Pazopanib HydrochlorideVEGFR/PDGFR/FGFR/c-Kit/ c-Fms inhibitor CAS# 635702-64-6 |
- SKLB610
Catalog No.:BCC3647
CAS No.:1125780-41-7
- JANEX-1
Catalog No.:BCC1668
CAS No.:202475-60-3
- WHI-P154
Catalog No.:BCC2202
CAS No.:211555-04-3
- Sunitinib malate
Catalog No.:BCC3664
CAS No.:341031-54-7
- Vandetanib hydrochloride
Catalog No.:BCC2028
CAS No.:524722-52-9
Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
Cas No. | 635702-64-6 | SDF | Download SDF |
PubChem ID | 11525740 | Appearance | Powder |
Formula | C21H24ClN7O2S | M.Wt | 473.98 |
Type of Compound | N/A | Storage | Desiccate at -20°C |
Synonyms | GW786034 | ||
Solubility | DMSO : 10 mg/mL (21.10 mM; Need ultrasonic) | ||
Chemical Name | 5-[[4-[(2,3-dimethylindazol-6-yl)-methylamino]pyrimidin-2-yl]amino]-2-methylbenzenesulfonamide;hydrochloride | ||
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.Cl | ||
Standard InChIKey | MQHIQUBXFFAOMK-UHFFFAOYSA-N | ||
Standard InChI | InChI=1S/C21H23N7O2S.ClH/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);1H | ||
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. |
||
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. |
||
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 (GW786034) 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 |
Pazopanib Hydrochloride Dilution Calculator
Pazopanib Hydrochloride Molarity Calculator
1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
1 mM | 2.1098 mL | 10.549 mL | 21.0979 mL | 42.1959 mL | 52.7448 mL |
5 mM | 0.422 mL | 2.1098 mL | 4.2196 mL | 8.4392 mL | 10.549 mL |
10 mM | 0.211 mL | 1.0549 mL | 2.1098 mL | 4.2196 mL | 5.2745 mL |
50 mM | 0.0422 mL | 0.211 mL | 0.422 mL | 0.8439 mL | 1.0549 mL |
100 mM | 0.0211 mL | 0.1055 mL | 0.211 mL | 0.422 mL | 0.5274 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. |
Calcutta University
University of Minnesota
University of Maryland School of Medicine
University of Illinois at Chicago
The Ohio State University
University of Zurich
Harvard University
Colorado State University
Auburn University
Yale University
Worcester Polytechnic Institute
Washington State University
Stanford University
University of Leipzig
Universidade da Beira Interior
The Institute of Cancer Research
Heidelberg University
University of Amsterdam
University of Auckland
TsingHua University
The University of Michigan
Miami University
DRURY University
Jilin University
Fudan University
Wuhan University
Sun Yat-sen University
Universite de Paris
Deemed University
Auckland University
The University of Tokyo
Korea University
Pazopanib HCl is a receptor tyrosine kinase inhibitor that targets multiple kinases, including VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit, and c-Fms, with IC50s 10nM, 30nM, 47nM, 84nM, 74nM, 140nM, and 146nM respectively [1-3]. Pazopanib inhibits both tumor growth and angiogenesis through suppressing these targets. In preclinical studies, it has shown anti-tumor activity against several human tumor xenografts, including renal, prostate, colon, lung, melanoma, head and neck, and breast cancer [4]. It also showed desirable pharmacokinetics and oral bioavailability in animal models [4].
Pazopanib has been approved for advanced/metastatic renal cell carcinoma and advanced soft tissue sarcomas by multiple regulatory administrations worldwide, including FDA, EMA, MHRA and TGA. In the clinical trial for soft tissue sarcomas, Pazopanib improved median progression-free survival (PFS) to 4.6 months compared to 1.6 months for patients receiving placebo [5]. In the trial for renal cell carcinoma, Pazopanib increased the median PFS from 4.2 monthe (placebo) to 9.2 months [5]. The most common adverse effect of Pazopanib were diarrhea, hypertension, hair color change, nausea, fatigue, anorexia, and vomiting [6].
