Brivanib | BMS-540215 | VEGFR2 Inhibitor | AmBeed-信号通路专用抑制剂

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产品名称	FGFR ↓ ↑	FGFR1 ↓ ↑	FGFR2 ↓ ↑	FGFR3 ↓ ↑	FGFR4 ↓ ↑	其他靶点	纯度
Tyrphostin AG1296	+ FGFR (Swiss 3T3), IC50: 12.3 μM					PDGFR	99%+
Pazopanib	+ FGFR, IC50: 140 nM						99%
Erdafitinib	✔					RET	99%+
Gambogenic acid	✔						98+%
Sulfatinib		+++ FGFR1, IC50: 15 nM					99+%
Nintedanib esylate		+ FGFR1, IC50: 69 nM	++ FGFR2, IC50: 37 nM	+ FGFR3, IC50: 108 nM			98%
Zoligratinib		+++ FGFR1, IC50: 9.3 nM	+++ FGFR2, IC50: 7.6 nM	++ FGFR3, IC50: 22 nM	+ FGFR4, IC50: 290 nM		99%+
MK-2461		+ FGFR1, IC50: 65 nM	++ FGFR2, IC50: 39 nM	++ FGFR3, IC50: 50 nM			98%+
SU 5402		++ FGFR1, IC50: 30 nM					98%
Brivanib		+ FGFR1, IC50: 148 nM					99%+
Lucitanib		++ FGFR1, IC50: 17.5 nM	+ FGFR2, IC50: 82.5 nM				99%+
Ponatinib		++++ FGFR1, IC50: 2.2 nM					98%
PD-166866		+ FGFR1, IC50: 52.4 nM					99%
Narazaciclib		++ FGFR1, IC50: 26 nM				RET	99%+
Lactate		+++ FGFR1, IC50: 8 nM		+++ FGFR3, IC50: 9 nM		FLT3,c-Kit	85%
Lenvatinib mesylate		++ FGFR1, IC50: 46 nM				c-RET	99%
LY2874455		++++ FGFR1, IC50: 2.8 nM	++++ FGFR2, IC50: 2.6 nM	+++ FGFR3, IC50: 6.4 nM	+++ FGFR4, IC50: 6 nM		99%+
FIIN-2		+++ FGFR1, IC50: 3.09 nM	+++ FGFR2, IC50: 4.3 nM	++ FGFR3, IC50: 27 nM	++ FGFR4, IC50: 45.3 nM		99%
FIIN-3		+++ FGFR1, IC50: 13.1 nM	++ FGFR2, IC50: 21 nM	++ FGFR3, IC50: 31.4 nM	++ FGFR4, IC50: 35.3 nM		98%
Infigratinib		++++ FGFR1, IC50: 0.9 nM	++++ FGFR2, IC50: 1.4 nM	++++ FGFR3, IC50: 1.0 nM FGFR3 (K650E), IC50: 4.9 nM	+ FGFR4, IC50: 60 nM		99%+
Danusertib		++ FGFR1, IC50: 47 nM				RET	99%+
R1530		++ FGFR1, IC50: 28 nM					98%
ENMD-2076		+ FGFR1, IC50: 92.7 nM	+ FGFR2, IC50: 70.8 nM			RET,FLT3	98%
Dovitinib		+++ FGFR1, IC50: 8 nM		+++ FGFR3, IC50: 9 nM		FLT3,c-Kit	99%+
Sorafenib		+ FGFR1, IC50: 580 nM					99%
SSR128129E		+ FGFR1, IC50: 1.9 μM					99%+
AZD-4547		++++ FGFR1, IC50: 0.2 nM	++++ FGFR2, IC50: 2.5 nM	++++ FGFR3, IC50: 1.8 nM			98%
Lenvatinib		++ FGFR1, IC50: 46 nM				RET	98%
PD173074		++ FGFR1, IC50: ~25 nM					99%+
S49076		++ FGFR1, IC50: 18 nM	+++ FGFR2, IC50: 17 nM	+++ FGFR3, IC50: 15 nM			98%
Futibatinib		++++ FGFR1, IC50: 1.8 nM	++++ FGFR2, IC50: 1.4 nM	++++ FGFR3, IC50: 1.6 nM	+++ FGFR4, IC50: 3.7 nM		99%+
Ferulic Acid		+ FGFR1, IC50: 3.78 μM	+ FGFR2, IC50: 12.5 μM				98%
Nintedanib		+ FGFR1, IC50: 69 nM	++ FGFR2, IC50: 37 nM	+ FGFR3, IC50: 108 nM	+ FGFR4, IC50: 610 nM		99+%
ASP5878		++++ FGFR1, IC50: 0.47 nM	++++ FGFR2, IC50: 0.6 nM	++++ FGFR3, IC50: 0.74 nM	+++ FGFR4, IC50: 3.5 nM		99%
PRN1371		++++ FGFR1, IC50: 0.6 nM	++++ FGFR2, IC50: 1.3 nM	+++ FGFR3, IC50: 4.1 nM	++ FGFR4, IC50: 19.3 nM		99%
Derazantinib		+++ FGFR1, IC50: 4.5 nM	++++ FGFR2, IC50: 1.8 nM	+++ FGFR3, IC50: 4.5 nM	++ FGFR4, IC50: 34 nM	RET	99%+
ODM-203		+++ FGFR1, IC50: 11 nM	+++ FGFR2, IC50: 16 nM	+++ FGFR3, IC50: 6 nM	++ FGFR4, IC50: 35 nM		99%+
Pemigatinib		++++ FGFR1, IC50: 0.4 nM	++++ FGFR2, IC50: 0.5 nM	++++ FGFR3, IC50: 1.2 nM	++ FGFR4, IC50: 30 nM		99%+
SKLB 610			✔			PDGFR	99%+
Alofanib			✔				99%+
Lirafugratinib			✔				99%
Masitinib mesylate				✔		FAK	99%+
BLU9931				+ FGFR3, IC50: 150 nM	+++ FGFR4, IC50: 3 nM		99%+
BO-264				✔			99%+
Fisogatinib					+++ FGFR4, IC50: 5 nM		99%+
H3B-6527					++++ FGFR4, IC50: <1.2 nM		99%+
Roblitinib					++++ FGFR4, IC50: 1.9 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	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。

