Referencia número: HY-10208

Pazopanib

(Synonyms: GW786034)

25 Cited Publications

Revisión del cliente

Based on 25 publication(s) in Google Scholar

Pazopanib (GW786034) is a novel 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.

Para uso exclusivo en investigación. No vendemos a pacientes.

Pureza: 99.91%
No. CAS: 444731-52-6
Fòrmula: C₂₁H₂₃N₇O₂S
Peso molecular:437.52

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Pazopanib Chemical Structure

No. CAS: 444731-52-6

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (25)
Solvente y solubilidad
- In Vitro
- In Vivo
Protocolo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

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)

Ver todos los productos específicos de isoformas VEGFR :

Ver todos los productos específicos de isoformas PDGFR :

Cellular Effect

Cell Line	Type	Value	Description	References
5637	IC₅₀	15 μM Compound: Pazopanib	Cytotoxicity against human 5637 cells assessed as reduction in cell viability incubated for 3 hrs by MTT assay Cytotoxicity against human 5637 cells assessed as reduction in cell viability incubated for 3 hrs by MTT assay	[PMID: 33951490]
A549	IC₅₀	2.94 μM Compound: PAZ	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by sulphorhodamine-B assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by sulphorhodamine-B assay	[PMID: 38810335]
ACHN	IC₅₀	>5 μM Compound: Pazopanib	Antiproliferative activity against human ACHN cells after 72 hrs by MTT assay Antiproliferative activity against human ACHN cells after 72 hrs by MTT assay	[PMID: 29787262]
AGS	IC₅₀	>5 μM Compound: Pazopanib	Antiproliferative activity against human AGS cells after 72 hrs by MTT assay Antiproliferative activity against human AGS cells after 72 hrs by MTT assay	[PMID: 29787262]
BEAS-2B	IC₅₀	>100 μM Compound: Pazopanib	Cytotoxicity against human BEAS2B cells assessed as growth inhibition after 24 hrs by MTT assay Cytotoxicity against human BEAS2B cells assessed as growth inhibition after 24 hrs by MTT assay	[PMID: 26968648]
HCC1937	IC₅₀	>10000 nM Compound: Paz	Antiproliferative activity against human HCC1937 cells assessed as cell growth inhibition in presence of 1:1 of compound:Olaparib Antiproliferative activity against human HCC1937 cells assessed as cell growth inhibition in presence of 1:1 of compound:Olaparib	[PMID: 37616488]
HCC1937	IC₅₀	>10000 nM Compound: Paz	Antiproliferative activity against human HCC1937 cells assessed as cell growth inhibition Antiproliferative activity against human HCC1937 cells assessed as cell growth inhibition	[PMID: 37616488]
HCT-116	IC₅₀	1.58 μM Compound: PAZ	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs by sulphorhodamine-B assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs by sulphorhodamine-B assay	[PMID: 38810335]
HEL	IC₅₀	>5 μM Compound: Pazopanib	Antiproliferative activity against human HEL cells after 72 hrs by MTT assay Antiproliferative activity against human HEL cells after 72 hrs by MTT assay	[PMID: 29787262]
HeLa	IC₅₀	>100 μM Compound: Pazopanib	Cytotoxicity against human HeLa cells assessed as growth inhibition after 24 hrs by MTT assay Cytotoxicity against human HeLa cells assessed as growth inhibition after 24 hrs by MTT assay	[PMID: 26968648]
HeLa	IC₅₀	>5 μM Compound: Pazopanib	Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay	[PMID: 29787262]
HT-1080	IC₅₀	>5 μM Compound: Pazopanib	Antiproliferative activity against human HT1080 cells after 72 hrs by MTT assay Antiproliferative activity against human HT1080 cells after 72 hrs by MTT assay	[PMID: 29787262]
HT-29	IC₅₀	>5 μM Compound: Pazopanib	Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 29787262]
HT-29	IC₅₀	873 nM Compound: 38	Inhibition of RIPK1 in human HT-29 cells assessed as reduction in TNFalpha-induced necroptosis incubated for 14 to 24 hrs in presence of Smac mimetic and z-VAD-FMK by cell titer glo-based luminescence assay Inhibition of RIPK1 in human HT-29 cells assessed as reduction in TNFalpha-induced necroptosis incubated for 14 to 24 hrs in presence of Smac mimetic and z-VAD-FMK by cell titer glo-based luminescence assay	[PMID: 31622096]
HT-29	IC₅₀	873 nM Compound: DDC-2036; 7	Anti-necroptic activity in human HT-29 cells Anti-necroptic activity in human HT-29 cells	[PMID: 36346971]
HT-29	EC₅₀	873 nM Compound: F4	Anti-necroptosis activity against TNFalpha-induced human HT-29 cells assessed as reduction in cell viability Anti-necroptosis activity against TNFalpha-induced human HT-29 cells assessed as reduction in cell viability	[PMID: 38199165]
