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帕唑帕尼 /Pazopanib {[allProObj[0].p_purity_real_show]}

货号:A135375 同义名: GW786034;GSK-VEG10003

Pazopanib(GW786034)是一种新型多靶点抑制剂,对VEGFR1VEGFR2VEGFR3PDGFRβc-KitFGFR1c-FmsIC50值分别为10 nM、30 nM、47 nM、84 nM、74 nM、140 nM和146 nM。

Pazopanib 化学结构 CAS号:444731-52-6
Pazopanib 化学结构
CAS号:444731-52-6
Pazopanib 3D分子结构
CAS号:444731-52-6
Pazopanib 化学结构 CAS号:444731-52-6
Pazopanib 3D分子结构 CAS号:444731-52-6
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Pazopanib 纯度/质量文件 产品仅供科研

货号:A135375 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 c-Kit 其他靶点 纯度
Tyrphostin AG1296 +

c-Kit (Swiss 3T3), IC50: 1.8 μM

PDGFR 99%+
Masitinib +

Kit, IC50: 200 nM

99%+
Motesanib Diphosphate +++

Kit, IC50: 8 nM

98%
Ki8751 ++

c-Kit, IC50: 40 nM

98+%
Tivozanib ++

c-Kit, IC50: 78 nM

99%+
Pazopanib +

c-Kit, IC50: 140 nM

99%
Sitravatinib +++

Kit, IC50: 6 nM

99%+
Pexidartinib +++

Kit, IC50: 10 nM

99%+
Lactate ++++

c-Kit, IC50: 2 nM

FLT3 85%
Amuvatinib +++

c-Kit (D816H), IC50: 10 nM

99%+
Imatinib Mesylate +

c-Kit, IC50: 100 nM

PDGFR 99%
AZD2932 +++

c-Kit, IC50: 9 nM

98%
Axitinib ++++

Kit, IC50: 1.7 nM

98%
Dovitinib ++++

c-Kit, IC50: 2 nM

FLT3 99%+
Sunitinib FLT3 98%
OSI-930 +

Kit, IC50: 80 nM

99%+
Telatinib ++++

c-Kit, IC50: 1 nM

99%+
Dasatinib monohydrate ++

c-Kit (D816V), IC50: 37 nM

c-Kit (wt), IC50: 79 nM

Src 98%
Dasatinib ++

c-Kit (D816V), IC50: 37 nM

c-Kit (wt), IC50: 79 nM

Src 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。
产品名称 PDGFR PDGFRα PDGFRβ 其他靶点 纯度
Tyrphostin A9 +

