Sunitinib | SU 11248 | 苏尼替尼 | VEGFR | PDGFR | c-Kit

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舒尼替尼 /Sunitinib 98%

货号：A157426 同义名： 苏尼替尼 / SU 11248 产品仅供科研

Sunitinib is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit.

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Type	HazMat fee for 500 gram (Estimated)
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Limited Quantity	USD 15-60
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Sunitinib 化学结构
CAS号：557795-19-4

Sunitinib 3D分子结构
CAS号：557795-19-4

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Sunitinib 纯度/质量文件

货号：A157426 标准纯度：98% 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 >

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		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 (wt), IC50: 79 nM c-Kit (D816V), IC50: 37 nM	Src	98%
Dasatinib	++ c-Kit (wt), IC50: 79 nM c-Kit (D816V), IC50: 37 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				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。

Sunitinib 生物活性

靶点	c-Kit c-Kit VEGFR2 VEGFR2, IC50:80 nM VEGFR2 VEGFR2 , IC50:80 nM
描述	VEGFR (vascular endothelial growth factor) and PDGFR (platelet-derived growth factor receptor) are critical roles in tumor growth and suvival via autocrine and paracrine loops, making them the well validated targets for the treatment of cancers. Sunitinib is a multiple RTKs inhibitor with IC50 values of 2nM and 80nM for VEGFR2 and PDGFRβ (measured by kinase activity)^[1], respectively, also shows inhibition against KIT and FLT3 receptor^[2]. The cellular kinase activity induced by VEGF/PDGF can be inhibited by Sunitinib with IC50 value of 5-50nM/10nM in 3T3 cells, while the PDGF-induced cell growth can be inhibited by Sunitinib with IC50 of 8nM^[1]. Daily oral administration of Sunitinib at dose of 80mg/kg reduced growth of established SF763T tumor xenografts in athymic mice, as well as suppressed Colo205 tumor growth. Consistent with the cellular kinase study, the inhibition by Sunitinib against p-PDGFRβ can be observed in tumor after a single dose at 80mg/kg in mice bearing SF767T tumors and mice bearing Colo205 tumors, as well as suppressed p-FLK1 in A375 xenograft mice dosed 40mg/kg Sunitinib^[2].
作用机制	Sunitinib is an ATP-competitive multitargeted tyrosine kinase inhibitor.^[3]

Sunitinib 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
3T3 cells		Function assay		Inhibition of PDGF-induced BrdU incorporation in 3T3 cells with 0.1% bovine serum albumin, IC50=7 nM	12646019
3T3 cells		Function assay		Inhibition of Vascular endothelial growth factor receptor in 3T3 cells, IC50=50 nM	12646019
HEK293 cells		Function assay		Binding affinity to FLT3 catalytic domain expressed in HEK293 cells by competitive binding assay, Kd=0.47 nM	19754199
human 697 cell		Growth inhibition assay		Inhibition of human 697 cell growth in a cell viability assay, IC50=0.61425 μM	SANGER

Sunitinib 动物研究

Dose	Rat: 0.5 mg/kg^[5] (p.o.), 1 mg/kg - 10 mg/kg^[6] (p.o.) Mice: 40 mg/kg^[7] (p.o.)
Administration	p.o.

Sunitinib 参考文献

[1]Sun L, Liang C, et al. Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl] -2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosine kinase. J Med Chem. 2003 Mar 27;46(7):1116-9.

[2]Mendel DB, Laird AD, et al. In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship. Clin Cancer Res. 2003 Jan;9(1):327-37.

[3]Shukla S, Robey RW, et al. Sunitinib (Sutent, SU11248), a small-molecule receptor tyrosine kinase inhibitor, blocks function of the ATP-binding cassette (ABC) transporters P-glycoprotein (ABCB1) and ABCG2. Drug Metab Dispos. 2009 Feb;37(2):359-65.

[4]Zhou Q, Gallo JM. Differential effect of sunitinib on the distribution of temozolomide in an orthotopic glioma model. Neuro Oncol. 2009;11(3):301-10.

Sunitinib 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.51mL

0.50mL

0.25mL

12.55mL

2.51mL

1.25mL

25.10mL

5.02mL

2.51mL

Sunitinib 技术信息

CAS号	557795-19-4
分子式	C₂₂H₂₇FN₄O₂
分子量	398.474

别名	苏尼替尼 ;SU 11248
运输	蓝冰

存储条件

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 20 mg/mL(50.19 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

