Pazopanib HCl | GW786034 Hydrochloride;Pazopanib HCl;GW786034 HCl | Tyrosine / EGF Receptor Protein Kinase Inhibitor | VEGFR | PDGFR | c-Kit

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盐酸帕唑帕尼 /Pazopanib HCl 99+%

货号：A623193 同义名： GW786034 Hydrochloride;Pazopanib HCl

Pazopanib HCl (GW786034 Hydrochloride)是一种新型多靶点抑制剂，对 VEGFR1、VEGFR2、VEGFR3、PDGFRβ、c-Kit、FGFR1 和 c-Fms 的 IC50 值分别为 10 nM、30 nM、47 nM、84 nM、74 nM、140 nM 和 146 nM。

Pazopanib HCl 化学结构
CAS号：635702-64-6

Pazopanib HCl 3D分子结构
CAS号：635702-64-6

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Pazopanib HCl 纯度/质量文件产品仅供科研

货号：A623193 标准纯度： 99+% 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Cell,2024. Ambeed. [ A125712 ]; • Cancer Discov., 2024. Ambeed. [ A285925 ]; • JMC, 2024. Ambeed. [ A288696 ]; • JMC, 2024. Ambeed. [ A524399 , A633512 , A144280 , A174613 ]; • EJNMMI Radiopharm. Chem., 2024, 9, 61. Ambeed. [ A1257961 , A622068 ]; 更多 >

c-Kit 亚型比较
PDGFR 亚型比较
VEGFR 亚型比较

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		99%+
Ki8751	++ c-Kit, IC50: 40 nM		99%+
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		99%+
Axitinib	++++ Kit, IC50: 1.7 nM		99%+
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	99%+
Dasatinib	++ c-Kit (D816V), IC50: 37 nM c-Kit (wt), IC50: 79 nM	Src	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	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				99%+
Pazopanib	++ PDGFR, IC50: 84 nM				99%
Imatinib	+ PDGFR, IC50: 100 nM			c-Kit	99%+
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	99%+
Tivozanib		++ PDGFRα, IC50: 40 nM	++ PDGFRβ, IC50: 49 nM		99%+
Ponatinib		++++ PDGFRα, IC50: 1.1 nM			99%+
Amuvatinib		++ PDGFRα (V561D), IC50: 40 nM			99%+
Axitinib		+++ PDGFRα, IC50: 5.0 nM	++++ PDGFRβ, IC50: 1.6 nM		99%+
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		99%+
Lactate			+++ PDGFRβ, IC50: 27 nM	FLT3,c-Kit	85%
Linifanib			++ PDGFRβ, IC50: 66 nM		99%+
AZD2932			+++ PDGFRβ, IC50: 4 nM	c-Kit	99%+
Dovitinib			+++ PDGFRβ, IC50: 27 nM	FLT3,c-Kit	99%+
Sorafenib			++ PDGFRβ, IC50: 57 nM mPDGFRβ, 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	99%+
Tivozanib	++ VEGFR1, IC50: 30 nM	+++ VEGFR2, IC50: 6.5 nM	++ VEGFR3, IC50: 15 nM		99%+
Brivanib	+ VEGFR1, IC50: 380 nM	++ VEGFR2, IC50: 25 nM Flk1, 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	FLT3,c-Kit	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/Flk1, IC50: 270 nM VEGFR2/KDR, IC50: 37 nM	+ VEGFR3/FLT4, IC50: 660 nM	c-Kit,c-Fms	99%+
Axitinib	++++ VEGFR1/FLT1, IC50: 0.1 nM	++++ VEGFR2/Flk1, IC50: 0.18 nM VEGFR2/KDR, IC50: 0.2 nM			99%+
Dovitinib	+++ VEGFR1/FLT1, IC50: 10 nM	+++ VEGFR2/Flk1, IC50: 13 nM	+++ VEGFR3/FLT4, IC50: 8 nM	FLT3,c-Kit	99%+
ZM 306416	+ VEGFR1, IC50: 0.33 μM			Src	99%+
KRN-633	+ VEGFR1, IC50: 170 nM	+ VEGFR2, IC50: 160 nM	+ VEGFR3, IC50: 125 nM	BTK,c-Kit	99%+
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		99%+
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			99%+
Cabozantinib S-malate		++++ VEGFR2/KDR, IC50: 0.035 nM			99+%
Ki8751		++++ VEGFR2, IC50: 0.9 nM		c-Kit	99%+
SU 5402		++ VEGFR2, IC50: 20 nM			99%+
Rivoceranib Mesylate		++++ VEGFR2, IC50: 1 nM		RET	99%+
Ponatinib		++++ VEGFR2, IC50: 1.5 nM			99%+
LY2874455		+++ VEGFR2, IC50: 7 nM			99%+
ZM323881 HCl		++++ VEGFR2, IC50: <2 nM			98%
AZD2932		+++ VEGFR-2, IC50: 8 nM		c-Kit	99%+
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			99%+
Semaxinib		+ VEGFR2/Flk1, IC50: 1.23 μM			98%
Vandetanib		++ VEGFR2, IC50: 40 nM	+ VEGFR3, IC50: 110 nM	EGFR	99%+
SAR131675			++ VEGFR3, IC50: 23 nM		99%+
ENMD-2076		+ VEGFR2/KDR, IC50: 58.2 nM	++ VEGFR3/FLT4, IC50: 15.9 nM	FLT3,RET	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 HCl 生物活性

