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Cabozantinib (BMS-907351)

目录号：S1119 别名: XL184 中文名称：卡博替尼

仅限科研使用

Cabozantinib (XL184, BMS-907351)是一种有效的VEGFR2抑制剂，在无细胞试验中IC50为0.035 nM，也能有效抑制c-Met、 Ret、 Kit、Flt-1/3/4、Tie2和AXL，IC50分别为1.3 nM，4 nM，4.6 nM，12 nM/11.3 nM/6 nM，14.3 nM 和 7 nM。Cabozantinib 在结肠癌细胞中可通过AKT/GSK-3β/NF-κB信号通路诱导PUMA依赖的凋亡。

Cabozantinib (BMS-907351) Chemical Structure

CAS: 849217-68-1

规格	价格	库存
10mM (1mL in DMSO)	RMB 1800.41	现货
5mg	RMB 902.82	现货
50mg	RMB 3837.48	现货
200mg	RMB 8176.22	现货
大包装	有超大折扣
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客户使用Selleck生产的Cabozantinib (BMS-907351)发表文献120篇：

产品安全说明书

VEGFR抑制剂选择性比较

生物活性

产品描述

靶点

VEGFR2/KDR ^[1] (Cell-free assay)	c-Met ^[1] (Cell-free assay)	Axl ^[1] (Cell-free assay)
0.035 nM	1.3 nM	7 nM

体外研究

XL184是多种受体酪氨酸激酶小分子抑制剂，尤其抑制c-Met 和VEGFR2。XL-184也有效作用于Ret, Kit, FLT1, FLT3, FLT4, Tie2, 和 AXL ， IC50分别为 4 nM, 4.6 nM, 12 nM, 11.3 nM, 6 nM, 14.3 nM, 和7 nM。XL184微弱抑制 RON 和PDGFR-β，IC50分别为 124 nM和 234 nM,而对FGFR1则几乎没有抑制活性，IC50 为5.294 μM。^[1] XL184低浓度(0.1-0.5 μM) 时处理MPNST细胞，也显著抑制组成型和诱导型Met磷酸化及其下游信号，且抑制 HGF诱导的MPNST细胞迁移和侵袭。XL184作用于细胞因子刺激的人脐静脉内皮细胞（HUVECs），也显著抑制Met和VEGFR2磷酸化。虽然XL184浓度为0.1 μM时不能抑制MPNST细胞生长，但是浓度为5-10 μM 时则能显著抑制MPNST细胞生长。^[2]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID

E98NT	M{nKUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NFjHZ\|QxNjBzLUGwJO69VQ>?		MUXEUXNQ	M37afWlEPTB;OEmgcm0>	M1vYUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|NEi0NFA3Lz5{M{S4OFAxPjxxYU6=
SNU-5	MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				NV6yUGNJUUN3ME2gNVkhdk1?	M{D2Z\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOUK2NVkyLz5{MUmyOlE6OTxxYU6=
Hs746T	M{\xTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				M2TlRWlEPTB;OT65JI5O	Mm\EQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF7Mk[xPVEoRjJzOUK2NVkyRC:jPh?=
SNU-1	NEPsdmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NF3lO4ZKSzVyPUWyNlMhdk1?	NWTvZ2ZFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG5NlYyQTFpPkKxPVI3OTlzPD;hQi=>
SNU-16	NVPSOFV6T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NHrycFVKSzVyPUGxOFkhdk1?	MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTl{NkG5NUc,OjF7Mk[xPVE9N2F-
MDA-MB-231	MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				NILHRlNKSzVyPTC2OFIyKG6P	MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTl{NkG5NUc,OjF7Mk[xPVE9N2F-
U87MG	NGHqSXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				NGPzVmJKSzVyPUG4OVEhdk1?	MlzFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF7Mk[xPVEoRjJzOUK2NVkyRC:jPh?=
H441	NEPDS2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				MWTJR\|UxRTJzN{CwJI5O	M4P6V\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOUK2NVkyLz5{MUmyOlE6OTxxYU6=
H69	MmrkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NF\yb4hKSzVyPUKwNlAxKG6P	NIXzXoM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUmyOlE6OSd-MkG5NlYyQTF:L3G+
PC3	NVe3Sm1nT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				M4LiO2lEPTB;MUC4NFAhdk1?	NXrHfJZVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG5NlYyQTFpPkKxPVI3OTlzPD;hQi=>
MTC-TT	NVyzb\|FiT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NE\GS4hKSzVyPUCuNFQhMyByLkCzJO69VQ>?	MonLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF2N{C5PVUoRjJzNEewPVk2RC:jPh?=
MZ-CRC	MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				M4DQSWlEPTB-IEWg{txO	M{LCVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNEewPVk2Lz5{MUS3NFk6PTxxYU6=
TPC-1	NV;PNHkyT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NELrPYxKSzVyPUCuNFYhMyByLkCyJO69VQ>?	MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTR5MEm5OUc,OjF2N{C5PVU9N2F-
NIH-3T3/TPR-Met	MmHDSpVv[3Srb36gZZN{[Xl?				NFLhVmlKdmirYnn0bY9vKG:oIHPlcIwheHKxbHnm[ZJifGmxbjDpckBud3W\|ZTDOTWguO1R\|L2TQVk1O\XRiY3XscJMtKEmFNUCgQUAyKM7:TT6=	NV7yXHpGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5PVYyPDRpPkK0PVk3OTR2PD;hQi=>
BA/F3	NH;YVmhIem:5dHigbY5pcWKrdHnvckBie3OjeR?=				NULS[lY3UW6qaXLpeIlwdiCxZjDUSWwu\nW\|ZXSgWmVITlJ{IDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJI1wfXOnIFLBM2Y{KGOnbHzzJIF{e2W\|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36sJGdKPTBiPTCwMlAxOyEQvF2u	NUXJeFQ2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[2OVI5PjBpPkK2OlUzQDZyPD;hQi=>
BaF3	NVm2boh5T3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		NVP1T4VDPDhiaILz		Mm\jTY5pcWKrdHnvckBw\iCWRVyt[pV{\WRiUnX0JHM5QTGDIH31eIFvfCBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDtc5V{\SCEYV[zJINmdGy\|IHHzd4V{e2WmIHHzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiR1m1NEA:KDBwMEGg{txONg>?	MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjZ3Mki2NEc,OjZ4NUK4OlA9N2F-