动物实验配方

IP 2% DMSO+water 0.2 mg/mL clear

PO 0.5% CMC-Na 34 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

3T3 cells	Function assay		Inhibition of PDGF-induced BrdU incorporation in 3T3 cells with 0.1% bovine serum albumin, IC50=7 nM	12646019
3T3 cells	Function assay		Inhibition of Vascular endothelial growth factor receptor in 3T3 cells, IC50=50 nM	12646019
HEK293 cells	Function assay		Binding affinity to FLT3 catalytic domain expressed in HEK293 cells by competitive binding assay, Kd=0.47 nM	19754199
human 697 cell	Growth inhibition assay		Inhibition of human 697 cell growth in a cell viability assay, IC50=0.61425 μM	SANGER
human A3-KAW cell	Growth inhibition assay		Inhibition of human A3-KAW cell growth in a cell viability assay, ic50=1.62546 μM	SANGER
human A431 cells	Function assay	60 mins	Inhibition of EGFR in human A431 cells compound pretreated for 60 min before EGF stimulation for 10 mins by phosphotyrosine ELISA cytoblot method, IC50=172.1 nM	25882519
human A4-Fuk cell	Growth inhibition assay		Inhibition of human A4-Fuk cell growth in a cell viability assay， IC50=1.34141 μM	SANGER
human A549 cells	Cytotoxic assay	72 h	Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=2.44 μM	23602441
human ALL-PO cell	Growth inhibition assay		Inhibition of human ALL-PO cell growth in a cell viability assay, IC50=79.89 nM	SANGER
human BL-70 cell	Growth inhibition assay		Inhibition of human BL-70 cell growth in a cell viability assay, IC50=1.11846 μM	SANGER
human CAKI-1 cells	Proliferation assay		Antiproliferative activity against human CAKI-1 cells after 48 hrs by SRB assay, GI50=0.63 μM	22560627
human CGTH-W-1 cell	Growth inhibition assay		Inhibition of human CGTH-W-1 cell growth in a cell viability assay, IC50=30.94 nM	SANGER
human CMK cell	Growth inhibition assay		Inhibition of human CMK cell growth in a cell viability assay, IC50=1.95517 μM	SANGER
human CTV-1 cell	Growth inhibition assay		Inhibition of human CTV-1 cell growth in a cell viability assay, IC50=1.72751 μM	SANGER
human EoL-1-cell cell	Growth inhibition assay		Inhibition of human EoL-1-cell cell growth in a cell viability assay, IC50=1.64e-06	SANGER
human ES6 cell	Growth inhibition assay		Inhibition of human ES6 cell growth in a cell viability assay, IC50=0.98106 μM	SANGER
human ETK-1 cell	Growth inhibition assay		Inhibition of human ETK-1 cell growth in a cell viability assay, IC50=1.2858 μM	SANGER
human GB-1 cell	Growth inhibition assay		Inhibition of human GB-1 cell growth in a cell viability assay, IC50=0.71023 μM	SANGER
human HAEC cells	Proliferation assay	72 h	Antiproliferative activity against human HAEC cells expressing VEGFR after 72 hrs by MTT assay, IC50=0.1 μM	22444679
human HL60 cells	Cytotoxic assay	48 h	Cytotoxicity against human HL60 cells assessed as cell viability after 48 hrs by MTT assay, IC50=36.8 nM	25089810
human HT-29 cells	Proliferation assay	72 h	Antiproliferative activity against human HT-29 cells expressing VEGFR after 72 hrs by MTT assay， IC50=0.33 μM	22444679
human Kasumi-1 cells	Function assay		Inhibition of c-Kit autophosphorylation in human Kasumi-1 cells by Western blot analysis, IC50=15 nM	20833039
human KM12 cell	Growth inhibition assay		Inhibition of human KM12 cell growth in a cell viability assay, IC50=0.35014 μM	SANGER
human KS-1 cell	Growth inhibition assay		Inhibition of human KS-1 cell growth in a cell viability assay, IC50=1.69247 μM	SANGER
human LB1047-RCC cell	Growth inhibition assay		Inhibition of human LB1047-RCC cell growth in a cell viability assay, IC50=1.81624 μM	SANGER
human LC-2-ad cell	Growth inhibition assay		Inhibition of human LC-2-ad cell growth in a cell viability assay, IC50=1.11407 μM	SANGER
human MCF7 cells	Proliferation assay	48 h	Antiproliferative activity against human MCF7 cells after 48 hrs by SRB assay, GI50=2 μM	22560627
human MDA-MB-435 cells	Cytotoxic assay	2 h	Cytotoxicity against human MDA-MB-435 cells, IC50=9.7 nM	24890652
human MDA-MB-435 cells	Proliferation assay	48 h	Antiproliferative activity against human MDA-MB-435 cells after 48 hrs by SRB assay, GI=2 μM	22560627
human MEG-01 cell	Growth inhibition assay		Inhibition of human MEG-01 cell growth in a cell viability assay, IC50=1.83563 μM	SANGER
human MOLM13 cells	Cytotoxic assay		Cytotoxicity against human MOLM13 cells assessed as cell viability after 48 hrs by MTT assay, IC50=17.7 nM	25089810