References:
1. Verweij J, Sleijfer S. Pazopanib, a new therapy for metastatic soft tissue sarcoma. Expert Opin Pharmacother 2013; 14: 929-935.
2. Pick AM, Nystrom KK. Pazopanib for the treatment of metastatic renal cell carcinoma. Clin Ther 2012; 34: 511-520.
3. Bukowski RM, Yasothan U, Kirkpatrick P. Pazopanib. Nat Rev Drug Discov 2010; 9: 17-18.
4. Sonpavde G, Hutson TE. Pazopanib: a novel multitargeted tyrosine kinase inhibitor. Curr Oncol Rep 2007; 9: 115-119.
5. http://www.cancer.gov/cancertopics/druginfo/fda-pazopanibhydrochloride
6. http://www.gsksource.com/gskprm/en/US/adirect/gskprm?cmd=ProductDetailPage&product_id=1336067580985&featureKey=603422
- Microhelenin C
Catalog No.:BCN7977
CAS No.:63569-07-3
- 8-Benzoyl-5,7-dihydroxy-2,2-dimethylchromane
Catalog No.:BCN1389
CAS No.:63565-07-1
- Rebaudioside C
Catalog No.:BCN2404
CAS No.:63550-99-2
- Adrafinil
Catalog No.:BCC4166
CAS No.:63547-13-7
- 24,25-Dihydroxydammar-20-en-3-one
Catalog No.:BCN4174
CAS No.:63543-53-3
- 24,25-Epoxydammar-20(21)-en-3-one
Catalog No.:BCN4173
CAS No.:63543-52-2
- LY404039
Catalog No.:BCC4592
CAS No.:635318-11-5
- 4,2'-Dihydroxy-4'-methoxychalcone
Catalog No.:BCN7704
CAS No.:63529-06-6
- Bilirubin
Catalog No.:BCN1047
CAS No.:635-65-4
- ANR 94
Catalog No.:BCC7815
CAS No.:634924-89-3
- Lithospermoside
Catalog No.:BCN1270
CAS No.:63492-69-3
- WAY-100635 maleate salt
Catalog No.:BCC2054
CAS No.:634908-75-1
- Darunavir Ethanolate
Catalog No.:BCC5627
CAS No.:635728-49-3
- Foscarnet Sodium
Catalog No.:BCC4782
CAS No.:63585-09-1
- Terazosin
Catalog No.:BCC5162
CAS No.:63590-64-7
- 6-Hydroxydopamine hydrobromide
Catalog No.:BCC7403
CAS No.:636-00-0
- D-(+)-Maltose monohydrate
Catalog No.:BCN8423
CAS No.:6363-53-7
- DADLE
Catalog No.:BCC6064
CAS No.:63631-40-3
- Coniferyl ferulate
Catalog No.:BCN8543
CAS No.:63644-62-2
- 1,5-Bis(4-hydroxy-3-methoxyphenyl)penta-1,4-diene
Catalog No.:BCN1388
CAS No.:63644-68-8
- Gamma-Methoxyisoeugenol
Catalog No.:BCN3999
CAS No.:63644-71-3
- Z-D-Glu-OH
Catalog No.:BCC2775
CAS No.:63648-73-7
- Betaxolol HCl
Catalog No.:BCC4343
CAS No.:63659-19-8
- H-Lys(Z)-OBzl.HCl
Catalog No.:BCC2987
CAS No.:6366-70-7
Analytical control of genotoxic impurities in the pazopanib hydrochloride manufacturing process.[Pubmed:19427156]
J Pharm Biomed Anal. 2009 Sep 8;50(2):144-50.