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 hydrochloride is the hydrochloride form of Pazopanib. 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 HCl 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
5637		Growth inhibitory assay		IC50=15.0 μM	23887605
5637	20 μM	Autophagy assay		triggers the autophagic process	23887605
5637	20 μM	Function assay		induces lysosomal-dependent necrosis	23887605
5637	20 μM	Function assay		induces lysosome alteration and inhibits CB activity	23887605

Pazopanib HCl 动物研究

Dose

Mice: 300 mg/kg^[3] (i.p.), 10 mg/kg - 100 mg/kg^[1] (p.o.)

Administration

i.p., p.o.

Pharmacokinetics

Animal	Nude mice^[2]
Dose	30 mg/kg
Administration	p.o.
C_max	130 μM
T_1/2	4.6 h
AUC_inf	1500 μM·h

Pazopanib HCl 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 <<
NCT00788580	Unspecified Adult Solid Tumor,... 展开 >> Protocol Specific 收起 <<	Phase 1	Withdrawn(Study was discontinu... 展开 >>ed.) 收起 <<	-	-
NCT01027598	-		Completed	-	-

Pazopanib HCl 参考文献

[1]Harris PA, Boloor A, et al. Discovery of 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino] -2-pyrimidinyl] amino] -2-methyl-benzenesulfonamide (Pazopanib), a novel and potent vascular endothelial growth factor receptor inhibitor. J Med Chem. 2008 Aug 14;51(15):4632-40.

[2]Kumar R, Knick VB, et al. Pharmacokinetic-pharmacodynamic correlation from mouse to human with pazopanib, a multikinase angiogenesis inhibitor with potent antitumor and antiangiogenic activity. Mol Cancer Ther. 2007 Jul;6(7):2012-21.

[3]Wang YK, Yang XN, et al. A metabolomic perspective of pazopanib-induced acute hepatotoxicity in mice. Xenobiotica. 2019 Jun;49(6):655-670.

Pazopanib HCl 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.11mL

0.42mL

0.21mL

10.55mL

2.11mL

1.05mL

21.10mL

4.22mL

2.11mL

Pazopanib HCl 技术信息

CAS号	635702-64-6
分子式	C₂₁H₂₄ClN₇O₂S
分子量	473.979

别名	GW786034 Hydrochloride;Pazopanib HCl;GW786034 HCl
运输	蓝冰

存储条件

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 9 mg/mL(18.99 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