BA/F3	MWLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		NYLlfXRqPDhiaILz		M{i5RWlvcGmkaYTpc44hd2Zid3ns[EB1gXCnIGTFUE1nfXOnZDDSSXQhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5ibX;1d4UhSkFxRkOgZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCJSUWwJF0hOC5yNTFOwG0v	NWew[m1DRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[2OVI5PjBpPkK2OlUzQDZyPD;hQi=>
TT	MkLzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		M2m1[FExKGSjeYO=		MkjITY5pcWKrdHnvckBw\iCURWSgR\|Y{PFdibYX0ZY51KGmwIHj1cYFvKFSWIHPlcIx{KGG\|c3Xzd4VlKGG\|IHPlcIwh\3Kxd4ToJIlvcGmkaYTpc44h[W[2ZYKgNVAh\GG7czDifUBOXFRiYYPzZZktKEeLNUCgQUAxNjF{IN88UU4>	NI\M[Hg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nk[1Nlg3OCd-Mk[2OVI5PjB:L3G+
BA/F3	M1HX[mdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		M2fxSlQ5KGi{cx?=		MnPMTY5pcWKrdHnvckBw\iCWRVyt[pV{\WRiUnX0JHY5ODSPIH31eIFvfCBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDtc5V{\SCEQT;GN{Bk\WyuczDhd5Nme3OnZDDhd{Bk\WyuIHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFfJOVAhRSByLki5JO69VS5?	NYewc\|YxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[2OVI5PjBpPkK2OlUzQDZyPD;hQi=>
BaF3	M3Lybmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		NIrkR3o1QCCqcoO=		M4jmemlvcGmkaYTpc44hd2ZiVFXMMYZ2e2WmIGLleEBXQDB2TDDteZRidnRiKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gcY92e2ViQnHGN{Bk\WyuczDhd5Nme3OnZDDhd{Bk\WyuIHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFfJOVAhRSByLkmxJO69VS5?	M13LdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NkWyPFYxLz5{Nk[1Nlg3ODxxYU6=
Nthy-ori 3-1	M2[4XGN6fG:2b4jpZ4l1gSCjc4PhfS=>		Mo\SNVAh\GG7cx?=		M1npWWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG51cHlvb4LpJFMuOSClZXzsd{Bi\nSncjCxNEBl[Xm\|IHL5JG1VXCCjc4PhfUwhT0l3MDC9JFQvQTNizszNMi=>	MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjZ3Mki2NEc,OjZ4NUK4OlA9N2F-
BAF3	MYLGeY5kfGmxbjDhd5NigQ>?	M{[yTlAvODFidH:gNVAhfU1?	MlnNNUBpeg>?		NIDvXY9KdmirYnn0bY9vKG:oIGTFUE1nfXOnZDD3bYxlKHS7cHWgVoV1KCi3bnvuc5dvKG:{aXfpckkheGixc4Doc5J6dGG2aX;uJIF1KFlzME[yM3k6ODViZYjwdoV{e2WmIHnuJI1wfXOnIFLBSlMh[2WubIOgZZQhOC5yMTD0c{AyOCC3TTDh[pRmeiBzIHjyJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?=	M4DZdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NkWyPFYxLz5{Nk[1Nlg3ODxxYU6=
TT	NEPMRoFHfW6ldHnvckBie3OjeR?=		NX;xOHN3PCCqcoO=		M2joW2lvcGmkaYTpc44hd2ZiYYX0c5Bpd3OyaH;yfYxifGmxbjDv[kBTTVRiQ{[zOHchdXW2YX70JIF1KFl7MEWgbY4hcHWvYX6gWHQh[2WubIOgZZQhOSC3TTDh[pRmeiB2IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm\|aYO=	M{fwRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NkWyPFYxLz5{Nk[1Nlg3ODxxYU6=
BAF3	MXXGeY5kfGmxbjDhd5NigQ>?	MmrrNE4xOSC2bzCxNEB2VQ>?	M3XlbVEhcHJ?		M3;jXGlvcGmkaYTpc44hd2ZiVFXMMYZ2e2WmIGLleEBUQDlzQTDteZRidnRiKIXub45wf25ib4Lp[4lvMSCyaH;zdIhwenmuYYTpc44h[XRiWUGwOlIwYTlyNTDlfJBz\XO\|ZXSgbY4hdW:3c3WgRmFHOyClZXzsd{BifCByLkCxJJRwKDFyIIXNJIFnfGW{IEGgbJIh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz	M4HYdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NkWyPFYxLz5{Nk[1Nlg3ODxxYU6=
BAF3	M4npVmZ2dmO2aX;uJIF{e2G7	M1OxcVAvODFidH:gNVAhfU1?	NF7teYcyKGi{		Mo\FTY5pcWKrdHnvckBw\iCWRVyt[pV{\WRiUnX0JHM5QTGDIH31eIFvfCBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDtc5V{\SCEQV[zJINmdGy\|IHHzd4V{e2WmIHHzJJN2eHC{ZYPzbY9vKG:oIIDoc5NxcG:{eXzheIlwdiCxZjDQUGNo[W2vYTDheEB[Pzh\|IHH0JFAvODFidH:gNVAhfU1iYX\0[ZIhOSCqcjDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN?	NHW2U409[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nk[1Nlg3OCd-Mk[2OVI5PjB:L3G+
