Ki8751 | VEGFR Inhibitor | AmBeed-信号通路专用抑制剂

Ki8751 {[allProObj[0].p_purity_real_show]}

货号：A187238

Ki8751是一种选择性 VEGFR2 抑制剂，IC50 为 0.9 nM。

Ki8751 化学结构
CAS号：228559-41-9

Ki8751 3D分子结构
CAS号：228559-41-9

规格	价格	会员价	库存	数量
{[ item.pr_size ]}	{[ getRatePriceInt(item.pr_rmb, 1,1) ]} {[ getRatePriceInt(item.pr_rmb_sale, 1,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]}	{[ getRatePriceInt(item.pr_rmb, 1,1) ]} {[ getRatePriceInt(item.pr_rmb,item.pr_rate,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]}	{[ getRatePriceInt(item.pr_rmb, 1,1) ]}{[ suihuo_tips(item.pr_tag_price, item.pr_am) ]}	{[ getRatePrice(item.pr_rmb_sale, 1,1,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate,item.mem_isinteger) ]}	现货	1周咨询	- +

购物车0 收藏询单

sales@ambeed.cn tech@ambeed.cn 400-920-2911 产品手册产品订购技术咨询
快速发货顺丰冷链运输，1-2 天到达

品质保证

技术支持

免费溶解

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		97%
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		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				97%
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			VEGFR,mTOR	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			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	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			++ 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	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	c-Kit,PDGFR,FGFR	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/CSF1R	99%+
Axitinib	++++ VEGFR1/FLT1, IC50: 0.1 nM	++++ VEGFR2/Flk1, IC50: 0.18 nM VEGFR2/KDR, IC50: 0.2 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	+++ 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			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/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	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。

Ki8751 生物活性

靶点

VEGFR2

VEGFR2, IC50:0.9 nM
PDGFRα

PDGFRα, IC50:67 nM
c-Kit

c-Kit, IC50:40 nM

描述

Ki8751 is a potent and selective inhibitor of VEGFR2 with IC50 of 0.9 nM, which is > 40-fold selective for VEGFR2 than c-Kit, PDGFRα and FGFR-2, little activity to EGFR, HGFR and InsR.

Ki8751 细胞实验

Cell Line HIMECs HeLa S3 cells U87 cells MCF-7 MDA-MB-231 HeLa S3 cells U38 cells	Concentration	Treated Time	Description	References
HIMECs	4.7 μg/mL	30 minutes	Ki8751 inhibited IL-17C CM-induced HIMEC migration.	Cells. 2020 Jun 1;9(6):1363.
HeLa S3 cells	10 µM	2 days	Ki8751 suppressed cell proliferation and caused nuclear shape changes, including binuclei and micronuclei.	Int J Mol Sci. 2018 Dec 12;19(12):4014.
U87 cells	2.5 µM	24 hours	Ki8751 treatment increased the expression of mitochondrial-related proteins in U87 cells, indicating that VEGFR2 inhibition suppresses glioblastoma cell proliferation by enhancing mitochondrial biogenesis.	J Transl Med. 2024 May 3;22(1):419.
MCF-7	2.5 µM and 5 µM	24, 48, and 72 hours	Ki8751 significantly reduced cancer cell proliferation and enhanced breast cancer cell apoptosis.	Cancer Biol Med. 2021 Feb 15;18(1):139-154.
MDA-MB-231	2.5 µM and 5 µM	24, 48, and 72 hours	Ki8751 significantly reduced cancer cell proliferation and enhanced breast cancer cell apoptosis.	Cancer Biol Med. 2021 Feb 15;18(1):139-154.
HeLa S3 cells	1 µM	3 hours	Ki8751 delayed M phase progression, causing misalignment of chromosomes and rotation of the mitotic spindle.	Int J Mol Sci. 2018 Dec 12;19(12):4014.
U38 cells	2.5 µM	48 hours	Ki8751 treatment increased the expression of mitochondrial-related proteins in U38 cells, indicating that VEGFR2 inhibition suppresses glioblastoma cell proliferation by enhancing mitochondrial biogenesis.	J Transl Med. 2024 May 3;22(1):419.

Cell Line

HIMECs HeLa S3 cells U87 cells MCF-7 MDA-MB-231 HeLa S3 cells U38 cells

Concentration

Treated Time

Description

References

HIMECs

4.7 μg/mL

30 minutes

Ki8751 inhibited IL-17C CM-induced HIMEC migration.

Cells. 2020 Jun 1;9(6):1363.

HeLa S3 cells

10 µM

2 days

Ki8751 suppressed cell proliferation and caused nuclear shape changes, including binuclei and micronuclei.

Int J Mol Sci. 2018 Dec 12;19(12):4014.

U87 cells

2.5 µM

24 hours

Ki8751 treatment increased the expression of mitochondrial-related proteins in U87 cells, indicating that VEGFR2 inhibition suppresses glioblastoma cell proliferation by enhancing mitochondrial biogenesis.

J Transl Med. 2024 May 3;22(1):419.

MCF-7

2.5 µM and 5 µM

24, 48, and 72 hours

Ki8751 significantly reduced cancer cell proliferation and enhanced breast cancer cell apoptosis.

Cancer Biol Med. 2021 Feb 15;18(1):139-154.

