Cat. No.: HY-12009

Pazopanib Hydrochloride

(Synonyms: GW786034 Hydrochloride)

25 Cited Publications

Customer Review

Based on 25 publication(s) in Google Scholar

Pazopanib Hydrochloride (GW786034 Hydrochloride) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with an IC₅₀ of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.

For research use only. We do not sell to patients.

Purity: 99.99%
CAS No.: 635702-64-6
Formula: C₂₁H₂₄ClN₇O₂S
Molecular Weight:473.98

Storage:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

Pazopanib Hydrochloride Chemical Structure

CAS No.: 635702-64-6

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (25)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

VEGFR1

10 nM (IC₅₀)

VEGFR2

30 nM (IC₅₀)

VEGFR3

47 nM (IC₅₀)

PDGFRβ

84 nM (IC₅₀)

FGFR1

140 nM (IC₅₀)

c-Kit

74 nM (IC₅₀)

c-Fms

146 nM (IC₅₀)

All PDGFR Isoforms :

All VEGFR Isoforms :

In Vitro

Pazopanib shows good potency against all the human VEGFR receptors with an IC₅₀ of 10, 30, and 47 nM for VEGFR-1, -2, and -3, respectively. Significant activity is also seen against the closely related tyrosine receptor kinases PDGFRβ, c-Kit, FGF-R1, and c-fms with IC₅₀s of 84, 74, 140, and 146 nM, respectively. In cellular assays, in addition to inhibiting the VEGF-induced proliferation of HUVECs, Pazopanib potently inhibits VEGF-induced phosphorylation of VEGFR-2 in HUVEC cells with an IC₅₀ of ~8 nM. Pazopanib possesses good pharmacokinetics in rat, dog, and monkey with low clearances (1.4-1.7 mL/min/kg) and good oral bioavailabilities (72, 47, 65%) dosed at 10, 1, and 5 mg/kg, respectively. The cytochrome P450 profile is also improved with inhibition >10 μM against the isozymes tested, with the exception of 2C9 (7.9 μM)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Treatment of mice with 100 mg/kg of Pazopanib twice daily for five days results in significant inhibition in the degree of vascularization. The antiangiogenic activity of Pazopanib is examined in mice bearing established human xenografts (200 250 mm³) using HT29 (colon carcinoma), A375P (melanoma), and HN5 (head and neck carcinoma) tumors following a standard three-week course of therapy. The HN5 and HT29 xenografts responded better at all doses compared to the A375P model, which is historically more resistant to VEGFR-2 inhibitors. As support that the observed inhibition of xenograft growth is working through an antiangiogenic rather than antitumor mechanism, no antiproliferative activity is observed below 10 μM for Pazopanib against these human tumor lines (HT29, HN5, A375P) growing in serum-containing media. No significant effect on the body weight of mice is observed, and the animals appeared healthy and active throughout the study duration^[1]. The quantity of adherent leukocytes in the Pazopanib eye drops group is less than untreated diabetic animals and more than the healthy animals. Average leukocytes adhered to the retinal vasculature in healthy animals is 37.2±7.8, whereas diabetic animals have an average value of 102±15.6, approximately 3-fold higher than healthy animals. Animals treated with 0.5 % w/v Pazopanib suspension demonstrate 69.5±9.5 leukocytes adhered in their retinal vasculature, which is found to be significantly lower than diabetic animals^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 635702-64-6
Appearance Solid
Molecular Weight 473.98
Formula C₂₁H₂₄ClN₇O₂S
Color White to off-white
SMILES

CC1=CC=C(C=C1S(N)(=O)=O)NC2=NC=CC(N(C3=CC4=NN(C(C)=C4C=C3)C)C)=N2.Cl
Synonyms

GW786034 Hydrochloride
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

Publications (25)

All Cell Proliferation/Viability AssayELISAWBRT-PCRCell Imaging/Staining

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Journal Impact Factor

Cell Metab

The thermogenic activity of adjacent adipocytes fuels the progression of ccRCC and compromises anti-tumor therapeutic efficacy. [Abstract]

2021 Oct 5;33(10):2021-2039.e8. PMID: 34508696
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Biomaterials

Automated discovery of nanomaterials via drug aggregation induced emission. [Abstract]

2022 Oct:289:121800. PMID: 36166893
J Nanobiotechnology

Matrix micro/nano-topography drives oncogenic signaling and drug response in a 3D osteosarcoma model. [Abstract]

2026 Mar 6;24(1):345. PMID: 41787498
Cell Rep Med

CAN-Scan: A multi-omic phenotype-driven precision oncology platform identifies prognostic biomarkers of therapy response for colorectal cancer. [Abstract]

2025 Apr 2:102053. PMID: 40187357
Acta Pharmacol Sin

Pazopanib alleviates neuroinflammation and protects dopaminergic neurons in LPS-stimulated mouse model by inhibiting MEK4-JNK-AP-1 pathway. [Abstract]

2023 Jun;44(6):1135-1148. PMID: 36536076

Pazopanib Hydrochloride purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2023 Jun;44(6):1135-1148. [Abstract]

Anti-inflammatory effect validation of VEGFR-TKIs by ELISA and immunoblot analysis. BV2 cells were treated with Pazopanib (10 μM) or DMSO for 4 h and then treated with LPS (1 μg/ml) or PBS for 20 h. Cell viability of the BV2 cells treated with VEGFR-TKIs for 24 h was measured by CCK8 assay.

