ZM323881 HCl | ZM 323881 (hydrochloride) | VEGFR Inhibitor

ZM323881 HCl {[allProObj[0].p_purity_real_show]}

货号：A652756 同义名： ZM 323881 (hydrochloride); ZM323881 hydrochloride

ZM323881 HCl是一种选择性很强的VEGFR2抑制剂，IC50小于2 nM，对VEGFR1、PDGFRβ、FGFR1、EGFR和ErbB2几乎没有活性。

ZM323881 HCl 化学结构
CAS号：193000-39-4

ZM323881 HCl 3D分子结构
CAS号：193000-39-4

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VEGFR 亚型比较

产品名称	VEGFR1 ↓ ↑	VEGFR2 ↓ ↑	VEGFR3 ↓ ↑	其他靶点	纯度
Motesanib Diphosphate	++++ VEGFR1, IC50: 2 nM	++++ VEGFR2, IC50: 3 nM VEGFR2/Flk1, IC50: 3 nM	+++ VEGFR3, IC50: 6 nM	RET,PDGFR	97%
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,PDGFR,c-Kit	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/KDR, IC50: 37 nM VEGFR2/Flk1, IC50: 270 nM	+ VEGFR3/FLT4, IC50: 660 nM	c-Fms/CSF1R,c-Kit	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	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	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	+++ hVEGFR2, IC50: 9 nM mVEGF2, IC50: 165 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			98%
Apatinib 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	99%
Cabozantinib		++++ VEGFR2/KDR, IC50: 0.035 nM			98%
Sorafenib		++ VEGFR2, IC50: 90 nM VEGFR2/Flk1, 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	99%
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。

ZM323881 HCl 生物活性

靶点

VEGFR2

VEGFR2, IC50:<2 nM

描述

ZZZM 323881 hydrochloride is a potent and selective VEGFR2 inhibitor with IC50 of < 2 nM, almost no activity on VEGFR1, PDGFRβ, FGFR1, EGFR and ErbB2.

ZM323881 HCl 细胞实验

Cell Line ARPE-19 cells Primary porcine RPE cells Rat primary cortical neurons ARPE-19 cells ARPE19 cells HfRPE cells Wistar rat glomeruli NCI-H460/MX20 cells HEK/ABCG2-R482 cells HEK/ABCG2-R482G cells HEK/ABCG2-R482T cells	Concentration	Treated Time	Description	References
ARPE-19 cells	10 nM	1 hour	Blocked the VEGF-E-induced decrease in TER	Exp Eye Res. 2007 Dec;85(6):762-71.
Primary porcine RPE cells	10 nM	1 hour	Blocked the VEGF-E-induced decrease in TER	Exp Eye Res. 2007 Dec;85(6):762-71.
Rat primary cortical neurons	10 nM	24 hours	To investigate the effect of ZM323881 on ketamine or VEGF 164-induced increase in dendritic branching, results showed that ZM323881 completely blocked these effects.	Am J Psychiatry. 2019 May 1;176(5):388-400.
ARPE-19 cells	10 nM	5 days	Inhibition of VEGF signaling pathway, induction of EMT and up-regulation of CCN2 expression	Sci Rep. 2024 Jun 17;14(1):13920.
ARPE19 cells	10 nM	6 hours	To evaluate the effect of ZM323881 on Glyc-alb-induced RPE barrier dysfunction, results showed that pretreatment with ZM323881 reversed the TEER reduction caused by Glyc-alb	Exp Eye Res. 2015 Aug;137:50-6.
HfRPE cells	10 nM	6 hours	To evaluate the effect of ZM323881 on Glyc-alb-induced RPE barrier dysfunction, results showed that pretreatment with ZM323881 reversed the TEER reduction caused by Glyc-alb	Exp Eye Res. 2015 Aug;137:50-6.
Wistar rat glomeruli	10 nM	60 minutes	To study the effect of ZM323881 on VEGF-induced elevation of glomerular ultrafiltration coefficient (LpA/Vi), results showed that ZM323881 significantly inhibited the VEGF-induced increase in LpA/Vi	J Physiol. 2006 Jan 1;570(Pt 1):141-56.
NCI-H460/MX20 cells	5 µM and 10 µM	72 hours	ZM323881 significantly decreased the cytotoxic doses of mitoxantrone and SN-38 in BCRP-overexpressing NCI-H460/MX20 cells, reversing BCRP-mediated multidrug resistance.	Biochem Pharmacol. 2017 May 15;132:29-37.
HEK/ABCG2-R482 cells	5 µM and 10 µM	72 hours	ZM323881 significantly decreased the IC50 values of mitoxantrone and SN-38 in HEK/ABCG2-R482 cells, reversing BCRP-mediated multidrug resistance.	Biochem Pharmacol. 2017 May 15;132:29-37.
HEK/ABCG2-R482G cells	5 µM and 10 µM	72 hours	ZM323881 significantly decreased the IC50 values of mitoxantrone and SN-38 in HEK/ABCG2-R482G cells, reversing BCRP-mediated multidrug resistance.	Biochem Pharmacol. 2017 May 15;132:29-37.
HEK/ABCG2-R482T cells	5 µM and 10 µM	72 hours	ZM323881 significantly decreased the IC50 values of mitoxantrone and SN-38 in HEK/ABCG2-R482T cells, reversing BCRP-mediated multidrug resistance.	Biochem Pharmacol. 2017 May 15;132:29-37.