PDGFR, IC50: 0.5 μM

EGFR 98%
Tyrphostin AG1296 99%+
Motesanib Diphosphate ++

PDGFR, IC50: 84 nM

98%
Pazopanib ++

PDGFR, IC50: 84 nM

99%
Imatinib +

PDGFR, IC50: 100 nM

c-Kit 98%
Imatinib Mesylate +

PDGFR, IC50: 100 nM

c-Kit 99%
Sennoside B 99%+
PP121 ++++

PDGFR, IC50: 2 nM

mTOR,VEGFR 99%+
Crenolanib ++++

PDGFRα, Kd: 2.1 nM

++++

PDGFRβ, Kd: 3.2 nM

99%+
Masitinib +

PDGFRα, IC50: 540 nM

+

PDGFRβ, IC50: 800 nM

99%+
Ki8751 ++

PDGFRα, IC50: 67 nM

c-Kit 98+%
Tivozanib ++

PDGFRα, IC50: 40 nM

++

PDGFRβ, IC50: 49 nM

99%+
Ponatinib ++++

PDGFRα, IC50: 1.1 nM

98%
Amuvatinib ++

PDGFRα (V561D), IC50: 40 nM

99%+
Axitinib +++

PDGFRα, IC50: 5.0 nM

++++

PDGFRβ, IC50: 1.6 nM

98%
CP-673451 +++

PDGFRα, IC50: 10 nM

++++

PDGFRβ, IC50: 1 nM

99%+
Telatinib +++

PDGFRα, IC50: 15 nM

c-Kit 99%+
Nintedanib ++

PDGFRα, IC50: 59 nM

++

PDGFRβ, IC50: 65 nM

99+%
Avapritinib ++++

PDGFRα (D842V), IC50: 0.5 nM

99%+
MK-2461 +++

PDGFRβ, IC50: 22 nM

98%+
Lactate +++

PDGFRβ, IC50: 27 nM

c-Kit,FLT3 85%
Linifanib ++

PDGFRβ, IC50: 66 nM

99%+
AZD2932 +++

PDGFRβ, IC50: 4 nM

c-Kit 98%
Dovitinib +++

PDGFRβ, IC50: 27 nM

c-Kit,FLT3 99%+
Sorafenib ++

mPDGFRβ, IC50: 57 nM

PDGFRβ, IC50: 57 nM

99%
Sunitinib ++++

PDGFRβ , IC50: 2 nM

FLT3 98%
Orantinib +++

PDGFRβ, Ki: 8 nM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。
产品名称 VEGFR1 VEGFR2 VEGFR3 其他靶点 纯度
Motesanib Diphosphate ++++