BAF3	MXzGeY5kfGmxbjDhd5NigQ>?	MmHRNE4xOSC2bzCxNEB2VQ>?	MY[xJIhz		NXHicY97UW6qaXLpeIlwdiCxZjDUSWwu\nW\|ZXSgVoV1KFN6OUHBJI12fGGwdDCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBud3W\|ZTDCRWY{KGOnbHzzJIF{e2W\|c3XkJIF{KHO3cIDy[ZN{cW:wIH;mJJBpd3OyaH;yfYxifGmxbjDv[kBUcGNiYYSgXVMyPyCjdDCwMlAyKHSxIEGwJJVOKGGodHXyJFEhcHJiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{	MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjZ3Mki2NEc,OjZ4NUK4OlA9N2F-
TT	Mmf3SpVv[3Srb36gZZN{[Xl?	MkTpNUB1dyBzMDD1US=>	MkfLOEBpenN?		NH\mPYJKdmirYnn0bY9vKG:oIGLFWEBEPjN2VzDteZRidnRiaX6gbJVu[W5iVGSgZ4VtdHNiYYPz[ZN{\WRiYYOgd5VxeHKnc4Ppc44hd2ZiUFzD[4FudWFicHjvd5Bpd3K7bHH0bY9vKGG2IGm3PFMh[XRiMTD0c{AyOCC3TTDh[pRmeiB2IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm\|aYO=	MkDGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ4NUK4OlAoRjJ4NkWyPFYxRC:jPh?=
TT	MmKwSpVv[3Srb36gZZN{[Xl?	MY[xJJRwKDFyIIXN	NHn4fpU1KGi{cx?=		NELBeYJKdmirYnn0bY9vKG:oIGLFWEBEPjN2VzDteZRidnRiaX6gbJVu[W5iVGSgZ4VtdHNiYYPz[ZN{\WRiYYOgd5VxeHKnc4Ppc44hd2ZiRWLLJJBpd3OyaH;yfYxifGmxbjDheEBVOjB{L2myNFQh[XRiMTD0c{AyOCC3TTDh[pRmeiB2IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm\|aYO=	NXrYRYcyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[2OVI5PjBpPkK2OlUzQDZyPD;hQi=>
TT	M1joOmZ2dmO2aX;uJIF{e2G7	MYSxJJRwKDFyIIXN	MWS0JIhzew>?		NX3NRZg2UW6qaXLpeIlwdiCxZjDSSXQhSzZ\|NGegcZV1[W62IHnuJIh2dWGwIGTUJINmdGy\|IHHzd4V{e2WmIHHzJJN2eHC{ZYPzbY9vKG:oIFHLWEBxcG:\|cHjvdplt[XSrb36gZZQhXDNyOD;TOFc{KGG2IEGgeI8hOTBidV2gZYZ1\XJiNDDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz	M4T5VVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NkWyPFYxLz5{Nk[1Nlg3ODxxYU6=
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SNU5	M2myZWFvfGmycn;sbYZmemG2aY\lJIF{e2G7		MnXHO\|IhcHK\|		NWHuVpRSSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTUnU2KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO\|YYmsJGlEPTBiPTCwMlAyOjFizszNMi=>	NXnmdYFpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyOFg3PTRpPkOwNlQ5PjV2PD;hQi=>
BAF3	NYr6cFVnTnWwY4Tpc44h[XO\|YYm=		M{LYe\|czKGi{cx?=		NVmwXnJXUW6qaXLpeIlwdiCxZjDUVHIufGGpZ3XkJI1mfCBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDtc5V{\SCEQV[zJINmdGy\|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiY3XscEBxem:uaX\ldoF1cW:wIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSByLkCxPVg3KM7:TT6=	NHq3OVc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9\|MEK0PFY2PCd-M{CyOFg3PTR:L3G+
NCI-H460	MnLvRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		NETqS3M4OiCqcoO=		MmjxRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCQQ1mtTFQ3OCClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG\|c3H5MEBKSzVyIE2gNE4xPDBzIN88UU4>	MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ2OE[1OEc,OzB{NEi2OVQ9N2F-
MGHU3	M37wdGFvfGmycn;sbYZmemG2aY\lJIF{e2G7		NWPkRmczPzJiaILz		M3W3VmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVfIWVMh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8h[XO\|YYm=	NUO1[IJwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CzNFk3PzFpPkOwN\|A6PjdzPD;hQi=>
RT112	NEC5clhCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		MlXRO\|IhcHK\|		MUXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFKWMUGyJINmdGy\|IHHmeIVzKDd{IHjyd{BjgSCFZXzsWIl1\XJvR3zvJIF{e2G7	NXHWdIQ1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CzNFk3PzFpPkOwN\|A6PjdzPD;hQi=>

Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID

Western blot	p-MET(Y1234/1235) / MET / p-EGFR(Y1068) / EGFR / p-Gab1(Y627) / Gab1 / p-AKT(S473) / p-ERK / p-EIF4E p-MET / p-ERK / p-AKT	29188469 29520051
Immunofluorescence	α-tubulin	29520051
Growth inhibition assay	Cell viability	23661005

体内研究

XL184按 30 mg/kg 剂量处理携带自发胰岛细胞瘤的RIP-Tag2 小鼠，扰乱 83%肿瘤血管, 降低周细胞和空基底膜袖，引起广泛瘤内缺氧和广泛的肿瘤细胞凋亡，且停药后延缓肿瘤血管再生长，与XL999相比更显著抑制VEGFR而不是c-Met，导致血管降低43％，说明抑制VEGFR，也抑制放大抑制血管新生的其他功能相关的受体酪氨酸激酶（RTK）。XL184也降低原发肿瘤的侵袭和减少转移。^[1] XL184 每天按30 mg/kg剂量处理SCID小鼠，显著废除人 MPNST移植瘤生长和转移。^[2] XL184 处理乳腺癌，肺癌胶质瘤模型，抑制肿瘤生长，这种作用存在剂量依赖性，降低肿瘤和内皮细胞增殖，促进凋亡。XL184按100 mg/kg 和 10 mg/kg剂量分别单独处理携带MDA-MB-231肿瘤的小鼠和携带C6肿瘤的大鼠，持续抑制肿瘤生长。^[3]

细胞实验： ^[2]	Cell lines: ST88-14, STS26T, 和MPNST724 Concentrations: 溶于DMSO,终浓度~10 μM Incubation Time: 48小时 Method: 使用不同浓度XL184处理细胞48小时。通过MTS实验使用CellTiter96 Aqueous 非放射性细胞增殖实验试剂盒测定细胞生长。然后在 490 nm处测定吸光值。
动物实验：^[1]	Animal Models: 携带自发胰岛肿瘤的RIP-TAG2转基因小鼠。 Dosages: ~60 mg/kg Administration: 口服饲喂

参考文献	[1] You WK, et al. Cancer Res, 2011, 71(14), 4758-4768. [2] Torres KE, et al. Clin Cancer Res, 2011, 17(12), 3943-3955. [3] Yakes FM, et al. Mol Cancer Ther, 2011, 10(12), 2298-2308.

溶解度（25°C）

体外


体内	从左到右依次将纯溶剂加入产品，现配现用(数据来自Selleck实验检测而非文献)： 2% DMSO+30% PEG 300+5% Tween 80+ddH2O 点击购买： PEG300 Tween 80	5mg/mL

* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量	501.51
化学式	C₂₈H₂₄FN₃O₅
CAS号	849217-68-1
储存条件	3年	-20°C	粉状
储存条件	2年	-80°C	溶于溶剂

Download Cabozantinib (BMS-907351) SDF

动物体内配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH₂O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

临床试验信息

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05048212	Not yet recruiting	Drug: Nivolumab\|Drug: Ipilimumab\|Drug: Cabozantinib	Brain Metastases\|Renal Cell Carcinoma	M.D. Anderson Cancer Center\|Exelixis\|Bristol-Myers Squibb	February 28 2022	Phase 2
NCT05182164	Not yet recruiting	Drug: Association of pembrolizumab + cabozantinib	Soft Tissue Sarcoma Adult\|Advanced Soft-tissue Sarcoma\|Ewing Sarcoma\|Osteosarcoma\|Undifferentiated Pleomorphic Sarcoma	Institut Bergonié\|Ipsen\|MSD France	December 31 2021	Phase 2
NCT05100082	Recruiting	Drug: Cabozantinib	Hepatocellular Cancer	Takeda	November 17 2021	--
NCT05135975	Active not recruiting	Drug: Cabozantinib	Neuroblastoma\|CNS Tumor\|Sarcoma	Nationwide Children''s Hospital\|Exelixis	October 18 2021	Phase 2
NCT05048901	Not yet recruiting	Drug: Cabozantinib\|Drug: Lanreotide	Neuroendocrine TumorsGastroenteropancreatic	National Health Research Institutes Taiwan\|National Taiwan University Hospital\|Taipei Veterans General Hospital Taiwan\|Mackay Memorial Hospital\|Tri-Service General Hospital\|Changhua Christian Hospital\|China Medical University Hospital\|National Cheng-Kung University Hospital\|Kaohsiung Medical University Chung-Ho Memorial Hospital	September 30 2021	Phase 1\|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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