SML3076
Pazopanib hydrochloride
≥98% (HPLC)
别名:
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
经验公式（希尔记法）:
C21H23N7O2S · xHCl
CAS号:
分子量:
437.52 (free base basis)
UNSPSC代码:
12352200
NACRES:
NA.77
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生化/生理作用
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.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
历史批次信息供参考:
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
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
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
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
Rakesh Kumar et al.
Molecular cancer therapeutics, 6(7), 2012-2021 (2007-07-11)
With the development of targeted therapeutics, especially for small-molecule inhibitors, it is important to understand whether the observed in vivo efficacy correlates with the modulation of desired/intended target in vivo. We have developed a small-molecule inhibitor of all three vascular
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