Abstract
The acceptable dose of oral pazopani is to be identified in order to investigate AMD.
Abstract
Pazopanib is a substrate for ATP-binding cassette family transporter that exhibits anti-gynecological cancer activity in combination with metronomic topotecan.
Abstract
Due to a progression-free survival observed in previous studies, pazopanib and sunitinib have been assessed for efficacy and safety in a randomized trial.
Abstract
The dual pathway blockade by tyrosine kinase inhibitors was examined.
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Pazopanib is a potent and selective second generation multi-targeted receptor tyrosine kinase inhibitor of vascular endothelial growth factor receptor (VEGFR), platelet-derived growth factor receptor (PDGFR) and c-kit tyrosine kinases. It is involved in inhibiting signaling pathways, angiogenesis, and cell proliferation. Pazopanib exhibited excellent anti-angiogenic and anti-tumor activity and synergism was observed in combination with chemotherapeutic drugs in several mouse models of a variety of tumors, accompanied by desirable pharmacokinetics and oral bioavailability. It inhibits the intracellular tyrosine kinase portion of all the VEGFR subtypes, and exhibits distinct pharmacokinetic and toxicity profiles compared with other agents among VEGF signaling pathway inhibitors. Recent studies elucidated its importance of signaling cascades related to angiogenesis in the management of RCC.
Reference
Sonpavde G, Hutson T E. Pazopanib: a novel multitargeted tyrosine kinase inhibitor. Current oncology reports. 2007; 9(2): 115 - 119.
Podar K, Tonon G, Sattler M, et al. The small-molecule VEGF receptor inhibitor pazopanib (GW786034B) targets both tumor and endothelial cells in multiple myeloma. Proceedings of the National Academy of Sciences. 2006; 103(51): 19478 - 19483.
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Determination of pazopanib (GW-786034) in mouse plasma and brain tissue by liquid chromatography-tandem mass spectrometry (LC/MS-MS).[Pubmed:22749591]
J Chromatogr B Analyt Technol Biomed Life Sci. 2012 Jul 15;901:85-92.
A simple, rapid and sensitive liquid chromatography-tandem mass spectrometric (LC/MS-MS) method has been developed and validated for the quantitative determination of pazopanib in mouse plasma and brain tissue homogenate. Single liquid-liquid extraction step with ethyl acetate was employed for analysis of pazopanib and the internal standard (IS); vandetanib. HPLC separation was performed on an XTerra((R)) MS C18 column 50 mm x 4.6 mm, 5.0 mum. The mobile phase consisted of 70% acetonitrile and 30% water with 0.1% formic acid, pumped at a flow rate of 0.25 ml/min. Analysis time was 3.5 min per run and both the analyte and IS eluted within 1.8-2.0 min. Multiple reactions monitoring (MRM) mode was utilized to detect the compounds of interest. The mass spectrometer was operated in the positive ion mode for detection. The precursor to product ions (Q1-->Q3) selected for pazopanib and internal standard during quantitative optimization were (m/z) 438.1-->357.2 and 475.0-->112.2 respectively. The calibration curves were linear over the range of 3.9-1000 ng/ml in both biological matrices. Lower limit of quantification (LLOQ) for mouse plasma and brain tissue was 3.9 ng/ml. The values for inter and intra day precision and accuracy were well within the ranges acceptable for analytical assessment (<15%). This method was applied to determine brain to plasma concentration ratio and relevant pharmacokinetic parameters of pazopanib after a single intravenous dose of 5 mg/kg in FVB wild type mice.
