SML3076
Pazopanib hydrochloride
≥98% (HPLC)
Synonym(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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About This Item
Empirical Formula (Hill Notation):
C21H23N7O2S · xHCl
CAS Number:
Molecular Weight:
437.52 (free base basis)
UNSPSC Code:
12352200
NACRES:
NA.77
Quality Level
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.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Regulatory Information
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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
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
Hideki Imano et al.
Toxicology in vitro : an international journal published in association with BIBRA, 71, 105063-105063 (2020-12-04)
Vascular endothelial growth factor (VEGF) promotes tumor angiogenesis through stimulating the proliferation and survival of endothelial cells. The severe adverse events caused by VEGF inhibitors might include immune-related ones; however, details of the mechanism have not been elucidated. We tested
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