MDA-MB-231

2.5 µM and 5 µM

24, 48, and 72 hours

Ki8751 significantly reduced cancer cell proliferation and enhanced breast cancer cell apoptosis.

Cancer Biol Med. 2021 Feb 15;18(1):139-154.

HeLa S3 cells

1 µM

3 hours

Ki8751 delayed M phase progression, causing misalignment of chromosomes and rotation of the mitotic spindle.

Int J Mol Sci. 2018 Dec 12;19(12):4014.

U38 cells

2.5 µM

48 hours

Ki8751 treatment increased the expression of mitochondrial-related proteins in U38 cells, indicating that VEGFR2 inhibition suppresses glioblastoma cell proliferation by enhancing mitochondrial biogenesis.

J Transl Med. 2024 May 3;22(1):419.

Ki8751 动物实验

Species Rats Mice Mice	Animal Model Middle cerebral artery occlusion-induced cerebral ischemia-reperfusion injury model C57BL/6 mice DLD-1 cell xenograft model	Administration	Dosage	Frequency	Description	References
Rats	Middle cerebral artery occlusion-induced cerebral ischemia-reperfusion injury model	Tail vein injection	0.5 mg/kg	Single dose 30 minutes prior to surgery	Ki8751 reversed the angiogenesis and protective effects induced by TQHXD through inhibition of VEGFR2 activity, decreasing both p-FAK and p-Paxillin protein levels.	Front Pharmacol. 2021 Jan 11;11:572624
Mice	C57BL/6 mice	Perfusion	1 nM	Single administration	Ki8751 significantly decreased outflow facility, with an average reduction of 34% (CI: -56, -2%; P=0.04, n=6).	Invest Ophthalmol Vis Sci. 2017 Mar 1;58(3):1899-1908
Mice	DLD-1 cell xenograft model	Subcutaneous injection	10 μg/tumor	Daily for 10 days	Ki8751 suppressed IL-17C-induced tumor growth and angiogenesis.	Cells. 2020 Jun 1;9(6):1363.

Species

Rats Mice Mice

Animal Model

Middle cerebral artery occlusion-induced cerebral ischemia-reperfusion injury model C57BL/6 mice DLD-1 cell xenograft model

Administration

Dosage

Frequency

Description

References

Rats

Middle cerebral artery occlusion-induced cerebral ischemia-reperfusion injury model

Tail vein injection

0.5 mg/kg

Single dose 30 minutes prior to surgery

Ki8751 reversed the angiogenesis and protective effects induced by TQHXD through inhibition of VEGFR2 activity, decreasing both p-FAK and p-Paxillin protein levels.

Front Pharmacol. 2021 Jan 11;11:572624

Mice

C57BL/6 mice

Perfusion

1 nM

Single administration

Ki8751 significantly decreased outflow facility, with an average reduction of 34% (CI: -56, -2%; P=0.04, n=6).

Invest Ophthalmol Vis Sci. 2017 Mar 1;58(3):1899-1908

Mice

DLD-1 cell xenograft model

Subcutaneous injection

10 μg/tumor

Daily for 10 days

Ki8751 suppressed IL-17C-induced tumor growth and angiogenesis.

Cells. 2020 Jun 1;9(6):1363.

Ki8751 参考文献

Ki8751 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.13mL

0.43mL

0.21mL

10.65mL

2.13mL

1.07mL

21.30mL

4.26mL

2.13mL

Ki8751 技术信息

CAS号	228559-41-9
分子式	C₂₄H₁₈F₃N₃O₄
分子量	469.41
SMILES Code	O=C(NC1=CC=C(OC2=CC=NC3=CC(OC)=C(OC)C=C23)C=C1F)NC4=CC=C(F)C=C4F
MDL No.	MFCD09971092

别名
运输	蓝冰
InChI Key	LFKQSJNCVRGFCC-UHFFFAOYSA-N
Pubchem ID	11317348

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, room temperature

溶解方案

细胞实验：

DMSO: 35 mg/mL(74.56 mM)，配合低频超声，并水浴加热至45℃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：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

Ki8751 {[allProObj[0].p_purity_real_show]}

Ki8751 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Ki8751 质控信息

Ki8751 生物活性

Ki8751 细胞实验

Ki8751 动物实验

Ki8751 参考文献

Ki8751 实验方案

Ki8751 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

靶点	VEGFR2 VEGFR2, IC50:0.9 nM PDGFRα PDGFRα, IC50:67 nM c-Kit c-Kit, IC50:40 nM
描述	Ki8751 is a potent and selective inhibitor of VEGFR2 with IC50 of 0.9 nM, which is > 40-fold selective for VEGFR2 than c-Kit, PDGFRα and FGFR-2, little activity to EGFR, HGFR and InsR.

VEGFR2	VEGFR2, IC50:0.9 nM
PDGFRα	PDGFRα, IC50:67 nM
c-Kit	c-Kit, IC50:40 nM

Ki8751 {[allProObj[0].p_purity_real_show]}

Ki8751 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Ki8751 质控信息

Ki8751 生物活性

Ki8751 细胞实验

Ki8751 动物实验

Ki8751 参考文献

Ki8751 实验方案

Ki8751 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

请登录您的专属账户

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

Ki8751 纯度/质量文件产品仅供科研