VEGFR1, IC50: 2 nM

++++

VEGFR2/Flk1, IC50: 3 nM

VEGFR2, IC50: 3 nM

+++

VEGFR3, IC50: 6 nM

RET,PDGFR 98%
Tivozanib ++

VEGFR1, IC50: 30 nM

+++

VEGFR2, IC50: 6.5 nM

++

VEGFR3, IC50: 15 nM

99%+
Brivanib +

VEGFR1, IC50: 380 nM

++

Flk1, IC50: 25 nM

VEGFR2, IC50: 25 nM

99%+
Regorafenib +++

VEGFR1, IC50: 13 nM

+++

VEGFR2, IC50: 4.2 nM

+

VEGFR3, IC50: 46 nM

RET 98%
Pazopanib +++

VEGFR1, IC50: 10 nM

++

VEGFR2, IC50: 30 nM

+

VEGFR3, IC50: 47 nM

FGFR,c-Kit,PDGFR 99%
Sitravatinib +++

VEGFR1 (FLT1), IC50: 6 nM

+++

VEGFR2 (KDR), IC50: 5 nM

++++

VEGFR3 (FLT4), IC50: 2 nM

99%+
Foretinib +++

VEGFR1/FLT1, IC50: 6.8 nM

++++

KDR, IC50: 0.86 nM

++++

VEGFR3/FLT4, IC50: 2.8 nM

Tie-2 99%+
MGCD-265 analog ++++

VEGFR1, IC50: 3 nM

++++

VEGFR2, IC50: 3 nM

++++

VEGFR3, IC50: 4 nM

Tie-2 99%+
Lactate +++

VEGFR1/FLT1, IC50: 10 nM

+++

VEGFR2/Flk1, IC50: 13 nM

+++

VEGFR3/FLT4, IC50: 8 nM

c-Kit,FLT3 85%
AEE788 +

FLT1, IC50: 59 nM

+

KDR, IC50: 77 nM

EGFR 98+%
Linifanib ++++

VEGFR1/FLT1, IC50: 3 nM

++++

VEGFR2/KDR, IC50: 4 nM

+

VEGFR3/FLT4, IC50: 190 nM

FLT3 99%+
Vatalanib 2HCl +

VEGFR1/FLT1, IC50: 77 nM

++

VEGFR2/KDR, IC50: 37 nM

VEGFR2/Flk1, IC50: 270 nM

+

VEGFR3/FLT4, IC50: 660 nM

c-Kit,c-Fms 99%+
Axitinib ++++

VEGFR1/FLT1, IC50: 0.1 nM

++++

VEGFR2/KDR, IC50: 0.2 nM

VEGFR2/Flk1, IC50: 0.18 nM

98%
Dovitinib +++

VEGFR1/FLT1, IC50: 10 nM

+++

VEGFR2/Flk1, IC50: 13 nM

+++

VEGFR3/FLT4, IC50: 8 nM

c-Kit,FLT3 99%+
ZM 306416 +

VEGFR1, IC50: 0.33 μM

Src 99%+
KRN-633 +

VEGFR1, IC50: 170 nM

+

VEGFR2, IC50: 160 nM

+

VEGFR3, IC50: 125 nM

c-Kit,BTK 98%
OSI-930 +++

FLT1, IC50: 8 nM

+++

KDR, IC50: 9 nM

99%+
Lenvatinib ++

VEGFR1/FLT1, IC50: 22 nM

++++

VEGFR2/KDR, IC50: 4.0 nM

+++

VEGFR3/FLT4, IC50: 5.2 nM

98%
NVP-BAW2881 +

hVEGFR1, IC50: 820 nM

+++

mVEGF2, IC50: 165 nM

hVEGFR2, IC50: 9 nM

+

hVEGFR3, IC50: 420 nM

98%
Cediranib +++

VEGFR1/FLT1, IC50: 5 nM

++++

VEGFR2/KDR, IC50: 0.5 nM

c-Kit 99%+
Nintedanib ++

VEGFR1, IC50: 34 nM

+++

VEGFR2, IC50: 13 nM

+++

VEGFR3, IC50: 13 nM

FLT3 99+%
BMS-794833 ++

VEGFR2, IC50: 15 nM

99%+
SKLB1002 ++

VEGFR2, IC50: 32 nM

98%
Cabozantinib S-malate ++++

VEGFR2/KDR, IC50: 0.035 nM

99+%
Ki8751 ++++

VEGFR2, IC50: 0.9 nM

c-Kit 98+%
SU 5402 ++

VEGFR2, IC50: 20 nM

98%
Rivoceranib Mesylate ++++

VEGFR2, IC50: 1 nM

RET 98+%
Ponatinib ++++

VEGFR2, IC50: 1.5 nM

98%
LY2874455 +++

VEGFR2, IC50: 7 nM

99%+
ZM323881 HCl ++++

VEGFR2, IC50: <2 nM

98%
AZD2932 +++

VEGFR-2, IC50: 8 nM

c-Kit 98%
Cabozantinib ++++

VEGFR2/KDR, IC50: 0.035 nM

98%
Sorafenib ++

VEGFR2/Flk1, IC50: 90 nM

VEGFR2, IC50: 90 nM

99%
CYC-116 ++

VEGFR2, Ki: 44 nM

FLT3 99%+
Golvatinib ++

VEGFR2, IC50: 16 nM

99%+
Sunitinib +

VEGFR2 , IC50: 80 nM

FLT3 98%
RAF265 ++

VEGFR2, EC50: 30 nM

99%+
PD173074 99%+
BFH772 ++++

VEGFR2, IC50: 3 nM

98%
Semaxinib +

VEGFR2/Flk1, IC50: 1.23 μM

98%
Vandetanib ++

VEGFR2, IC50: 40 nM

+

VEGFR3, IC50: 110 nM

EGFR 98%
SAR131675 ++

VEGFR3, IC50: 23 nM

99%+
ENMD-2076 +

VEGFR2/KDR, IC50: 58.2 nM

++

VEGFR3/FLT4, IC50: 15.9 nM

RET,FLT3 98%
Telatinib +++

VEGFR2, IC50: 6 nM

++++

VEGFR3, IC50: 4 nM

c-Kit 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Pazopanib 生物活性

靶点
  • VEGFR1

    VEGFR1, IC50:10 nM

  • VEGFR3

    VEGFR3, IC50:47 nM

  • VEGFR2

    VEGFR2, IC50:30 nM

  • PDGFR

    PDGFR, IC50:84 nM