Cell Line HepG2-SR cells HepG2 Huh7 Hep3B	Concentration	Treated Time	Description	References
HepG2-SR cells	2.5, 5 μM	48 hrs/72 hrs	Brivanib, as a positive control, reduced the viability of HepG2-SR cells and induced apoptosis.	J Ginseng Res. 2022 May;46(3):418-425.
HepG2	60 μM	72 h	To evaluate the effect of Notch3 silencing on Brivanib response, results showed that Notch3 silencing enhanced the apoptotic effect of Brivanib on HepG2 cells.	Br J Cancer. 2019 Mar;120(6):601-611.
Huh7	60 μM	72 h	To evaluate the effect of Notch3 silencing on Brivanib response, results showed that Notch3 silencing enhanced the apoptotic effect of Brivanib on Huh7 cells.	Br J Cancer. 2019 Mar;120(6):601-611.
Hep3B	60 μM	72 h	To evaluate the effect of Notch3 silencing on Brivanib response, results showed that Notch3 silencing did not significantly enhance the apoptotic effect of Brivanib on Hep3B cells.	Br J Cancer. 2019 Mar;120(6):601-611.

Species Mice Mice BALB/c- nu/nu mice Mice Rats	Animal Model MCF-7 E2 tumor model RIP1-Tag2 transgenic mice HepG2-SR hepatoma model Liver fibrosis models induced by bile duct ligation (BDL), chronic carbon tetrachloride (CCl4), and chronic thioacetamide (TAA) DENA-induced HCC model	Administration	Dosage	Frequency	Description	References
Mice	MCF-7 E2 tumor model	Oral	0.05 mg/g and 0.1 mg/g	Daily for 6 weeks	To evaluate the effect of Brivanib Alaninate on the growth of MCF-7 E2 tumors. Results showed that the high dose (0.1 mg/g) significantly inhibited tumor growth, while the low dose (0.05 mg/g) had no significant effect.	Eur J Cancer. 2010 Jun;46(9):1537-53
Mice	RIP1-Tag2 transgenic mice	Oral	75 mg/kg	Once daily for 5.5 weeks	To evaluate the therapeutic efficacy of Brivanib in the RIP1-Tag2 transgenic mouse model of pancreatic neuroendocrine tumors (PNET). Results showed that Brivanib treatment significantly extended the lifespan of the mice and maintained tumor stasis during the 5.5 weeks of therapy.	Clin Cancer Res. 2011 Aug 15;17(16):5299-310
BALB/c- nu/nu mice	HepG2-SR hepatoma model	Oral administration	100 mg/kg	Once daily for 15 consecutive days	Brivanib, as a positive control, significantly inhibited HepG2-SR tumor growth.	J Ginseng Res. 2022 May;46(3):418-425.
Mice	Liver fibrosis models induced by bile duct ligation (BDL), chronic carbon tetrachloride (CCl4), and chronic thioacetamide (TAA)	Oral	25 mg/kg, 50 mg/kg, 100 mg/kg	Administered for 5 consecutive days with 2 days off on weekends, lasting for 4 weeks	To evaluate the effect of brivanib on liver fibrosis, results showed that brivanib significantly reduced liver fibrosis and decreased the expression of collagen Iα1 and α-smooth muscle actin in the liver.	PLoS One. 2014 Apr 7;9(4):e92273
Rats	DENA-induced HCC model	Oral gavage	60 mg/kg	Once daily for 15 days	To evaluate the effect of Brivanib combined with Notch3 silencing on the HCC model, results showed that Notch3 silencing significantly enhanced the inhibitory effect of Brivanib on tumor growth.	Br J Cancer. 2019 Mar;120(6):601-611.