HUVEC	IC₅₀	8 nM Compound: 13	Inhibition of VEGF-induced VEGFR2 phosphorylation in HUVEC Inhibition of VEGF-induced VEGFR2 phosphorylation in HUVEC	[PMID: 18620382]
HUVEC	IC₅₀	21 nM Compound: 4	Inhibition of VEGF-induced cell proliferation of HUVEC pre-incubated for 30 mins before VEGF stimulation for 72 hrs by BrdUrd incorporation assay Inhibition of VEGF-induced cell proliferation of HUVEC pre-incubated for 30 mins before VEGF stimulation for 72 hrs by BrdUrd incorporation assay	[PMID: 28844802]
HUVEC	IC₅₀	720 nM Compound: 4	Inhibition of FGF-induced cell proliferation of HUVEC pre-incubated for 30 mins before FGF stimulation for 72 hrs by BrdUrd incorporation assay Inhibition of FGF-induced cell proliferation of HUVEC pre-incubated for 30 mins before FGF stimulation for 72 hrs by BrdUrd incorporation assay	[PMID: 28844802]
HUVEC	IC₅₀	4.6 μM Compound: Paz	Inhibition of cell survival in VEGF165-treated HUVEC cells incubated for 48 hrs in presence of Olaparib by CCK8 assay Inhibition of cell survival in VEGF165-treated HUVEC cells incubated for 48 hrs in presence of Olaparib by CCK8 assay	[PMID: 37616488]
Jurkat	IC₅₀	373 nM Compound: DDC-2036; 7	Anti-necroptic activity in TNF alpha stimulated FADD-deficient human Jurkat T cells incubated for 24 hrs by celltiter-glo luminescent cell viability assay Anti-necroptic activity in TNF alpha stimulated FADD-deficient human Jurkat T cells incubated for 24 hrs by celltiter-glo luminescent cell viability assay	[PMID: 36346971]
Jurkat	EC₅₀	254 nM Compound: F4	Anti-necroptosis activity against TNFalpha-induced human Jurkat cells assessed as reduction in cell viability Anti-necroptosis activity against TNFalpha-induced human Jurkat cells assessed as reduction in cell viability	[PMID: 38199165]
K562	IC₅₀	>89.32 μM Compound: Pazopanib	Cytotoxicity against human K562 cells assessed as growth inhibition after 24 hrs by MTT assay Cytotoxicity against human K562 cells assessed as growth inhibition after 24 hrs by MTT assay	[PMID: 26968648]
K562	IC₅₀	>5 μM Compound: Pazopanib	Antiproliferative activity against human K562 cells after 72 hrs by MTT assay Antiproliferative activity against human K562 cells after 72 hrs by MTT assay	[PMID: 29787262]
KG-1	IC₅₀	>5 μM Compound: Pazopanib	Antiproliferative activity against human KG1 cells after 72 hrs by MTT assay Antiproliferative activity against human KG1 cells after 72 hrs by MTT assay	[PMID: 29787262]
MCF7	IC₅₀	76.78 μM Compound: Pazopanib	Cytotoxicity against human MCF7 cells assessed as growth inhibition after 24 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as growth inhibition after 24 hrs by MTT assay	[PMID: 26968648]
MCF7	IC₅₀	>10000 nM Compound: Paz	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition in presence of 1:1 of compound:Olaparib Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition in presence of 1:1 of compound:Olaparib	[PMID: 37616488]
MCF7	IC₅₀	>10000 nM Compound: Paz	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition	[PMID: 37616488]
MDA-MB-231	IC₅₀	>5 μM Compound: Pazopanib	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 29787262]
MDA-MB-231	IC₅₀	>10000 nM Compound: Paz	Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition in presence of 1:1 of compound:Olaparib Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition in presence of 1:1 of compound:Olaparib	[PMID: 37616488]
MDA-MB-231	IC₅₀	>10000 nM Compound: Paz	Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition	[PMID: 37616488]
MDA-MB-436	IC₅₀	>10000 nM Compound: Paz	Antiproliferative activity against human MDA-MB-436 cells assessed as cell growth inhibition in presence of 1:1 of compound:Olaparib Antiproliferative activity against human MDA-MB-436 cells assessed as cell growth inhibition in presence of 1:1 of compound:Olaparib	[PMID: 37616488]
MDA-MB-436	IC₅₀	>10000 nM Compound: Paz	Antiproliferative activity against human MDA-MB-436 cells assessed as cell growth inhibition Antiproliferative activity against human MDA-MB-436 cells assessed as cell growth inhibition	[PMID: 37616488]
MOLT-4	IC₅₀	>5 μM Compound: Pazopanib	Antiproliferative activity against human MOLT4 cells after 72 hrs by MTT assay Antiproliferative activity against human MOLT4 cells after 72 hrs by MTT assay	[PMID: 29787262]
PC-3	IC₅₀	>100 μM Compound: Pazopanib	Cytotoxicity against human PC3 cells assessed as growth inhibition after 24 hrs by MTT assay Cytotoxicity against human PC3 cells assessed as growth inhibition after 24 hrs by MTT assay	[PMID: 26968648]
PC-3	IC₅₀	>5 μM Compound: Pazopanib	Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay	[PMID: 29787262]