30% PEG400+0.5% Tween80+5% propylene glycol+water 30 mg/mL suspension

细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源

5637		Growth inhibitory assay	IC50=15.0 μM	23887605
5637	20 μM	Autophagy assay	triggers the autophagic process	23887605
5637	20 μM	Function assay	induces lysosomal-dependent necrosis	23887605
5637	20 μM	Function assay	induces lysosome alteration and inhibits CB activity	23887605
CEC	~10 μg/mL	Function assay	down-regulates VEGF levels	21620822
CEC	~5 μg/mL	Function assay	blocks endothelial cell migration	21620822
CRL1749	~10 μM	cytotoxicity assay	IC50=22.69 μM	21529900
Dox40	10 μg/mL	Growth inhibitory assay	inhibits MM Cell Growth	17164332
Dox40	20 μg/mL	cytotoxicity assay	inhibits MM Cell Survival	17164332
Dox40		Function assay	suppresses VEGF-Induced Endothelial Cell Proliferation and Migration.	17164332
HBMEC	~10 μM	Growth inhibitory assay	IC50=1 μM	21081656
HBMEC	~1 μM	Function assay	abrogates the phosphorylation of VEGFR2 with disruption of downstream PLCγ1	21081656
HBMEC	~1 μM	Function assay	disrupts the Ras-Raf-ERK pathway through decreased phosphorylated MEK1/2 and ERK1/2	21081656
HBMEC	~20 μM	Function assay	disrupts 50% of tube formation at 1 μM	21081656
HSC-39	5 μM	Growth inhibitory assay	blocks proliferation	25249557
HSC-39	~10 μM	cytotoxicity assay	IC50=0.1 to 2.0 μmol/L	25249557
HT1376	~10 μM	cytotoxicity assay	IC50=28.21 μM	21529900
HTB3	~10 μM	cytotoxicity assay	IC50=14.16 μM	21529900
HTB9	~10 μM	cytotoxicity assay	IC50=11.84 μM	21529900
HUVEC		Growth inhibitory assay	inhibits the VEGF-induced proliferation of HUVECs	18620382
HUVEC		Kinase assay	inhibits VEGF-induced phosphorylation of VEGFR-2 in HUVEC cells with an IC50 of ∼8 nM	18620382
INA-6	10 μg/mL	Growth inhibitory assay	inhibits MM Cell Growth	17164332
INA-6	20 μg/mL	cytotoxicity assay	inhibits MM Cell Survival	17164332
J82	~10 μM	cytotoxicity assay	IC50=24.57 μM	21529900
J82		Growth inhibitory assay	IC50=18.4 μM	23887605
J82	20 μM	Autophagy assay	triggers the autophagic process	23887605
J82	20 μM	Function assay	induces lysosomal-dependent necrosis	23887605
J82	20 μM	Function assay	induces lysosome alteration and inhibits CB activity	23887605
KATO-II	5 μM	Growth inhibitory assay	blocks proliferation	25249557
KATO-II	~10 μM	cytotoxicity assay	IC50=0.1 to 2.0 μmol/L	25249557
KATO-III	1 μM	Function assay	induces cell-cycle arrest	25249557
KATO-III	1 μM	Apoptosis assay	induces apoptosis	25249557
KATO-III	1 μM	Function assay	inhibits FGFR2 phosphorylation and downstream signaling molecules	25249557
MDA-MB-231	~10 μM	Growth inhibitory assay	IC50=5 μM	21081656
MDA-MB-231	0.5 μM	Function assay	inhibits the ERK1/2 signaling pathway	21081656
MDA-MB-231	5 μM	Function assay	induces a cell-cycle arrest	21081656
MM		Kinase assay	inhibits VEGF-induced phosphorylation of flt1	17164332
MM.1R	10 μg/mL	Growth inhibitory assay	inhibits MM Cell Growth	17164332
MM.1R	20 μg/mL	cytotoxicity assay	inhibits MM Cell Survival	17164332
MM.1R		Function assay	suppresses VEGF-Induced Endothelial Cell Proliferation and Migration.	17164332
MM.1S	10 μg/mL	Growth inhibitory assay	inhibits MM Cell Growth	17164332
MM.1S	20 μg/mL	cytotoxicity assay	inhibits MM Cell Survival	17164332
MM.1S		Function assay	suppresses VEGF-Induced Endothelial Cell Proliferation and Migration.	17164332
NIH 3T3	~10 μM	Growth inhibitory assay	inhibits cell growth and colony formation	25249557
OCUM-2M	5 μM	Growth inhibitory assay	blocks proliferation	25249557
OCUM-2M	~10 μM	cytotoxicity assay	IC50=0.1 to 2.0 μmol/L	25249557
OCUM-2M	1 μM	Function assay	induces cell-cycle arrest	25249557
OCUM-2M	1 μM	Apoptosis assay	induces apoptosis	25249557
OPM2	10 μg/mL	Growth inhibitory assay	inhibits MM Cell Growth	17164332
OPM2	20 μg/mL	cytotoxicity assay	inhibits MM Cell Survival	17164332
OPM2		Function assay	suppresses VEGF-Induced Endothelial Cell Proliferation and Migration.	17164332
RPE	~10 μg/mL	Function assay	down-regulates VEGF levels	21620822
RPMI	10 μg/mL	Growth inhibitory assay	inhibits MM Cell Growth	17164332
RPMI	20 μg/mL	cytotoxicity assay	inhibits MM Cell Survival	17164332
RT4	~10 μM	cytotoxicity assay	IC50=5.14 μM	21529900
SNU-16	5 μM	Growth inhibitory assay	blocks proliferation	25249557
SNU-16	~10 μM	cytotoxicity assay	IC50=0.1 to 2.0 μmol/L	25249557
Sup	~10 μM	cytotoxicity assay	IC50=53.32 μM	21529900
T24	~10 μM	cytotoxicity assay	IC50=52.45 μM	21529900
U266	10 μg/mL	Growth inhibitory assay	inhibits MM Cell Growth	17164332
U266	20 μg/mL	cytotoxicity assay	inhibits MM Cell Survival	17164332

盐酸帕唑帕尼 /Pazopanib HCl 99+%

Pazopanib HCl 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Pazopanib HCl 质控信息

Pazopanib HCl 生物活性

Pazopanib HCl 细胞研究

Pazopanib HCl 动物研究

Pazopanib HCl 临床研究

Pazopanib HCl 参考文献

Pazopanib HCl 实验方案

Pazopanib HCl 技术信息

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Pazopanib HCl 质控信息

Pazopanib HCl 生物活性

Pazopanib HCl 细胞研究

Pazopanib HCl 动物研究

Pazopanib HCl 临床研究

Pazopanib HCl 参考文献

Pazopanib HCl 实验方案

Pazopanib HCl 技术信息

最近浏览的产品

大规格询价

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