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

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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 (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				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	c-Kit,FLT3	85%
Linifanib			++ PDGFRβ, IC50: 66 nM		99%+
AZD2932			+++ PDGFRβ, IC50: 4 nM	c-Kit	99%
Dovitinib			+++ PDGFRβ, IC50: 27 nM	c-Kit,FLT3	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	PDGFR,RET	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	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/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	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	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	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。

Cell Line Mouse retinal ganglion cells CD8+ T cells HMLER-FOXC2 cells HMLER-Snail cells Human umbilical vein endothelial cells (HUVECs) 786-0 cells 786-0shRNA and 786-0shEZH2 cells 786-O cells ACHN cells	Concentration	Treated Time	Description	References
Mouse retinal ganglion cells	1 µM	72 hours	To evaluate the effect of Pamoic acid on the survival of mouse retinal ganglion cells, results showed that Pamoic acid had no detrimental effect on cell survival at concentrations as high as 10 mg/mL.	Pharmaceutics. 2021 May 1;13(5):647
CD8+ T cells	2.5 μM	overnight	Sunitinib inhibits Stat3 activity in CD8+ T cells	Cancer Res. 2010 Dec 1;70(23):9599-610.
HMLER-FOXC2 cells	10 µM	7 days	To test the effect of Sunitinib on mammosphere formation in HMLER-FOXC2 cells, results showed that Sunitinib significantly reduced mammosphere formation.	Cancer Res. 2013 Mar 15;73(6):1981-92.
HMLER-Snail cells	10 µM	7 days	To test the effect of Sunitinib on mammosphere formation in HMLER-Snail cells, results showed that Sunitinib significantly reduced mammosphere formation.	Cancer Res. 2013 Mar 15;73(6):1981-92.
Human umbilical vein endothelial cells (HUVECs)	1 nM	9 days	To evaluate the effect of Sunitinib on IL-36 or VEGF-A stimulated HUVECs angiogenesis, results showed that Sunitinib significantly inhibited IL-36 and VEGF-A induced angiogenesis	Front Immunol. 2018 Feb 26;9:200.
786-0 cells	2μM to 5μM		Establishment of sunitinib-resistant cell line 786-0R and evaluation of its resistance to sunitinib.	Mol Cancer Ther. 2015 Feb;14(2):513-22.
786-0shRNA and 786-0shEZH2 cells	2μM, 4μM, 6μM, 8μM	48 h	Evaluation of the effect of EZH2 knockdown on sunitinib sensitivity, results showed increased sensitivity to sunitinib after EZH2 knockdown.	Mol Cancer Ther. 2015 Feb;14(2):513-22.
786-O cells	100 μM	24 h	To validate the impact of AA on Sunitinib's inhibition of ccRCC cell proliferation and invasion, results showed that AA enhanced the inhibitory effect of Sunitinib.	Nat Commun. 2023 Jul 17;14(1):4274.
ACHN cells	100 μM	24 h	To validate the impact of AA on Sunitinib's inhibition of ccRCC cell proliferation and invasion, results showed that AA enhanced the inhibitory effect of Sunitinib.	Nat Commun. 2023 Jul 17;14(1):4274.

Species Rat C.B17/Icr-scid mice Mice NOD/SCID mice Mice Mice	Animal Model Optic nerve injury model PNX0010 xenograft tumour model Renca renal cell carcinoma model HMLER-FOXC2 tumor model Nude mice RP-R-01 and RP-R-02 patient-derived ccRCC xenograft models	Administration	Dosage	Frequency	Description	References
Rat	Optic nerve injury model	Subconjunctival injection	200 μg	Single injection, sustained for 20 weeks	To evaluate the neuroprotective effect of SPC microcrystals on retinal ganglion cells, results showed that a single subconjunctival injection of SPC microcrystals provided sustained retina drug levels for 20 weeks and neuroprotection in a rat model of optic nerve injury.	Pharmaceutics. 2021 May 1;13(5):647
C.B17/Icr-scid mice	PNX0010 xenograft tumour model	Oral	40 mg/kg	5 days per week	To examine the effect of a high-fat/high-cholesterol diet on the antitumour efficacy of Sunitinib, and found that the high-fat/high-cholesterol diet diminished the antitumour effect of Sunitinib	Br J Cancer. 2017 Apr 25;116(9):1203-1207
Mice	Renca renal cell carcinoma model	Oral	30-40 mg/kg	Once daily for up to 14 days	Sunitinib combined with CD8+ T cell adoptive transfer significantly inhibited tumor growth and inhibited Stat3 activity	Cancer Res. 2010 Dec 1;70(23):9599-610.
NOD/SCID mice	HMLER-FOXC2 tumor model	Oral	40 mg/kg	5 days a week for 30 days	To evaluate the effect of Sunitinib on HMLER-FOXC2 tumor growth and animal survival, results showed that Sunitinib significantly reduced tumor growth and extended event-free survival.	Cancer Res. 2013 Mar 15;73(6):1981-92.
Mice	Nude mice	Gavage feeding	40 mg/kg/mouse	Five times a week	Establishment of sunitinib-resistant renal cell carcinoma cell lines	Cancer Sci. 2020 May;111(5):1607-1618
Mice	RP-R-01 and RP-R-02 patient-derived ccRCC xenograft models	Oral gavage	40 mg/kg	5 days/week, until tumor resistance	Evaluation of the effect of sunitinib dose escalation on overcoming resistance in ccRCC xenograft models, results showed that dose escalation restored tumor sensitivity to sunitinib.	Mol Cancer Ther. 2015 Feb;14(2):513-22.

细胞研究

细胞系	浓度	检测类型	检测时间	活性说明	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

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

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.

CAS号	557795-19-4
分子式	C₂₂H₂₇FN₄O₂
分子量	398.47
SMILES Code	CCN(CCNC(C(C(C)=C1/C([H])=C(C2=O)/C3=C(N2)C=CC(F)=C3)=C(N1)C)=O)CC
MDL No.	MFCD09260778

别名	苏尼替尼 ;SU 11248
运输	蓝冰
InChI Key	WINHZLLDWRZWRT-ATVHPVEESA-N
Pubchem ID	5329102

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

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