临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT00594984	Metastatic Colorectal Cancer (... 展开 >>MCRC) 收起 <<	Phase 1 Phase 2	Completed	-	United States, California ... 展开 >> Usc/Norris Comprehensive Cancer Center Hospital Los Angeles, California, United States, 90033 Usc/Norris Comprehensive Cancer Center Los Angeles, California, United States, 90033 United States, Kentucky James Graham Brown Cancer Center Louisville, Kentucky, United States, 40202 United States, Missouri Washington University Saint Louis, Missouri, United States, 63110 Argentina Local Institution Buenos Aires, Argentina, C1426ANZ Denmark Local Institution Odense C, Denmark, 5000 Italy Local Institution Meldola Fc, Italy, 47014 Local Institution Milano, Italy, 20141 Korea, Republic of Local Institution Seoul, Korea, Republic of, 135-710 Spain Local Institution Madrid, Spain, 28050 Sweden Local Institution Stockholm, Sweden, 17176 Local Institution Uppsala, Sweden, 75185 收起 <<
NCT00300027	Gastrointestinal Neoplasms	Phase 1	Terminated	-	United States, Arkansas ... 展开 >> Local Institution Little Rock, Arkansas, United States United States, California Local Institution Los Angeles, California, United States United States, District of Columbia Local Institution Washington, District of Columbia, United States United States, Iowa Local Institution Iowa City, Iowa, United States United States, North Carolina Local Institution Durham, North Carolina, United States United States, Texas Local Institution Temple, Texas, United States 收起 <<
NCT01046864	Gastro-Intestinal Cancer	Phase 1	Completed	-	United States, California ... 展开 >> Usc/Norris Comprehensive Cancer Center Los Angeles, California, United States, 90033 United States, Texas Texas Oncology Dallas, Texas, United States, 75246 Scott & White Memorial Hospital And Clinic Temple, Texas, United States, 76508 Canada, Alberta Local Institution Edmonton, Alberta, Canada, T6G 1Z2 Canada, Ontario Local Institution Ottawa, Ontario, Canada, K1H 8L6 France Local Institution Villejuif Cedex, France, 94800 收起 <<
NCT00207103	Tumors Neopla... 展开 >>sm Metastasis 收起 <<	Phase 1	Completed	-	United States, California ... 展开 >> Premiere Oncology Santa Monica, California, United States, 90404 United States, Indiana Indiana University Med Center Indianapolis, Indiana, United States, 46202 United States, Wisconsin University Of Wisconsin Comprehensive Center Madison, Wisconsin, United States, 53792 Canada, Alberta Local Institution Edmonton, Alberta, Canada, T6G 1Z2 Canada, Ontario Local Institution Ottawa, Ontario, Canada, K1H 1C4 Italy Local Institution Milano, Italy, 20141 United Kingdom Local Institution Middlesex, Greater London, United Kingdom, HA6 2RN Local Institution Manchester, Greater Manchester, United Kingdom, M20 4BX 收起 <<
NCT00858871	Hepato Cellular Carcinoma (HCC... 展开 >>) 收起 <<	Phase 3	Completed	-	-
NCT00798252	Advanced Cancer	Phase 1	Completed	-	United States, California ... 展开 >> Usc/Norris Comprehensive Cancer Center Los Angeles, California, United States, 90033 United States, Massachusetts Dana Farber Cancer Institute Boston, Massachusetts, United States, 02215 United States, Michigan Wayne State University Detroit, Michigan, United States, 48201 Canada, Alberta Local Institution Edmonton, Alberta, Canada, T6G 1Z2 Canada, Ontario Local Institution Toronto, Ontario, Canada, M5G 2M9 收起 <<