Pharmaceutical regulatory agencies are increasingly concerned with trace-level genotoxic impurities in drug substances, requiring manufacturers to deliver innovative approaches for their analysis and control. The need to control most genotoxic impurities in the low ppm level relative to the active pharmaceutical ingredient (API), combined with the often reactive and labile nature of genotoxic impurities, poses significant analytical challenges. Therefore, sophisticated analytical methodologies are often developed to test and control genotoxic impurities in drug substances. From a quality-by-design perspective, product quality (genotoxic impurity levels in this case) should be built into the manufacturing process. This necessitates a practical analysis and control strategy derived on the premise of in-depth process understanding. General guidance on how to develop strategies for the analysis and control of genotoxic impurities is currently lacking in the pharmaceutical industry. In this work, we demonstrate practical examples for the analytical control of five genotoxic impurities in the manufacturing process of Pazopanib Hydrochloride, an anticancer drug currently in Phase III clinical development, which may serve as a model for the other products in development. Through detailed process understanding, we implemented an analysis and control strategy that enables the control of the five genotoxic impurities upstream in the manufacturing process at the starting materials or intermediates rather than at the final API. This allows the control limits to be set at percent levels rather than ppm levels, thereby simplifying the analytical testing and the analytical toolkits to be used in quality control laboratories.
Analytical control of process impurities in Pazopanib hydrochloride by impurity fate mapping.[Pubmed:20189340]
J Pharm Biomed Anal. 2010 Aug 1;52(4):493-507.
Understanding the origin and fate of organic impurities within the manufacturing process along with a good control strategy is an integral part of the quality control of drug substance. Following the underlying principles of quality by design (QbD), a systematic approach to analytical control of process impurities by impurity fate mapping (IFM) has been developed and applied to the investigation and control of impurities in the manufacturing process of Pazopanib Hydrochloride, an anticancer drug approved recently by the U.S. FDA. This approach requires an aggressive chemical and analytical search for potential impurities in the starting materials, intermediates and drug substance, and experimental studies to track their fate through the manufacturing process in order to understand the process capability for rejecting such impurities. Comprehensive IFM can provide elements of control strategies for impurities. This paper highlights the critical roles that analytical sciences play in the IFM process and impurity control. The application of various analytical techniques (HPLC, LC-MS, NMR, etc.) and development of sensitive and selective methods for impurity detection, identification, separation and quantification are highlighted with illustrative examples. As an essential part of the entire control strategy for Pazopanib Hydrochloride, analytical control of impurities with 'meaningful' specifications and the 'right' analytical methods is addressed. In particular, IFM provides scientific justification that can allow for control of process impurities up-stream at the starting materials or intermediates whenever possible.
Characterization of forced degradation products of pazopanib hydrochloride by UHPLC-Q-TOF/MS and in silico toxicity prediction.[Pubmed:26349647]
J Mass Spectrom. 2015 Jul;50(7):918-28.
Pazopanib (PZ), an anti-cancer drug, was subjected to forced degradation under hydrolytic (acid, base and neutral), oxidative, photolytic and thermal stress conditions as per International Conference on Harmonization guidelines. A selective stability indicating validated method was developed using a Waters Acquity UPLC HSS T3 (100 x 2.1 mm, 1.7 microm) column in gradient mode with ammonium acetate buffer (10 mM, pH 5.0) and acetonitrile. PZ was found to degrade only in photolytic conditions to produce six transformation products (TPs). All the TPs were identified and characterized by liquid chromatography/atmospheric pressure chemical ionization-quadrupole-time of flight mass spectrometry experiments in combination with accurate mass measurements. Plausible mechanisms have been proposed for the formation of TPs. In silico toxicity was predicted using TOPKAT and DEREK softwares for all the TPs. The TP, N4-(2,3-dimethyl-2H-indazol-6-yl)-N4-methylpyrimidine-2,4-diamine, was found to be genotoxic, whereas all other TPs with sulfonamide moiety were hepatotoxic. The data reported here are expected to be of significance as this study foresees the formation of one potential genotoxic and five hepatotoxic degradation/transformation products.