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Pazopanib HCl
点击次数：205发布时间：2013/4/2 10:12:19
更新日期：2022/8/19 17:45:40
所 在 地：美洲
产品型号：
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详细内容
Pazopanib HCl
上海义森生物科技有限公司
技术数据:
分子量（MW）: 473.98 
化学式: C21H23N7O2S.HCl
溶解度: DMSO 70mg/mL Water 17mg/mL Ethanol <1mg/mL 纯度: 98% 稳定性: at -20℃ 2 years CAS号: 635702-64-6, 444731-52-6 （free base）
生物活性
VEGFR enzyme assays for VEGGR1,VEGFR2 ａnd VEGFR3 were running 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.
Pazopanib HCl showed good potency against all the human VEGFR receptors with an IC50 of 10, 30, ａnd 47 nM for VEGFR-1, -2, ａnd -3, respectively. Significant activity was also seen against the closely related tyrosine receptor kinases PDGFR beta, c-Kit, FGF-R1, ａnd c-fms with IC50’s of 84, 74, 140,and 146 nM, respectively. In cellular assays, in addition to inhibiting the VEGF-induced proliferation of HUVECs, Pazopanib HCl potently inhibited VEGF-induced phosphorylation of VEGFR-2 in HUVEC cells with an IC50 of ∼8 nM.
The cytochrome P450 profile was also improved with inhibition >10 μM against the isozymes tested, with the exception of 2C9 （7.9 μM）. [1]
技术数据:
| 分子量（MW）: | 473.98 | |
|---|---|---|
| 化学式: | C21H23N7O2S.HCl | |
| 溶解度: | DMSO 70mg/mL Water 17mg/mL Ethanol <1mg/mL | |
| 纯度: | 98% | |
| 稳定性: | at -20℃ 2 years | |
| CAS号: | 635702-64-6, 444731-52-6 （free base） |
生物活性
VEGFR enzyme assays for VEGGR1,VEGFR2 ａnd VEGFR3 were running 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.
Pazopanib HCl showed good potency against all the human VEGFR receptors with an IC50 of 10, 30, ａnd 47 nM for VEGFR-1, -2, ａnd -3, respectively. Significant activity was also seen against the closely related tyrosine receptor kinases PDGFR beta, c-Kit, FGF-R1, ａnd c-fms with IC50’s of 84, 74, 140,and 146 nM, respectively. In cellular assays, in addition to inhibiting the VEGF-induced proliferation of HUVECs, Pazopanib HCl potently inhibited VEGF-induced phosphorylation of VEGFR-2 in HUVEC cells with an IC50 of ∼8 nM.
The cytochrome P450 profile was also improved with inhibition >10 μM against the isozymes tested, with the exception of 2C9 （7.9 μM）. [1]
