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Purity: ≥98%
Pazopanib (formerly GW-786034; GW786034; brand name Votrient) is a novel and potent multi-kinase inhibitor with potential antitumor activity. In cell-free assays, it inhibits several kinases, including PDGFR, FGFR, c-Kit, c-Fms, VEGFR1, VEGFR2, and VEGFR3, with IC50 values of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM, and 146 nM, respectively. Vascular endothelial growth factor receptors (VEGFR)-1, -2, and -3, c-kit, and platelet-derived growth factor receptor (PDGF-R) are all specifically inhibited bypazopanib, which may prevent angiogenesis in tumors where these receptors are overexpressed. An FDA-approved medication calledpazopanib is used to treat advanced soft tissue sarcomas and advanced/metastatic renal cell carcinomas.
| Targets |
VEGFR1 (IC50 = 10 nM); VEGFR2 (IC50 = 30 nM); VEGFR3 (IC50 = 47 nM); PDGFRβ (IC50 = 84 nM); FGFR1 (IC50 = 140 nM); c-Kit (IC50 = 74 nM); c-Fms (IC50 = 146 nM)
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| Enzyme Assay |
In 384-well microtiter plates, homogeneous time-resolved fluorescence (HTRF) VEGFR enzyme assays for VEGGR1, VEGFR2, and VEGFR3 are conducted using a purified, baculovirus-expressed glutathione-S-transferase (GST) fusion protein that encodes the catalytic c-terminus of human VEGFR receptor kinases 1, 2, or 3. The reactions commence with the addition of 10 μL of activated VEGFR2 kinase solution [final concentration: 1 nM enzyme in 0.1 M HEPES, pH 7.5, containing 0.1 mg/mL bovine serum albumin (BSA), 300 μM dithiothreitol (DTT)] to 10 μL of substrate solution [final concentration: 360 nM peptide, (biotin-aminohexyl-EEEEYFELVAKKKK-NH2), 75 μM ATP, 10 μM MgCl2], and 1 μL of titrated Pazopanib in DMSO]. After incubating the plates for 60 minutes at room temperature, 20 μL of 100 mM ethylene diamine tetraacetic acid (EDTA) is added to quench the reaction. Following the quenching process, 20 μL of HTRF reagents (final concentration: 15 nM Streptavidin-linked allophycocyanin, 1 nM antiphosphotyrosine antibody labeled in 0.1 mg/mL BSA, 0.1 M HEPES, pH 7.5) are added, and the plates are then incubated for a minimum of 10 minutes. With a 50 μs time delay, the fluorescence at 665 nM is measured using a Wallac Victor plate reader.
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| Cell Assay |
Using commercially available kits, the 5-bromo-2-deoxyuridine (BrdU) incorporation method is used to measure the impact of Pazopanib on cell proliferation. In 96-well plates coated with type 1 collagen, HUVEC are seeded in a medium containing 5% fetal bovine serum (FBS) and incubated for an entire night at 37°C with 5% CO2. After the medium is removed from the cells, each well is filled with different concentrations of Pazopanib in serum-free medium. Either VEGF (10 ng/mL) or bFGF (0.3 ng/mL) is added to the wells after 30 minutes. After an extra 72 hours of incubation, cells receive an addition of BrdU (10 μM) for the final 18 to 24 hours of incubation. ELISA is used to measure the amount of BrdU incorporated into cells at the end of incubation. A curve that fits the data is given by the formula y=Vmax(1−(x/(K+x))), where K is the IC50.
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| Animal Protocol |
Mice: In 8–12 week old nude mice, tumors are started by injecting tumor cell suspension. After tumors grow to a volume of 100–200 mm3, mice are randomly assigned to eight-groups. Pazopanib is given at 10, 30, or 100 mg/kg once or twice a day. When the study is over, the animals are put to death by breathing in CO2. Tumor volume (mm3) = (length×width2)/2 is the equation used to measure tumor volume twice a week using calipers. % inhibition=1−(average growth of the drug-treated population/average growth of the vehicle-treated control population) is a common way to report results.
Rats: Brown man from Norway Prior to any experimental procedure, 200–250 g pigmented rats, or BN rats, are acclimatized for at least two days. An intraperitoneal injection of 30 mg/mL streptozotocin solution in 10 mM citrate buffer (pH 4.5) is given (60 mg/kg body weight) to induce diabetes after an overnight fasting period of 12–16 hours. The animals are fed a regular diet after receiving a streptozotocin injection for 3–4 hours, and a blood sample (5–10 μL) is drawn via a tail vein 24 hours later. A glucose monitor is used to measure the blood glucose levels in the animals. Animals classified as diabetics have blood glucose levels higher than 250 mg/dL. Three groupings of animals are created. Group 1: Healthy (n = 12), Group 2: Diabetic (n = 12), and Group 3: Diabetic+Treatment (n = 12). Upon induction of diabetes, treatment is initiated promptly. On day 31, 16–17 hours after the last dose on day 30, animals in all groups are sacrificed. Both eyes are dosed twice daily for 30 days with 0.5% w/v Pazopanib suspension (10 μL volume in each eye). |
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| References |
| Molecular Formula |
C21H23N7O2S
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| Molecular Weight |
437.52
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| Exact Mass |
437.16
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| Elemental Analysis |
C, 57.65; H, 5.30; N, 22.41; O, 7.31; S, 7.33
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| CAS # |
444731-52-6
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| Related CAS # |
Pazopanib Hydrochloride;635702-64-6;Pazopanib-d6;1219592-01-4;Pazopanib-13C,d3;1261734-88-6
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| Appearance |
white solid powder
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| 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
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| InChi Key |
CUIHSIWYWATEQL-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
5-[[4-[(2,3-dimethylindazol-6-yl)-methylamino]pyrimidin-2-yl]amino]-2-methylbenzenesulfonamide
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| Synonyms |
GW-78603; GW78603; GW 78603; GW-786034; GW786034; GW 786034; Pazopanib; trade name: Votrient
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.71 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.71 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: ≥ 0.43 mg/mL (0.98 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 0.43 mg/mL (0.98 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2856 mL | 11.4280 mL | 22.8561 mL | |
| 5 mM | 0.4571 mL | 2.2856 mL | 4.5712 mL | |
| 10 mM | 0.2286 mL | 1.1428 mL | 2.2856 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01767636 | Active Rrecruiting |
Drug: Pazopanib Hydrochloride | Stage IV Renal Cell Cancer Kidney Oncocytoma |
Mayo Clinic | May 16, 2013 | Phase 2 |
| NCT03260894 | Active Rrecruiting |
Drug: Pazopanib Drug: Sunitinib |
Renal Cell Carcinoma (RCC) |
Incyte Corporation | December 7, 2017 | Phase 3 |
| NCT01217931 | Active Rrecruiting |
Drug: Pazopanib Drug: Bevacizumab |
Kidney Cancer | M.D. Anderson Cancer Center | January 19, 2011 | Phase 2 |
| NCT01575548 | Active Rrecruiting |
Other: Placebo Administration Drug: Pazopanib |
Clear Cell Renal Cell Carcinoma Stage IV Renal Cell Cancer AJCC v7 |
National Cancer Institute (NCI) |
August 8, 2012 | Phase 3 |
| NCT02180867 | Active Rrecruiting |
Drug: Pazopanib Drug: Pazopanib Hydrochloride |
Liposarcoma Leiomyosarcoma |
National Cancer Institute (NCI) |
July 11, 2014 | Phase 2 Phase 3 |
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