Pazopanib Hydrochloride purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2023 Jun;44(6):1135-1148. [Abstract]

Pazopanib (10 μM) had significant inhibitory effects on the production of TNF-α by BV2 cells that were treated with LPS measured using ELISA.

Pazopanib Hydrochloride purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2023 Jun;44(6):1135-1148. [Abstract]

Immunoblot analyses showed that Pazopanib (10 μM) had inhibitory effects on LPS-induced BV2 activation, which was indicated by the decreases in inducible nitric oxide synthase (iNOS) and cyclooxygenase-2.

Pazopanib Hydrochloride purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2023 Jun;44(6):1135-1148. [Abstract]

BV2 cells were treated with Pazopanib (5 μM) for 4 h or DMSO followed by LPS treatment for 12 h, and total RNA was collected to measure the mRNA levels of iNOS, COX2, IL-1β using qPCR assays.

Pazopanib Hydrochloride purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2023 Jun;44(6):1135-1148. [Abstract]

BV2 cells were treated with Pazopanib (5 μM) for 4 h and then exposed to LPS (1 μg) for 15 min. After the treatment, cells were fixed and labeled with anti-p65 antibodies (red), while nuclei were labeled with DAPI (blue). The cells were imaged with a fluorescence microscope.
Acta Pharmacol Sin

Osimertinib successfully combats EGFR-negative glioblastoma cells by inhibiting the MAPK pathway. [Abstract]

2021 Jan;42(1):108-114. PMID: 32398685
Cell Syst

A Library of Phosphoproteomic and Chromatin Signatures for Characterizing Cellular Responses to Drug Perturbations. [Abstract]

2018 Apr 25;6(4):424-443.e7. PMID: 29655704
Cell Rep Methods

RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]

2023 Oct 23;3(10):100599. PMID: 37797618
ACS Chem Biol

A Chemical Probe Strategy for Interrogating Inhibitor Selectivity Across the MEK Kinase Family. [Abstract]

2017 May 19;12(5):1245-1256. PMID: 28263556
Bioengineering (Basel)

Precision Oncology for High-Grade Gliomas: A Tumor Organoid Model for Adjuvant Treatment Selection. [Abstract]

2025 Oct 19;12(10):1121. PMID: 41155119
Cell Signal

GLI2/Parkin-mediated mitophagy promotes pazopanib resistance in clear cell renal cell carcinoma. [Abstract]

2025 Nov:135:112054. PMID: 40780617
J Cell Sci

Crucial role of TRPC6 in maintaining the stability of HIF-1α in glioma cells under hypoxia. [Abstract]

2015 Sep 1;128(17):3317-29. PMID: 26187851
Exp Cell Res

Network-based analysis with primary cells reveals drug response landscape of acute myeloid leukemia. [Abstract]

2020 Aug 1;393(1):112054. PMID: 32376287
Hum Cell

Establishment and characterization of the novel myxofibrosarcoma cell line, SMU-MFS. [Abstract]

2024 Dec 3;38(1):25. PMID: 39625530
PLoS One

A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]

2024 Nov 1;19(11):e0308647. PMID: 39485774
Cell Physiol Biochem

Triggering of Suicidal Erythrocyte Death by Pazopanib. [Abstract]

2016;38(3):926-38. PMID: 26937949

Pazopanib Hydrochloride purchased from MedChemExpress. Usage Cited in: Cell Physiol Biochem. 2016;38(3):926-38. [Abstract]

Arithmetic means±SEM (n=16) of erythrocyte annexin-V-binding following incubation for 48 hours to Ringer solution without (white bar) or with (black bars) Pazopanib (10-50 µg/mL).
J Toxicol Sci

Validation of a new protocol for a zebrafish MEFL (malformation or embryo-fetal lethality) test method that conforms to the ICH S5 (R3) guideline. [Abstract]

2024;49(8):337-348. PMID: 39098043
bioRxiv

2025 Dec 5.
bioRxiv

2025 Sep 21.
Hong Kong Polytechnic University

2025.
bioRxiv

Closing the loop: Teaching single-cell foundation models to learn from perturbations. [Abstract]

2025 Jul 12:2025.07.08.663754. PMID: 40672312
bioRxiv

A Microphysiological HHT-on-a-Chip Platform Recapitulates Patient Vascular Lesions. [Abstract]

2024 Mar 12:2024.03.11.584490. PMID: 38559155
Patent

US20210299273A1.
J BUON

The HDAC inhibitor OBP-801 suppresses the growth of myxofibrosarcoma cells. [Abstract]

Jan-Feb 2020;25(1):464-471. PMID: 32277670

Solvent & Solubility

In Vitro:

DMSO : 10 mg/mL (21.10 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1098 mL