Cell Line

Concentration

Treated Time

Description

References

ARPE-19 cells

10 nM

1 hour

Blocked the VEGF-E-induced decrease in TER

Exp Eye Res. 2007 Dec;85(6):762-71.

Primary porcine RPE cells

10 nM

1 hour

Blocked the VEGF-E-induced decrease in TER

Exp Eye Res. 2007 Dec;85(6):762-71.

Rat primary cortical neurons

10 nM

24 hours

To investigate the effect of ZM323881 on ketamine or VEGF 164-induced increase in dendritic branching, results showed that ZM323881 completely blocked these effects.

Am J Psychiatry. 2019 May 1;176(5):388-400.

ARPE-19 cells

10 nM

5 days

Inhibition of VEGF signaling pathway, induction of EMT and up-regulation of CCN2 expression

Sci Rep. 2024 Jun 17;14(1):13920.

ARPE19 cells

10 nM

6 hours

To evaluate the effect of ZM323881 on Glyc-alb-induced RPE barrier dysfunction, results showed that pretreatment with ZM323881 reversed the TEER reduction caused by Glyc-alb

Exp Eye Res. 2015 Aug;137:50-6.

HfRPE cells

10 nM

6 hours

To evaluate the effect of ZM323881 on Glyc-alb-induced RPE barrier dysfunction, results showed that pretreatment with ZM323881 reversed the TEER reduction caused by Glyc-alb

Exp Eye Res. 2015 Aug;137:50-6.

Wistar rat glomeruli

10 nM

60 minutes

To study the effect of ZM323881 on VEGF-induced elevation of glomerular ultrafiltration coefficient (LpA/Vi), results showed that ZM323881 significantly inhibited the VEGF-induced increase in LpA/Vi

J Physiol. 2006 Jan 1;570(Pt 1):141-56.

NCI-H460/MX20 cells

5 µM and 10 µM

72 hours

ZM323881 significantly decreased the cytotoxic doses of mitoxantrone and SN-38 in BCRP-overexpressing NCI-H460/MX20 cells, reversing BCRP-mediated multidrug resistance.

Biochem Pharmacol. 2017 May 15;132:29-37.

HEK/ABCG2-R482 cells

5 µM and 10 µM

72 hours

ZM323881 significantly decreased the IC50 values of mitoxantrone and SN-38 in HEK/ABCG2-R482 cells, reversing BCRP-mediated multidrug resistance.

Biochem Pharmacol. 2017 May 15;132:29-37.