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.

Chemical Information

No. CAS 444731-52-6
Appearance Solid
Peso molecular 437.52
Fòrmula C₂₁H₂₃N₇O₂S
Color White to off-white
SMILES

O=S(C1=CC(NC2=NC=CC(N(C3=CC4=NN(C(C)=C4C=C3)C)C)=N2)=CC=C1C)(N)=O
Synonyms

GW786034
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (25)

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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
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
Biomaterials

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

2022 Oct:289:121800. PMID: 36166893
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 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 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 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 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 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
Cell Signal

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

2025 Nov:135:112054. PMID: 40780617
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
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
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
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 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

Solvente y solubilidad

In Vitro:

DMSO : 50 mg/mL (114.28 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculadora de molaridad

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

Mass Mass

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Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

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Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 2

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

Solubility: ≥ 2.5 mg/mL (5.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 3

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: ≥ 0.43 mg/mL (0.98 mM); Clear solution

Protocol 4

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)

Solubility: ≥ 0.43 mg/mL (0.98 mM); Clear solution

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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

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Please enter your animal formula composition:

%
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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

Protocolo

Kinase Assay^[1]

VEGFR enzyme assays for VEGGR1, VEGFR2, and VEGFR3 are run in homogeneous time-resolved fluorescence (HTRF) format in 384-well microtiter plates using a purified, baculovirus-expressed glutathione-S-transferase (GST) fusion protein encoding the catalytic c-terminus of human VEGFR receptor kinases 1, 2, or 3. Reactions 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 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 Wallac Victor plate reader using a time delay of 50 μs^[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.

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Referencias

[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]

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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

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2856 mL	11.4280 mL	22.8561 mL	57.1402 mL
	5 mM	0.4571 mL	2.2856 mL	4.5712 mL	11.4280 mL
	10 mM	0.2286 mL	1.1428 mL	2.2856 mL	5.7140 mL
	15 mM	0.1524 mL	0.7619 mL	1.5237 mL	3.8093 mL
	20 mM	0.1143 mL	0.5714 mL	1.1428 mL	2.8570 mL
	25 mM	0.0914 mL	0.4571 mL	0.9142 mL	2.2856 mL
	30 mM	0.0762 mL	0.3809 mL	0.7619 mL	1.9047 mL
	40 mM	0.0571 mL	0.2857 mL	0.5714 mL	1.4285 mL
	50 mM	0.0457 mL	0.2286 mL	0.4571 mL	1.1428 mL
	60 mM	0.0381 mL	0.1905 mL	0.3809 mL	0.9523 mL
	80 mM	0.0286 mL	0.1429 mL	0.2857 mL	0.7143 mL
	100 mM	0.0229 mL	0.1143 mL	0.2286 mL	0.5714 mL

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