human MOLT-16 cell	Growth inhibition assay		Inhibition of human MOLT-16 cell growth in a cell viability assay, IC50=0.63132 μM	SANGER
human MONO-MAC-6 cell	Growth inhibition assay		Inhibition of human MONO-MAC-6 cell growth in a cell viability assay, IC50=33.8 nM	SANGER
human MV-4-11 cell	Growth inhibition assay		Inhibition of human MV-4-11 cell growth in a cell viability assay, IC50=0.272 nM	SANGER
human MV411 cells	Proliferation assay	48 h	Antiproliferative activity against human MV411 cells after 48 hrs by MTT assay, ic50=3 nM	24904961
human NB1 cell	Growth inhibition assay		Inhibition of human NB1 cell growth in a cell viability assay, IC50=1.96117 μM	SANGER
human NCI-H3122 cells	Proliferation assay	72 h	Antiproliferative activity against human NCI-H3122 cells after 72 hrs by MTT assay, IC50=0.83 μM	24904961
human NCI-H526 cells	Proliferation assay	72 h	Antiproliferative activity against human NCI-H526 cells after 72 hrs by MTT assay, IC50=1.01 μM	24904961
human NKM-1 cell	Growth inhibition assay		Inhibition of human NKM-1 cell growth in a cell viability assay, IC50=98.52 nM	SANGER
human NOS-1 cell	Growth inhibition assay		Inhibition of human NOS-1 cell growth in a cell viability assay, IC50=15.3 nM	SANGER
human RS4-11 cells	Function assay		Inhibition of FLT3 autophosphorylation in human RS4-11 cells after 2 hrs by electrochemiluminescence assay, IC50=9.9 nM	19654408
human RS4-11 cells	Function assay		Inhibition of FLT3 autophosphorylation in human RS4-11 cells by Western blot analysis, IC50=16 nM	20833039
human SH-SY5Y cells	Function assay		Inhibition of PDGFRbeta in human SH-SY5Y cells by phosphotyrosine ELISA assay, IC50=83.1 nM	24890652
human SR cell	Growth inhibition assay		Inhibition of human SR cell growth in a cell viability assay, IC50=1.54572 μM	SANGER
human SW620 cells	Proliferation assay	48 h	Antiproliferative activity against human SW620 cells after 48 hrs by SRB assay, GI50=1.3 μM	22560627
human SW756 cell	Growth inhibition assay		Inhibition of human SW756 cell growth in a cell viability assay, IC50=19.1351 μM	SANGER
human TE-11 cell	Growth inhibition assay		Inhibition of human TE-11 cell growth in a cell viability assay, IC50=1.83985 μM	SANGER
human TE-12 cell	Growth inhibition assay		Inhibition of human TE-12 cell growth in a cell viability assay, IC50=0.80455 μM	SANGER
human TE-15 cell	Growth inhibition assay		Inhibition of human TE-15 cell growth in a cell viability assay, IC50=0.50761 μM	SANGER
human THP1 cells	Cytotoxic assay	48 h	Cytotoxicity against human THP1 cells assessed as cell viability after 48 hrs by MTT assay, IC50=45.7 nM	25089810
human TT cells	Proliferation assay	72 h	Antiproliferative activity against human TT cells pretreated for 72 hrs followed by compound-washout measured after 72 hrs by MTT assay, IC50=40 nM	24904961
human U251 cells	Function assay		Inhibition of VEGFR2 in human U251 cells by phosphotyrosine ELISA, IC50=18.9 nM	24900865
human U251 cells	Function assay	60 mins	Inhibition of PDGFR-beta in human U251 cells compound pretreated for 60 min before PDGF-BB stimulation for 10 mins by phosphotyrosine ELISA cytoblot method, IC50=83.1 nM	25882519
HUVEC	Cytotoxic assay		Cytotoxicity against HUVEC, IC50=11.8 nM	24890652
HUVEC cell	Function assay	24 h	Inhibition of VEGF-A induced HUVEC cell sprouting after 24 hrs by angiogenesis assay, IC50=0.12 μM	21741249
IM9 cells	Cytotoxic assay		Cytotoxicity against Homo sapiens (human) IM9 cells assessed as growth inhibition by MTT assay, IC50=1.35 μM	SANGER
MCF7 cells	Cytotoxic assay		Cytotoxicity against human ER-positive MCF7 cells, IC50=27.1 nM	24890652
MDA-MB-231 cells	Cytotoxic assay		Cytotoxicity against human triple negative MDA-MB-231 cells, IC50=22.3 nM	24890652
mouse triple negative 4T1 cells	Cytotoxic assay		Cytotoxicity against mouse triple negative 4T1 cells, IC50=16 nM	24890652
NIH3T3 cells	Function assay	1 h	Inhibitory concentration against human KDR kinase expressed in NIH3T3 cells with 4 uM Biotin-Ahx-AEEEYFFLFA-amide at ambient temperature for 1 hr	16162008
Sf9 cells	Function assay		Inhibition of GST-tagged VEGFR expressed in Sf9 cells, IC50=0.185 μM	19854051

舒尼替尼 /Sunitinib 98%

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c-Kit
c-Kit
VEGFR2	VEGFR2, IC50:80 nM
VEGFR2	VEGFR2 , IC50:80 nM
VEGFR2	VEGFR2, IC50:80 nM
VEGFR2	VEGFR2 , IC50:80 nM
PDGFRβ	PDGFRβ, IC50:2 nM
PDGFRβ	PDGFRβ , IC50:2 nM
PDGFRβ	PDGFRβ, IC50:2 nM
PDGFRβ	PDGFRβ , IC50:2 nM

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