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MedKoo Cat#: 202161 | Name: Pazopanib
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Pazopanib is an approved drug, is a small molecule inhibitor of multiple protein tyrosine kinases with potential antineoplastic activity. Pazopanib selectively inhibits vascular endothelial growth factor receptors (VEGFR)-1, -2 and -3, c-kit and platelet derived growth factor receptor (PDGF-R), which may result in inhibition of angiogenesis in tumors in which these receptors are upregulated. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Chemical Structure

Pazopanib
Pazopanib
CAS#444731-52-6 (free base)

Theoretical Analysis

MedKoo Cat#: 202161

Name: Pazopanib

CAS#: 444731-52-6 (free base)

Chemical Formula: C21H23N7O2S

Exact Mass: 437.1634

Molecular Weight: 437.52

Elemental Analysis: C, 57.65; H, 5.30; N, 22.41; O, 7.31; S, 7.33

Price and Availability

Size Price Availability Quantity
100mg USD 150.00 Ready to ship
200mg USD 225.00 Ready to ship
500mg USD 450.00 Ready to ship
1g USD 750.00 Ready to ship
2g USD 1,250.00 Ready to ship
5g USD 2,250.00 Ready to ship
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Related CAS #
635702-64-6 (HCl) 444731-52-6 (free base)
Synonym
GW786034; GW786034; GW 786034; Pazopanib; US brand name: Votrient.
IUPAC/Chemical Name
5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzenesulfonamide
InChi Key
CUIHSIWYWATEQL-UHFFFAOYSA-N
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)
SMILES Code
O=S(C1=CC(NC2=NC=CC(N(C3=CC4=NN(C)C(C)=C4C=C3)C)=N2)=CC=C1C)(N)=O
Appearance
white solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Pazopanib hydrochloride is a white to slightly yellow solid. It is very slightly soluble at pH 1 and practically insoluble above pH 4 in aqueous media. Tablets of VOTRIENT are for oral administration. Each 200 mg tablet of VOTRIENT contains 216.7 mg of pazopanib hydrochloride, equivalent to 200 mg of pazopanib free base. The inactive ingredients of VOTRIENT are: Tablet Core: Magnesium stearate, microcrystalline cellulose, povidone, sodium starch glycolate. Coating: Gray film-coat: Hypromellose, iron oxide black, macrogol/polyethylene glycol 400 (PEG 400), polysorbate 80, titanium dioxide.   Pazopanib is a multi-tyrosine kinase inhibitor of vascular endothelial growth factor receptor (VEGFR)-1, VEGFR-2, VEGFR-3, platelet-derived growth factor receptor (PDGFR)-α and -β, fibroblast growth factor receptor (FGFR) -1 and -3, cytokine receptor (Kit), interleukin-2 receptor inducible T-cell kinase (Itk), leukocyte-specific protein tyrosine kinase (Lck), and transmembrane glycoprotein receptor tyrosine kinase (c-Fms). In vitro, pazopanib inhibited ligand-induced autophosphorylation of VEGFR-2, Kit and PDGFR-β receptors. In vivo, pazopanib inhibited VEGF-induced VEGFR-2 phosphorylation in mouse lungs, angiogenesis in a mouse model, and the growth of some human tumor xenografts in mice    
Biological target:
Pazopanib (GW786034) is a multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC50s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.
In vitro activity:
Gastric cancer cell lines were treated with pazopanib to investigate whether inhibition of FGFR2 kinase activity is effective against gastric cancer cell lines harboring FGFR2 amplification and to test the potential therapeutic relevance of these findings. Treatment of the KATO-III, OCUM-2M, SNU-16, and HSC-39 gastric cancer cell lines harboring FGFR2 amplification with pazopanib resulted in marked decreases in cell survival with IC50 in ranges of 0.1 to 2.0 μmol/L, whereas similar treatment of the cell lines without FGFR2 amplification had no effect (Fig. 2A). Reference: Mol Cancer Ther. 2014 Nov;13(11):2527-36. https://mct.aacrjournals.org/content/13/11/2527.long