10.5490 mL

21.0979 mL

5 mM

0.4220 mL

2.1098 mL

4.2196 mL

10 mM

0.2110 mL

1.0549 mL

2.1098 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 1 mg/mL (2.11 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 1 mg/mL (2.11 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 1 mg/mL (2.11 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocol

Kinase Assay^[1]

VEGFR enzyme assays are initiated by the addition of 10 μL of activated VEGFR2 kinase solution [final concentration, 1 nM enzyme in 0.1 M 4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES), pH 7.5, containing 0.1 mg/mL bovine serum albumin (BSA), 300 μM dithiothreitol (DTT)] to 10 μL substrate solution [final concentration, 360 nM peptide, (biotin-aminohexyl-EEEEYFELVAKKKK-NH2), 75 μM ATP, 10 μM MgCl₂], and 1 μL of titrated compound (Pazopanib) in DMSO. Plates are incubated at room temperature for 60 min, and then the reaction is quenched by the addition of 20 μL of 100 mM ethylene diamine tetraacetic acid (EDTA). After quenching, 20 μL HTRF reagents (final concentration, 15 nM Streptavidin-linked allophycocyanin, 1 nM Europium-labeled antiphosphotyrosine antibody diluted in 0.1 mg/mL BSA, 0.1 M HEPES, pH 7.5) is added and the plates incubated for a minimum of 10 min. The fluorescence at 665 nM is measured with a plate reader^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay^[1]

The effect of Pazopanib on cell proliferation is measured using 5-bromo-2-deoxyuridine (BrdU) incorporation method using commercially available kits. HUVEC is seeded in medium containing 5% fetal bovine serum (FBS) in type 1 collagen coated 96-well plates and incubated overnight at 37°C, 5% CO₂. The medium is aspirated from the cells, and various concentrations of Pazopanib in serum-free medium are added to each well. After 30 min, either VEGF (10 ng/mL) or bFGF (0.3 ng/mL) is added to the wells. Cells are incubated for an additional 72 h and BrdU (10 μM) is added during the last 18 to 24 h of incubation. At the end of incubation, BrdU incorporation in cells is measured by ELISA. Data are fitted with a curve described by the equation, y=V_max(1−(x/(K+x))), where K is equal to the IC₅₀^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[1]^[2]

Mice^[1]
Tumors are initiated by injection of tumor cell suspension in 8−12 week old nude mice. When tumors reach a volume of 100−200 mm³, mice are randomized and divided into groups of eight. Pazopanib is administered once or twice daily at 10, 30, or 100 mg/kg. Animals are euthanized by inhalation of CO₂ at the completion of the study. Tumor volume is measured twice weekly by calipers, using the equation: tumor volume (mm³)=(length×width²)/2. Results are routinely reported as % inhibition=1−(average growth of the drug treated population/average growth of vehicle treated control population).
Rats^[2]
Male Brown-Norway (BN; pigmented) rats weighing 200 to 250 g are acclimatized for at least two days prior to any experimental procedure. After overnight fasting for 12-16 h, an intraperitoneal injection of 30 mg/mL solution of Streptozotocin in 10 mM citrate buffer (pH 4.5) is administered (60 mg/kg body weight) to induce diabetes. After 3-4 h of Streptozotocin injection, animals are put on a regular diet and 24 h after Streptozotocin injection, blood sample (5-10 μL) is collected via tail vein. The blood glucose levels in the animals are determined with a glucose monitor. Animals with blood glucose levels greater than 250 mg/dL are considered diabetic. The animals are divided into three groups. Group 1: Healthy (n=12), Group 2: Diabetic (n=12) and Group 3: Diabetic+Treatment (n=12). Treatment is started immediately after diabetes induction. Both eyes are dosed twice daily for 30 days with 0.5 % w/v Pazopanib suspension (10 μL volume in each eye) and animals in all groups are sacrificed on day 31, 16-17 h after last dose on day 30.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Harris PA, et al. Discovery of 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide (Pazopanib), a novel and potent vascular endothelial growth factor receptor inhibitor. J Med Chem. 2008, 51(15), 4632-4640. [Content Brief]

[2]. Thakur A, et al. Pazopanib, a multitargeted tyrosine kinase inhibitor, reduces diabetic retinal vascular leukostasis and leakage. Microvasc Res. 2011 Nov;82(3):346-50. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1098 mL	10.5490 mL	21.0979 mL	52.7448 mL
	5 mM	0.4220 mL	2.1098 mL	4.2196 mL	10.5490 mL
	10 mM	0.2110 mL	1.0549 mL	2.1098 mL	5.2745 mL
	15 mM	0.1407 mL	0.7033 mL	1.4065 mL	3.5163 mL
	20 mM	0.1055 mL	0.5274 mL	1.0549 mL	2.6372 mL

Keywords

Pazopanib Hydrochloride

25 Cited Publications

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Pazopanib Hydrochloride

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Publications Citing Use of MedChemExpress (MCE) Pazopanib Hydrochloride

All PDGFR Isoforms

All VEGFR Isoforms

Biological Activity

Chemical Information

Publications (25)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Pazopanib Hydrochloride Related Classifications

HY-12009 Related Classifications