Pazopanib

製品コードS3012 バッチS301206

印刷

化学情報

Synonyms

GW786034

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₁H₂₃N₇O₂S

分子量

437.52

CAS No.

444731-52-6

Solubility (25°C)*

体外

DMSO (warmed with 50ºC water bath)

87 mg/mL (198.84 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.250mg/ml (0.57mM)	Taking the 1 mL working solution as an example, add 50 μL of 5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	1.650mg/ml (3.77mM)	Taking the 1 mL working solution as an example, add 50 μL of 33 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms/CSF1R with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces cathepsin B activation and autophagy.
in vitro	Pazopanib potently inhibits VEGF-induced phosphorylation of VEGFR2 in HUVEC cells with IC50 of 8 nM. ^[1] This compound shows dose-dependent growth inhibition in all synovial sarcoma cell lines including SYO-1 and HS-SY-II cells. Proliferation of SYO-1 and HS-SY-II cells is inhibited even at 1 µg/mL of this chemical and is completely abolished at 5 µg/mL. It induces G1 arrest, and thereby suppresses the growth of synovial sarcoma cells. Phosphorylation of Akts, GSK-3β, JNKs, p70 S6 Kinase, and mTOR is suppressed in this compound-treated SYO-1 cells compared with that in the vehicle-treated cells. ^[2] This chemical between 20 m g/mL and 22.5 m g/mL shows an increasing reduction of RPE cell viability. ^[3]
in vivo	The mice treated with 30 mg/kg or 100 mg/kg Pazopanib reveals a significant decrease in tumor burden compared with the mice treated with vehicle or 10 mg/kg this compound. Treatment with this agent is well-tolerated and there is no significant difference in the body weight among the mice in each group. ^[2]

製品説明

Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms/CSF1R with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces cathepsin B activation and autophagy.

in vitro

Pazopanib potently inhibits VEGF-induced phosphorylation of VEGFR2 in HUVEC cells with IC50 of 8 nM. ^[1]

This compound shows dose-dependent growth inhibition in all synovial sarcoma cell lines including SYO-1 and HS-SY-II cells. Proliferation of SYO-1 and HS-SY-II cells is inhibited even at 1 µg/mL of this chemical and is completely abolished at 5 µg/mL. It induces G1 arrest, and thereby suppresses the growth of synovial sarcoma cells. Phosphorylation of Akts, GSK-3β, JNKs, p70 S6 Kinase, and mTOR is suppressed in this compound-treated SYO-1 cells compared with that in the vehicle-treated cells. ^[2]

This chemical between 20 m g/mL and 22.5 m g/mL shows an increasing reduction of RPE cell viability. ^[3]

in vivo

The mice treated with 30 mg/kg or 100 mg/kg Pazopanib reveals a significant decrease in tumor burden compared with the mice treated with vehicle or 10 mg/kg this compound. Treatment with this agent is well-tolerated and there is no significant difference in the body weight among the mice in each group. ^[2]

プロトコル(参考用のみ)

キナーゼアッセイ	Kinase enzyme assays
キナーゼアッセイ	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 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 this 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.
細胞アッセイ	細胞株	Cell-free assays
	濃度	IC50 of 10, 30, 47, 84, 74, 140 and 146 nM for VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms/CSF1R, respectively.
	反応時間
	実験の流れ
動物実験	動物モデル	Immunodeficient mice bearing SYO-1 cells
	投薬量	0 mg/kg, 10 mg/kg, 30 mg/kg, or 100 mg/kg
	投与方法	Oral administration

参考

https://pubmed.ncbi.nlm.nih.gov/18620382/
https://pubmed.ncbi.nlm.nih.gov/22359392/
https://pubmed.ncbi.nlm.nih.gov/22466477/

カスタマーフィードバック

: Data from [Data independently produced by Expert Opin Pharmacother, 2014, 15(11), 1489-99]

: Data from [J Virol, 2011, 85(5), 2296-303]

: Data from [Data independently produced by , , Arch Toxicol, 2018, 92(4):1435-1451]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

The NEXT complex regulates H3K27me3 levels to affect cancer progression by degrading G4/U-rich lncRNAs [ Nucleic Acids Res, 2025, 53(4)gkaf107]	PubMed: 39988317
Exploiting collateral sensitivity in the evolution of resistance to tyrosine kinase inhibitors in soft tissue sarcomas [ Commun Biol, 2025, 8(1):1185]	PubMed: 40781553
Biofabrication of pheochromocytoma and paraganglioma tumor organoids and assessment of response to systemic therapy [ Sci Rep, 2025, 15(1):35889]	PubMed: 41087622
Targeting PDGF signaling of cancer-associated fibroblasts blocks feedback activation of HIF-1α and tumor progression of clear cell ovarian cancer [ Cell Rep Med, 2024, S2666-3791(24)00201-5]	PubMed: 38670097
Unveiling the antitumor synergy between pazopanib and metformin on lung cancer through suppressing p-Akt/ NF-κB/ STAT3/ PD-L1 signal pathway [ Biomed Pharmacother, 2024, 180:117468]	PubMed: 39332188
Melatonin alleviates chronic stress-induced hippocampal microglia pyroptosis and subsequent depression-like behaviors by inhibiting Cathepsin B/NLRP3 signaling pathway in rats [ Transl Psychiatry, 2024, 14(1):166]	PubMed: 38538614
Patient-derived rhabdomyosarcoma cells recapitulate the genetic and transcriptomic landscapes of primary tumors [ iScience, 2024, 27(10):110862]	PubMed: 39319271
Targeting the core program of metastasis with a novel drug combination [ Cancer Med, 2024, 13(11):e7291]	PubMed: 38826119
Extensive analysis of 59 sarcoma-related fusion genes identified pazopanib as a potential inhibitor to COL1A1-PDGFB fusion gene [ Cancer Sci, 2023, 114(10):4089-4100]	PubMed: 37592448
Extensive analysis of 59 sarcoma-related fusion genes identified pazopanib as a potential inhibitor to COL1A1-PDGFB fusion gene [ Cancer Sci, 2023, 10.1111/cas.15915]	PubMed: 37592448

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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