KRN-633 | VEGFR Inhibitor | AmBeed-信号通路专用抑制剂

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KRN-633 99%+

货号：A263491 产品仅供科研

KRN-633 can inhibit VEGFR1, VEGFR2 and VEGFR3 with IC50 of 170 nM, 160 nM, and 125 nM, respectively.

KRN-633 化学结构
CAS号：286370-15-8

KRN-633 3D分子结构
CAS号：286370-15-8

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KRN-633 纯度/质量文件

货号：A263491 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: • Mar. Drugs, 2024, 22(5): 194. Ambeed. [ A104599 ]; • Pharmaceuticals, 2024, 17(5): 570. Ambeed. [ A224421 ]; 更多 >

PDGFR 亚型比较
VEGFR 亚型比较

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	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		99%+
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, IC50: 3 nM VEGFR2/Flk1, IC50: 3 nM	+++ VEGFR3, IC50: 6 nM	PDGFR,RET	99%+
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	PDGFR,c-Kit,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	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	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		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, 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			99%+
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。

KRN-633 生物活性

靶点

VEGFR1

VEGFR1, IC50:170 nM
VEGFR1

VEGFR1, IC50:170 nM
VEGFR3

VEGFR3, IC50:125 nM
VEGFR3

VEGFR3, IC50:125 nM

描述

The vascular endothelial growth factor (VEGF)-VEGF receptor (R) system is deeply involved in angiogenesis and lymphangiogenesis^[3]. KRN-633 inhibits tyrosine phosphorylation of VEGFR-1, VEGFR2, c-Kit, and PDGFR-β (IC50=11.7, 1.16, 8.01, 130 nM) in human umbilical vein endothelial cells. KRN-633 also inhibits the VEGF-driven proliferation of HUVECs (IC50=14.9 nM). KRN-633 suppresses capillary tube formation of endothelial cells. KRN-633 inhibits tumor growth in several tumor xenograft models with diverse tissue origins, including lung, colon, and prostate, in athymic mice and rats. KRN-633 also causes the regression of some well-established tumors and those that have regrown after the cessation of treatment. KRN-633 is well tolerated and has no significant effects on body weight or the general health of the animals. Histologic analysis of tumor xenografts treated with KRN-633 reveals a reduction in the number of endothelial cells in non-necrotic areas and a decrease in vascular permeability^[4]. Reduction in the expression levels of VEGF and VEGF receptor-2 in the CL precedes the impairment of luteal circulation and a series of events leading to parturition (i.e., reduction of plasma progesterone, enhancement of myometrium contractility, and onset of parturition). Blocking of VEGF signaling by using the inhibitor of VEGFR tyrosine kinase KRN633 at mid-pregnancy caused a similar sequence of events and induced preterm birth^[5]. In retinas of rats injected subcutaneously with KRN633 (10 mg/kg), simplified vasculature attributable to capillary regression and prevention of endothelial cell growth were seen, whereas no visible changes in the morphology of the retinal layers were observed^[6].

KRN-633 参考文献

[1]Ban HS, Uno M, Nakamura H. Suppression of hypoxia-induced HIF-1alpha accumulation by VEGFR inhibitors: Different profiles of AAL993 versus SU5416 and KRN633. Cancer Lett. 2010 Oct 1;296(1):17-26.

[2]Nakamura K, Yamamoto A, et al. KRN633: A selective inhibitor of vascular endothelial growth factor receptor-2 tyrosine kinase that suppresses tumor angiogenesis and growth. Mol Cancer Ther. 2004 Dec;3(12):1639-49.

[3]Masabumi Shibuya. VEGF-VEGFR System as a Target for Suppressing Inflammation and other Diseases. Endocr Metab Immune Disord Drug Targets. 2015;15(2):135-44.

[4]Nakamura K, et al. KRN633: A selective inhibitor of vascular endothelial growth factor receptor-2 tyrosine kinase that suppresses tumor angiogenesis and growth. Mol Cancer Ther. 2004 Dec;3(12):1639-49.

[5]Yoshiko Wada,et al. Role of vascular endothelial growth factor in maintenance of pregnancy in mice. Endocrinology. 2013 Feb;154(2):900-10.

[6]Daiki Asano,et al. Regression of retinal capillaries following N-methyl-D-aspartate-induced neurotoxicity in the neonatal rat retina. J Neurosci Res. 2015 Feb;93(2):380-90.

KRN-633 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.40mL

0.48mL

0.24mL

11.99mL

2.40mL

1.20mL

23.99mL

4.80mL

2.40mL

KRN-633 技术信息

CAS号	286370-15-8
分子式	C₂₀H₂₁ClN₄O₄
分子量	416.86

别名
运输	蓝冰

存储条件

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 25 mg/mL(59.97 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

0.5% methylcellulose+0.2% Tween 80+water 10 mg/mL suspension

KRN-633 99%+

KRN-633 纯度/质量文件

全球学术期刊中引用的产品

KRN-633 生物活性

KRN-633 参考文献

KRN-633 实验方案

KRN-633 技术信息

最近浏览的产品

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靶点

总药量计算器

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VEGFR1	VEGFR1, IC50:170 nM
VEGFR1	VEGFR1, IC50:170 nM
VEGFR3	VEGFR3, IC50:125 nM
VEGFR3	VEGFR3, IC50:125 nM
VEGFR2	VEGFR2, IC50:160 nM
VEGFR2	VEGFR2, IC50:160 nM

KRN-633 99%+

KRN-633 纯度/质量文件

全球学术期刊中引用的产品

KRN-633 生物活性

KRN-633 参考文献

KRN-633 实验方案

KRN-633 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

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