In vivo activity:
NSCLC (non-small cell lung cancer) xenograft mouse models were used to evaluate the efficacy of pazopanib in vivo. Immune-deficient beige-nude mice were inoculated in the flank with 1 × 107 of two types of NSCLC cells (A549-luc, L9981-luc), which are cell lines stably expressing a luciferase reporter gene. When the tumors reached a palpable size, mice were randomized into a treated group (pazopanib 100 mg/kg) and a control group. Pazopanib or vehicle was orally administered daily. Tumor growths in the treated groups were significantly delayed compared with the control groups (Fig 2A–C, Fig 3A–B), and pazopanib also reduced the number of metastases in the xenograft mice (Fig 2D). Pazopanib prolonged the mouse survival in the treated group, and the mean OS (overall survival) was days 46.1 and 50.4 in the treated group of A549 and L9981 mice, versus days 55.3 and 56 in the control groups (Fig 2E, Fig 3C). Reference: Thorac Cancer. 2015 Mar;6(2):133-40. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4448486/
Solvent mg/mL mM
Solubility
DMSO 8.3 19.00
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 437.52 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Kim ST, Jang HL, Lee SJ, Lee J, Choi YL, Kim KM, Cho J, Park SH, Park YS, Lim HY, Yashiro M, Kang WK, Park JO. Pazopanib, a novel multitargeted kinase inhibitor, shows potent in vitro antitumor activity in gastric cancer cell lines with FGFR2 amplification. Mol Cancer Ther. 2014 Nov;13(11):2527-36. doi: 10.1158/1535-7163.MCT-14-0255. Epub 2014 Sep 23. PMID: 25249557. 2. Zhao H, Yang F, Shen W, Wang Y, Li X, You J, Zhou Q. Pazopanib diminishes non-small cell lung cancer (NSCLC) growth and metastases in vivo. Thorac Cancer. 2015 Mar;6(2):133-40. doi: 10.1111/1759-7714.12138. Epub 2015 Mar 2. PMID: 26273349; PMCID: PMC4448486. 3. Craveiro RB, Ehrhardt M, Holst MI, Pietsch T, Dilloo D. In comparative analysis of multi-kinase inhibitors for targeted medulloblastoma therapy pazopanib exhibits promising in vitro and in vivo efficacy. Oncotarget. 2014 Aug 30;5(16):7149-61. doi: 10.18632/oncotarget.2240. PMID: 25216529; PMCID: PMC4196191.
In vitro protocol:
1. Kim ST, Jang HL, Lee SJ, Lee J, Choi YL, Kim KM, Cho J, Park SH, Park YS, Lim HY, Yashiro M, Kang WK, Park JO. Pazopanib, a novel multitargeted kinase inhibitor, shows potent in vitro antitumor activity in gastric cancer cell lines with FGFR2 amplification. Mol Cancer Ther. 2014 Nov;13(11):2527-36. doi: 10.1158/1535-7163.MCT-14-0255. Epub 2014 Sep 23. PMID: 25249557. 2. Zhao H, Yang F, Shen W, Wang Y, Li X, You J, Zhou Q. Pazopanib diminishes non-small cell lung cancer (NSCLC) growth and metastases in vivo. Thorac Cancer. 2015 Mar;6(2):133-40. doi: 10.1111/1759-7714.12138. Epub 2015 Mar 2. PMID: 26273349; PMCID: PMC4448486.
In vivo protocol:
1. Craveiro RB, Ehrhardt M, Holst MI, Pietsch T, Dilloo D. In comparative analysis of multi-kinase inhibitors for targeted medulloblastoma therapy pazopanib exhibits promising in vitro and in vivo efficacy. Oncotarget. 2014 Aug 30;5(16):7149-61. doi: 10.18632/oncotarget.2240. PMID: 25216529; PMCID: PMC4196191. 2. Zhao H, Yang F, Shen W, Wang Y, Li X, You J, Zhou Q. Pazopanib diminishes non-small cell lung cancer (NSCLC) growth and metastases in vivo. Thorac Cancer. 2015 Mar;6(2):133-40. doi: 10.1111/1759-7714.12138. Epub 2015 Mar 2. PMID: 26273349; PMCID: PMC4448486.
