A multi-kinase inhibitor; inhibits VEGFR1

Pazopanib – 50 mg

Brand:
Cayman
CAS:
444731-52-6
Storage:
-20
UN-No:
Non-Hazardous - /

Pazopanib is a multi-kinase inhibitor that inhibits the VEGF receptors VEGFR1, VEGFR2, and VEGFR3 (IC50s = 10, 30, and 47 nM, respectively, in a cell-free enzyme assay).{37765} It also inhibits PDGFRα, PDGFRβ, and c-Kit (IC50s = 71, 84, and 74 nM, respectively, in a cell-free enzyme assay) as well as additional receptor tyrosine kinases. Pazopanib inhibits upregulation of the surface adhesion proteins ICAM-1 and VCAM-1 induced by VEGF in multiple myeloma cells cocultured with human umbilical vein endothelial cells (HUVECs) and decreases multiple myeloma cell adhesion to HUVECs.{29172} It also inhibits proliferation of multiple myeloma cells cocultured with HUVECs. Pazopanib (30 and 100 mg/kg) reduces tumor growth, induces apoptosis, decreases angiogenesis, and increases survival in a multiple myeloma mouse xenograft model. Formulations containing pazopanib have been used in the treatment of cancer.  

 

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SKU: 12097 - 50 mg Category:

Description

A multi-kinase inhibitor; inhibits VEGFR1, VEGFR2, and VEGFR3 (IC50s = 10, 30, and 47 nM, respectively); inhibits PDGFRα, PDGFRβ, and c-Kit (IC50s = 71, 84, and 74 nM, respectively) as well as additional receptor tyrosine kinases; inhibits VEGF-induced upregulation of ICAM-1 and VCAM-1 and inhibits adhesion of multiple myeloma cells to HUVECs and proliferation of multiple myeloma cells; reduces tumor growth, induces apoptosis, decreases angiogenesis, and increases survival in a multiple myeloma mouse xenograft model at 30 and 100 mg/kg

Formal name: 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide

Synonyms:  GSK-VEG10003|GW786034B

Molecular weight: 437.5

CAS: 444731-52-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|PDGFR Family||Product Type|Biochemicals|Kinase Inhibitors|VEGFR Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Angiogenesis||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling||Research Area|Cell Biology|Cell Signaling|Growth Factor Receptors||Research Area|Cell Biology|ECM & Adhesion Molecules

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