NCT01253668	Renal Cell Carcinoma	Phase 2	Completed	-	United States, Pennsylvania ... 展开 >> Abramson Cancer Center of the University of Pennsylvania Philadelphia, Pennsylvania, United States, 19104 收起 <<
NCT00390936	Solid Tumors	Phase 1	Completed	-	Japan ... 展开 >> Local Institution Sunto-Gun, Shizuoka, Japan, 411-8777 收起 <<
NCT00640471	Colorectal Cancer	Phase 3	Completed	-	-
NCT00908752	Hepatocellular Carcinoma	Phase 3	Completed	-	-
NCT00207051	Colorectal Cancer	Phase 1	Completed	-	United States, California ... 展开 >> Usc/Norris Comprehensive Cancer Center Los Angeles, California, United States, 90033 United States, District of Columbia Georgetn Univ Lombardi Can Ctr Washington, District of Columbia, United States, 20007 United States, Florida University Of Miami Miller School Of Medicine Miami, Florida, United States, 33010 H. Lee Moffitt Cancer Center Tampa, Florida, United States, 33612 United States, Michigan Karmanos Cancer Institute Detroit, Michigan, United States, 48201 Canada, Ontario Local Institution Hamilton, Ontario, Canada, L8V 2C5 Local Institution Toronto, Ontario, Canada, M5G 2M9 Netherlands Local Institution Amsterdam, Netherlands, 1081 HV 收起 <<
NCT00435669	Tumors	Phase 1	Completed	-	United States, Ohio ... 展开 >> Cleveland Clinic Foundation Cleveland, Ohio, United States, 44195 收起 <<
NCT00888173	-		Completed	-	-
NCT01267253	Cervical Adenocarcinoma ... 展开 >> Cervical Adenosquamous Carcinoma Cervical Squamous Cell Carcinoma, Not Otherwise Specified Persistent Disease Recurrent Cervical Carcinoma 收起 <<	Phase 2	Active, not recruiting	-	-
NCT01267253	-		Active, not recruiting	-	-
NCT00355238	Hepatocellular Carcinoma (HCC)	Phase 2	Completed	-	-
NCT00437424	Carcinoma, Hepatocellular	Phase 1	Completed	-	United States, Alabama ... 展开 >> University Of Alabama At Birmingham Birmingham, Alabama, United States, 35294 United States, California Usc/Norris Comprehensive Cancer Center Los Angeles, California, United States, 90033 United States, Ohio Case Western Reserve University Clleveland, Ohio, United States, 44106 United States, Texas South Texas Accelerated Research Therapeutics, Llc San Antonio, Texas, United States, 78229 Spain Local Institution Sevilla, Spain, 41013 收起 <<
NCT00633789	Advanced Non-small Cell Lung C... 展开 >>ancer Transitional Cell Carcinoma Soft Tissue Sarcoma Gastric/Esophageal Adenocarcinoma Pancreatic Cancer Including Ampulla of Vater 收起 <<	Phase 2	Completed	-	-
NCT01367275	Colorectal Cancer ... 展开 >> Colorectal Adenocarcinoma 收起 <<	Phase 2	Terminated(Sponsor closed stud... 展开 >>y) 收起 <<	-	United States, Texas ... 展开 >> UT MD Anderson Cancer Center Houston, Texas, United States, 77030 收起 <<
NCT01108705	Carcinoma, Hepatocellular	Phase 3	Terminated	-	-
NCT00888173	Endometrial Adenocarcinoma ... 展开 >> Endometrial Clear Cell Adenocarcinoma Endometrial Mixed Adenocarcinoma Endometrial Mucinous Adenocarcinoma Endometrial Serous Adenocarcinoma Endometrial Squamous Cell Carcinoma Endometrial Transitional Cell Carcinoma Endometrial Undifferentiated Carcinoma Recurrent Uterine Corpus Carcinoma 收起 <<	Phase 2	Completed	-	-