1: Damassi A, Cremante M, Signori A, Rebuzzi SE, Malgeri A, Napoli MD, Caffo O, Vignani F, Cavo A, Roviello G, Prati V, Tudini M, Atzori F, Messina M, Morelli F, Prati G, Nolè F, Catalano F, Murianni V, Rescigno P, Banna GL, Fornarini G, Buti S. Prognostic value of type of prior TKI in pretreated metastatic renal cell carcinoma patients receiving nivolumab. Immunotherapy. 2024 Aug 19:1-9. doi: 10.1080/1750743X.2024.2385881. Epub ahead of print. PMID: 39155821. 2: Mobaraki S, Nissen PH, Donskov F, Wozniak A, Van Herck Y, Coosemans L, van Nieuwenhuyse T, Lambrechts D, Bechter O, Baldewijns M, Roussel E, Laenen A, Beuselinck B. Cabozantinib Induces Isolated Hyperbilirubinemia in Renal Cell Carcinoma Patients carrying the UGT1A1*28 Polymorphism. Clin Genitourin Cancer. 2024 Jul 27:102180. doi: 10.1016/j.clgc.2024.102180. Epub ahead of print. PMID: 39155162. 3: Zhou S, Xue J, Yang Q, Zang W, Chen Y, Zhao Y, Gao X. Clinical significance of LIN28A gene polymorphisms and expression in pan-cancer: a meta- analysis and bioinformatic analysis. Nucleosides Nucleotides Nucleic Acids. 2024 Aug 18:1-10. doi: 10.1080/15257770.2024.2393316. Epub ahead of print. PMID: 39154245. 4: Jo JK, Seo SI, Kang M, Chung J, Kwak C, Hong SH, Song C, Park JY, Jeong CW, Choi SH, Kim SH, Chang Hwang E, Lee CH, Lee H. Optimal sequential therapy using tyrosine kinase inhibitors as the first-line treatment in patients with metastatic renal cell carcinoma: A nationwide multicenter study. Asian J Urol. 2024 Jul;11(3):450-459. doi: 10.1016/j.ajur.2022.11.004. Epub 2023 Mar 17. PMID: 39139527; PMCID: PMC11318389. 5: Konda B, Sherman EJ, Massarelli E, Nieva J, Muzaffar J, Morris Iii JC, Ryder M, Ho AL, Agulnik M, Wei L, Handley D, Moses C, Jacob R, Wright J, Streicher H, Carson W, Shah MH. Cabozantinib plus ipilimumab/nivolumab in patients with previously treated advanced differentiated thyroid cancer. J Clin Endocrinol Metab. 2024 Aug 12:dgae512. doi: 10.1210/clinem/dgae512. Epub ahead of print. PMID: 39133806. 6: Tan L, Ni Y, Huang Z, Yan J, Wu M, Zhang Z, Zhang F, Wang Z. Efficacy and safety of VEGFR inhibitors for recurrent ovarian cancer: a systematic review. Future Oncol. 2024 Aug 12:1-19. doi: 10.1080/14796694.2024.2373680. Epub ahead of print. PMID: 39129672. 7: Sarg NH, Hersi FH, Zaher DM, Hamouda AO, Ibrahim SI, El-Seedi HR, Omar HA. Unveiling the therapeutic potential of Taxifolin in Cancer: From molecular mechanisms to immune modulation and synergistic combinations. Phytomedicine. 2024 Aug 3;133:155934. doi: 10.1016/j.phymed.2024.155934. Epub ahead of print. PMID: 39128306. 8: Ma X, Xu J, Ye X, Yang F, Wang Z, Feng J. Early recurrence and extensive retroperitoneal metastasis after surgery for high‑grade mucinous tubular and spindle cell carcinoma: A case report and literature review. Oncol Lett. 2024 Jul 31;28(4):467. doi: 10.3892/ol.2024.14600. PMID: 39119228; PMCID: PMC11306991. 9: Czarnecka AM, Chmiel P, Błoński P, Świtaj T, Rogala P, Falkowski S, Koseła- Paterczyk H, Teterycz P, Kopeć S, Morysiński T, Wągrodzki M, Rutkowski P. Long- term outcomes of sequential chemotherapy in epithelioid sarcoma. J Chemother. 2024 Aug 8:1-12. doi: 10.1080/1120009X.2024.2385261. Epub ahead of print. PMID: 39115147. 10: Matsuoka H, Yoshida KI, Nakai S, Suzuki R, Imura Y, Takami H, Watanabe M, Wakamatsu T, Tamiya H, Outani H, Yagi T, Kakunaga S, Takenaka S. Successful pazopanib treatment of undifferentiated pleomorphic sarcoma with coamplification of PDGFRA, VEGFR2 and KIT: A case report. Mol Clin Oncol. 