描述 VEGF/VEGFR (vascular endothelial growth factor vascular endothelial growth factor receptor) pathway plays a key role in tumor angiogenesis by promotion of vascular and lymphatic endothelial, as well as survival, and invasion, thus resulting in neovascularization, tumor growth and metastasis. In addition, blockade of additional proangiogenic receptor tyrosine kinases, including PDGFR and FGFR, may improve long-term clinical outcomes. Pazopanib is a pan VEGFR inhibitor with IC50 values of 10nM, 30nM and 47nM for VEGFR1, VEGFR2 and VEGFR3 (measured by HTRF), respectively, less potent to c-Kit, PDGFR, FGFR and c-Fms with IC50 values of 74nM, 84nM, 140nM and 146nM. In cellular studies, Pazopanib inhibited VEGF/bFGF-induced proliferation of HUVECs with IC50 value of 21nM/720nM, as well as potently inhibited VEGF-induced the phosphorylation of VEGFR-2 with IC50 value of ∼8nM. As prediction by the inhibition of VEGFR and FGFR, matrigel plug assay showed that once-daily oral administration of Pazopanib at dose of 30mg/kg and 100mg/kg inhibited angiogenesis by 57% and 83%, respectively, in female swiss nu/nu mice, as well as achieved tumor inhibition by 32%, 59% and 69% in HT29 xenograft, 16%, 35% and 55% in A375P xenograft, 99%, 102% and 110% in HN5 xenograft at dose of 10mg/kg, 30mg/kg and 100mg/kg[1].
作用机制 Pazopanib is an ATP-competitive inhibitor of human VEGFR2.[2]

Pazopanib 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
Daudi cell Growth inhibition assay Inhibition of human LB1047-RCC cell growth in a cell viability assay, IC50=3.53164 μM SANGER
human A172 cell Growth inhibition assay Inhibition of human A172 cell growth in a cell viability assay, IC50=3.7379 μM SANGER
human A204 cell Growth inhibition assay Inhibition of human A204 cell growth in a cell viability assay, IC50=109.06 nM SANGER
human A375P cells Proliferation assay Antiproliferative activity against human A375P cells in serum containing medium 18620382

Pazopanib 动物研究

Dose Mice: 30 mg/kg - 100 mg/kg[3] (p.o., BID)
Administration p.o.
Pharmacokinetics
Animal Rats[4] Dogs[4] Monkeys[4]
Dose 10 mg/kg 1 mg/kg 5 mg/kg
Administration i.v. or p.o. i.v. or p.o. i.v. or p.o.
F 72% (p.o.) 47% (p.o.) 49% (p.o.)
T1/2 3.6 h (i.v.) 2.2 h (i.v.) 4.7 h (i.v.)
CL 1.7 ml/min/kg (i.v.) 1.4 ml/min/kg (i.v.) 1.6 ml/min/kg (i.v.)
Vdss 0.478 L/kg (i.v.) 0.297 L/kg (i.v.) 0.283 L/kg (i.v.)

Pazopanib 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01027598 Non Small Cell Lung Cancer Phase 2 Completed - United States, Florida ... 展开 >> Florida Cancer Specialists Fort Myers, Florida, United States, 33901 United States, Georgia Suburban Hem Onc Lawrenceville, Georgia, United States, 30045 United States, Ohio Oncology Hematology Care Cincinnati, Ohio, United States, 45242 United States, South Carolina South Carolina Oncology Associates, PA Columbia, South Carolina, United States, 29210 United States, Tennessee Chattanooga Oncology Hematology Associates Chattanooga, Tennessee, United States, 37404 Family Cancer Center Collerville, Tennessee, United States, 38119 Tennessee Oncology, PLLC Nashville, Tennessee, United States, 37023 United States, Virginia Virginia Cancer Institute Richmond, Virginia, United States, 23235 收起 <<
NCT01027598 - Completed - -
NCT01407562 Unspecified Adult Solid Tumor ... 展开 >>- Protocol Specific Breast Cancer - Female 收起 << Phase 1 Active, not recruiting June 2019 United States, New Jersey ... 展开 >> Rutgers Cancer Institute of New Jersey New Brunswick, New Jersey, United States, 08903 收起 <<

Pazopanib 参考文献

[1]Gril B, Palmieri D, et al. The B-Raf status of tumor cells may be a significant determinant of both antitumor and anti-angiogenic effects of pazopanib in xenograft tumor models. PLoS One. 2011;6(10):e25625.

[2]GW-786034

Pazopanib 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.29mL

0.46mL

0.23mL

11.43mL

2.29mL

1.14mL

22.86mL

4.57mL

2.29mL

Pazopanib 技术信息

CAS号444731-52-6
分子式C21H23N7O2S
分子量 437.52
别名 GW786034;GSK-VEG10003;GW786034B
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature

溶解度

DMSO: 50 mg/mL(114.28 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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