HEK/ABCG2-R482G cells

5 µM and 10 µM

72 hours

ZM323881 significantly decreased the IC50 values of mitoxantrone and SN-38 in HEK/ABCG2-R482G cells, reversing BCRP-mediated multidrug resistance.

Biochem Pharmacol. 2017 May 15;132:29-37.

HEK/ABCG2-R482T cells

5 µM and 10 µM

72 hours

ZM323881 significantly decreased the IC50 values of mitoxantrone and SN-38 in HEK/ABCG2-R482T cells, reversing BCRP-mediated multidrug resistance.

Biochem Pharmacol. 2017 May 15;132:29-37.

ZM323881 HCl 动物实验

Species Dutch-belted rabbits Dutch Belted rabbits Frogs	Animal Model Diabetic retinopathy model Subretinal bleb resorption model Mesenteric microvessels	Administration	Dosage	Frequency	Description	References
Dutch-belted rabbits	Diabetic retinopathy model	Intravitreal injection	1 μM	Single injection, assessed after 48 hours	To evaluate the effect of ZM323881 on Glyc-alb-induced RPE dysfunction, results showed that ZM323881 reversed the reduction in RPE fluid resorption caused by Glyc-alb	Exp Eye Res. 2015 Aug;137:50-6.
Dutch Belted rabbits	Subretinal bleb resorption model	Intravitreal injection	10 µM	Single dose 1 hour prior	To inhibit the effect of VEGF on subretinal fluid resorption, results showed that ZM323881 reversed the VEGF-induced decrease in fluid resorption	Invest Ophthalmol Vis Sci. 2014 Apr 9;55(4):2269-75
Frogs	Mesenteric microvessels	Perfusion	10 nM	Single administration, lasting 5 minutes	To determine whether VEGF165b increases permeability via VEGF-R2 signaling, results showed that ZM323881 does not block the VEGF165b-induced increase in permeability.	J Physiol. 2006 Apr 1;572(Pt 1):243-57

Species

Dutch-belted rabbits Dutch Belted rabbits Frogs

Animal Model

Diabetic retinopathy model Subretinal bleb resorption model Mesenteric microvessels

Administration

Dosage

Frequency

Description

References

Dutch-belted rabbits

Diabetic retinopathy model

Intravitreal injection

1 μM

Single injection, assessed after 48 hours

To evaluate the effect of ZM323881 on Glyc-alb-induced RPE dysfunction, results showed that ZM323881 reversed the reduction in RPE fluid resorption caused by Glyc-alb

Exp Eye Res. 2015 Aug;137:50-6.

Dutch Belted rabbits

Subretinal bleb resorption model

Intravitreal injection

10 µM

Single dose 1 hour prior

To inhibit the effect of VEGF on subretinal fluid resorption, results showed that ZM323881 reversed the VEGF-induced decrease in fluid resorption

Invest Ophthalmol Vis Sci. 2014 Apr 9;55(4):2269-75

Frogs

Mesenteric microvessels

Perfusion

10 nM

Single administration, lasting 5 minutes

To determine whether VEGF165b increases permeability via VEGF-R2 signaling, results showed that ZM323881 does not block the VEGF165b-induced increase in permeability.

J Physiol. 2006 Apr 1;572(Pt 1):243-57

ZM323881 HCl 参考文献

ZM323881 HCl 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.43mL

0.49mL

0.24mL

12.14mL

2.43mL

1.21mL

24.28mL

4.86mL

2.43mL

ZM323881 HCl 技术信息

CAS号	193000-39-4
分子式	C₂₂H₁₉ClFN₃O₂
分子量	411.86
SMILES Code	CC1=C(O)C=C(NC2=C3C=CC(OCC4=CC=CC=C4)=CC3=NC=N2)C(F)=C1.Cl
MDL No.	MFCD08703130

别名	ZM 323881 (hydrochloride); ZM323881 hydrochloride
运输	蓝冰

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, 2-8°C

溶解方案

细胞实验：

DMSO: 50 mg/mL(121.4 mM)，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：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用；以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

方案二

方案三

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ZM323881 HCl 动物实验

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最近浏览的产品

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总药量计算器

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