2024 Jul 29;21(4):69. doi: 10.3892/mco.2024.2767. PMID: 39113850; PMCID: PMC11304161. 11: Edelbach BM, Gospodarev V, Raghavan R, Dye J. Primary intracranial sarcoma, DICER-1 mutant, with hemorrhagic presentation: A case report. Surg Neurol Int. 2024 Jul 26;15:253. doi: 10.25259/SNI_259_2024. PMID: 39108364; PMCID: PMC11302587. 12: Basiri R, Ziaei Moghaddam A, Rikhtegar A, Jafarian AH. Primary Pulmonary Angiosarcoma Found Incidentally in a Complicated Patient: A Rare Case Report. Clin Respir J. 2024 Aug;18(8):e13818. doi: 10.1111/crj.13818. PMID: 39107956; PMCID: PMC11303451. 13: Kumar NN, Sharma S. Stability Indicating UPLC Method Development and Validation for the Quantitative Estimation of Pazopanib in Pure form and Marketed Pharmaceutical Dosage form. Zhongguo Ying Yong Sheng Li Xue Za Zhi. 2024 Aug 6;40:e20240018. doi: 10.62958/j.cjap.2024.018. PMID: 39103242. 14: Cao RB, Ge Y, Zhang WX, Lin GH, Kuang BH, Wang BC. The efficacy and safety of antiangiogenesis tyrosine kinase inhibitors in patients with advanced anaplastic thyroid cancer: A meta-analysis of prospective studies. Medicine (Baltimore). 2024 Aug 2;103(31):e38679. doi: 10.1097/MD.0000000000038679. PMID: 39093805; PMCID: PMC11296411. 15: Mustafa D, Ibrahim B, Erten A. Adsorptive removal of anticarcinogen pazopanib from aqueous solutions using activated carbon: isotherm, kinetic and thermodynamic studies. Sci Rep. 2024 Aug 1;14(1):17765. doi: 10.1038/s41598-024-68666-3. PMID: 39085425; PMCID: PMC11291750. 16: Ohno M, Kawaguchi Y, Sugino H, Yoshida A, Takahashi M, Yanagisawa S, Osawa S, Tsuchiya T, Fujita S, Narita Y. Resection and postoperative pazopanib for intraspinal recurrent solitary fibrous tumor: illustrative case. J Neurosurg Case Lessons. 2024 Jul 29;8(5):CASE24217. doi: 10.3171/CASE24217. PMID: 39074397; PMCID: PMC11301598. 17: Jakobsson M, Strambi A, Nilsson F, Arpegård J, Dalén J. Real-world experience of second-line axitinib in metastatic renal cell carcinoma: analysis of the Swedish population. Future Oncol. 2024 Jul 26:1-8. doi: 10.1080/14796694.2024.2351352. Epub ahead of print. PMID: 39057291. 18: Lara PN Jr, Villanueva L, Ibanez C, Erman M, Lee JL, Heinrich D, Lipatov ON, Gedye C, Gokmen E, Acevedo A, Semenov A, Park SH, Gafanov RA, Kose F, Jones M, Du X, Munteanu M, Perini R, Choueiri TK, Motzer RJ. A randomized, open-label, phase 3 trial of pembrolizumab plus epacadostat versus sunitinib or pazopanib as first-line treatment for metastatic renal cell carcinoma (KEYNOTE-679/ECHO-302). BMC Cancer. 2024 Jul 25;23(Suppl 1):1253. doi: 10.1186/s12885-023-10971-7. PMID: 39054430; PMCID: PMC11270760. 19: Xu Z, Zhou Z, Yang X, Thakur A, Han N, Li HT, Li LG, Hu J, Li TF, Yan Y. Determining M2 macrophages content for the anti-tumor effects of metal-organic framework-encapsulated pazopanib nanoparticles in breast cancer. J Nanobiotechnology. 2024 Jul 20;22(1):429. doi: 10.1186/s12951-024-02694-z. PMID: 39033109; PMCID: PMC11264935. 20: Del Re M, Crucitta S, Brighi N, Kinspergher S, Mercinelli C, Rizzo M, Conteduca V, Rebuzzi SE, Beninato T, Venturi G, Doni L, Verzoni E, Puglisi S, Landriscina M, Porta C, Manfredi F, Caffo O, De Giorgi U, Fogli S, Danesi R. Concomitant Administration of VEGFR Tyrosine Kinase and Proton Pump Inhibitors May Impair Clinical Outcome of Patients With Metastatic Renal Cancer. Clin Genitourin Cancer. 2024 Jun 27:102147. doi: 10.1016/j.clgc.2024.102147. Epub ahead of print. PMID: 39030142.