NCT03516071	Hepatocellular Carcinoma (HCC)	Phase 2	Recruiting	May 10, 2019	China, Anhui ... 展开 >> Anhui Provincial Hospital Recruiting Hefei, Anhui, China Contact: Yueyin Pan China, Guangdong Nanfang Hospital Recruiting Guangzhou, Guangdong, China Contact: Jinlin Hou Sun Yat-sen University Cancer Center Recruiting Guangzhou, Guangdong, China Contact: Li Xu China, Heilongjiang Harbin Medical University Cancer Hospital Recruiting Harbin, Heilongjiang, China Contact: Yuxian Bai China, Henan Henan Cancer Hospital Recruiting Zhengzhou, Henan, China Contact: Xinfang Hou China, Hunan Hunan Cancer Hospital Recruiting Changsha, Hunan, China Contact: Shanzhi Gu China, Jiangsu China PLA 81st hospital Recruiting Nanjing, Jiangsu, China Contact: Shukui Qin China, Jilin The first Hospital of Jilin University Recruiting Changchun, Jilin, China Contact: Wei Li China, Liaoning Army General Hospital of Shenyang military region Recruiting Shenyang, Liaoning, China Contact: Zhendong Zheng China, Shanghai Fudan University Shanghai Cancer Center Recruiting Shanghai, Shanghai, China Contact: Zhiqiang Meng Zhongshan Hospital Recruiting Shanghai, Shanghai, China Contact: Zhenggang Ren China, Shanxi Tangdu Hospital Recruiting Xi'an, Shanxi, China Contact: Helong Zhang China, Sichuan West China Hospital West China School of Medicine Sichuan University Recruiting Chengdu, Sichuan, China Contact: Hong Zhu China, Tianjin Tianjin Medical University Cancer Institute & Hospital Recruiting Tianjin, Tianjin, China Contact: Tianqiang Song China, Zhejiang Zhejiang Cancer Hospital Recruiting Hangzhou, Zhejiang, China Contact: Jieer Ying 收起 <<
NCT00825955	Liver Cancer	Phase 3	Terminated(Efficacy endpoint m... 展开 >>et, however, overall experimental dosing regimen is not considered optimal to support further clinical development in this patient population) 收起 <<	-	-
NCT01540461	Hepatocellular Carcinoma	Phase 1	Completed	-	China, Beijing ... 展开 >> Local Institution Beijing, Beijing, China, 100071 China, Heilongjiang Local Institution Ha Erbin, Heilongjiang, China, 150040 China, Jiangsu Local Institution Nanjing, Jiangsu, China, 210002 收起 <<
NCT00437437	Tumors	Phase 1	Completed	-	United States, Massachusetts ... 展开 >> Dana-Farber Harvard Cancer Care Boston, Massachusetts, United States, 02115 United States, Michigan Wayne State University Detroit, Michigan, United States, 48201-2194 United States, North Carolina Duke University Medical Center-Dept Of Medicine Durham, North Carolina, United States, 27710 收起 <<

靶点	VEGFR1 VEGFR1, IC50:380 nM VEGFR2 Flk1, IC50:25 nM VEGFR2, IC50:25 nM FGFR1 FGFR1, IC50:148 nM
描述	Brivanib is an ATP-competitive inhibitor against VEGFR2 with IC50 of 25 nM, moderate potency against VEGFR-1 and FGFR-1, but > 240-fold against PDGFR-β.

CAS号	649735-46-6
分子式	C₁₉H₁₉FN₄O₃
分子量	370.38
SMILES Code	C[C@@H](O)COC1=CN2N=CN=C(OC3=C(F)C4=C(NC(C)=C4)C=C3)C2=C1C
MDL No.	MFCD13194684

别名	BMS-540215
运输	蓝冰
InChI Key	WCWUXEGQKLTGDX-LLVKDONJSA-N
Pubchem ID	11234052

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VEGFR1	VEGFR1, IC50:380 nM
VEGFR2	Flk1, IC50:25 nM VEGFR2, IC50:25 nM
FGFR1	FGFR1, IC50:148 nM

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