SML3076
Pazopanib hydrochloride
≥98% (HPLC)
Synonyme(s) :
5-[[4-[(2,3-Dimethyl-2H-indazol-6-yl)(methyl)amino]pyrimidin-2-yl]amino]-2-methylbenzenesulfonamide hydrochloride, 5-[[4-[(2,3-Dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzenesulfonamide, hydrochloride, GW 786034 HCl, GW 786034B, GW786034 HCl, GW786034B
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A propos de cet article
Formule empirique (notation de Hill) :
C21H23N7O2S · xHCl
Numéro CAS:
Poids moléculaire :
437.52 (free base basis)
NACRES:
NA.77
UNSPSC Code:
12352200
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assay
≥98% (HPLC)
form
powder
storage condition
desiccated
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Biochem/physiol Actions
Orally active receptor tyrosine kinase inhibitor against VEGFR (Flt-1/KDR/Flt-4), PDGFR1/2, and KIT with anti-angiogenesis efficacy in vitro and in vivo.
Pazopanib is an orally active receptor tyrosine kinases inhibitor against VEGFR1/2/3 (IC50 = 10/30/47 nM), PDGFR1/2 (IC50 = 84/71 nM) and c-Kit (IC50 = 74 nM), exhibiting reduced or no potency toward FGFR1/3 (IC50 = 140/130 nM), c-fms (IC50 = 146 nM), and other kinases tested (IC50 from >400 nM to >20 μM). Pazopanib exhibits anti-cancer efficacy in cultures (IC50 from 5 to 15 μg/mL; multiple myeloma migration and survival) and in mice in vivo (30-100 mg/kg/day p.o. against human MM xenografts) via angiogenesis inhibition and apoptosis induction.
Classe de stockage
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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Klaus Podar et al.
Proceedings of the National Academy of Sciences of the United States of America, 103(51), 19478-19483 (2006-12-14)
A critical role for vascular endothelial factor (VEGF) has been demonstrated in multiple myeloma (MM) pathogenesis. Here, we characterized the effect of the small-molecule VEGF receptor inhibitor pazopanib on MM cells in the bone marrow milieu. Pazopanib inhibits VEGF-triggered signaling
Baran Akagunduz et al.
Experimental animals, 70(2), 169-176 (2020-11-27)
Pazopanib is a tyrosine kinase inhibitor that is generally used for the treatment of metastatic renal cell cancer and advanced soft tissue sarcoma. It can cause various degrees of hepatotoxicity. Our study aimed to investigate the effect of taxifolin on
Chiao-Yun Lin et al.
Journal of molecular medicine (Berlin, Germany), 98(8), 1175-1188 (2020-07-09)
Pazopanib-a multitargeted tyrosine kinase inhibitor with prominent antiangiogenic effects-has shown promise in the treatment of soft-tissue sarcomas. Hyperthermia has been also applied as an adjunctive treatment to chemotherapy for these malignancies. Here, we show that pazopanib and hyperthermia act synergistically
Katerina Stamati et al.
Journal of tissue engineering, 11, 2041731420920597-2041731420920597 (2020-06-04)
Pazopanib is a tyrosine kinase inhibitor used to treat renal cell carcinoma. Few in vitro studies investigate its effects towards cancer cells or endothelial cells in the presence of cancer. We tested the effect of Pazopanib on renal cell carcinoma
Adrian Georg Simon et al.
Journal of cancer research and clinical oncology, 146(9), 2255-2265 (2020-06-14)
To investigate the synergistic effect of glycolysis inhibition on therapy answer to tyrosine kinase inhibitors in renal carcinoma. Primary cell cultures from 33 renal tumors including clear cell RCC (ccRCC), papillary RCC and the rare subtype chromophobe RCC as well
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