Pazopanib
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MedKoo CAT#: 202161

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

Description: 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

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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: 437.16339
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
100.0mg USD 150.0 Same day
200.0mg USD 250.0 Same day
500.0mg USD 350.0 Same day
1.0g USD 550.0 Same day
2.0g USD 850.0 Same day
5.0g USD 1550.0 Same day
10.0g USD 2650.0 Same day
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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

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/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 8.3 19.0

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.

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  1: Jeldres C, Sun M, Perrotte P, Karakiewicz PI. Pazopanib trial data cannot support first-line use. Nat Rev Urol. 2010 Jun;7(6):307-8. PubMed PMID: 20535144.

2: Altorki N, Lane ME, Bauer T, Lee PC, Guarino MJ, Pass H, Felip E, Peylan-Ramu N, Gurpide A, Grannis FW, Mitchell JD, Tachdjian S, Swann RS, Huff A, Roychowdhury DF, Reeves A, Ottesen LH, Yankelevitz DF. Phase II Proof-of-Concept Study of Pazopanib Monotherapy in Treatment-Naive Patients With Stage I/II Resectable Non-Small-Cell Lung Cancer. J Clin Oncol. 2010 Jun 1. [Epub ahead of print] PubMed PMID: 20516450.

3: Sideras K, Menefee ME, Burton JK, Erlichman C, Bible KC, Ivy SP. Profound Hair and Skin Hypopigmentation in an African American Woman Treated With the Multi-Targeted Tyrosine Kinase Inhibitor Pazopanib. J Clin Oncol. 2010 Jun 1. [Epub ahead of print] PubMed PMID: 20516434.

4: Tailor TD, Hanna G, Yarmolenko PS, Dreher MR, Betof AS, Nixon AB, Spasojevic I, Dewhirst MW. Effect of pazopanib on tumor microenvironment and liposome delivery. Mol Cancer Ther. 2010 Jun;9(6):1798-808. Epub 2010 Jun 1. PubMed PMID: 20515941.

5: Hamberg P, Verweij J, Sleijfer S. (Pre-)Clinical Pharmacology and Activity of Pazopanib, a Novel Multikinase Angiogenesis Inhibitor. Oncologist. 2010 May 28. [Epub ahead of print] PubMed PMID: 20511320.

6: Böhm S, Hess D, Gillessen S, Brändle M. Improved glycemic control with the multi-receptor tyrosine kinase inhibitor pazopanib. Diabetes Care. 2010 Jun;33(6):e82. PubMed PMID: 20508227.

7: Sternberg CN. Pazopanib in renal cell carcinoma. Clin Adv Hematol Oncol. 2010 Apr;8(4):232-3. PubMed PMID: 20505644.

Pazopanib

100.0mg / USD 150.0


Additional Information

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