Cabozantinib (BMS-907351)

For research use only. Not for use in humans.

目录号:S1119 别名: XL184 中文名称:卡博替尼

Cabozantinib (BMS-907351) Chemical Structure

CAS No. 849217-68-1

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。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1800.41 现货
RMB 902.82 现货
RMB 3837.48 现货
RMB 8176.22 现货
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客户使用Selleck生产的Cabozantinib (BMS-907351)发表文献94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 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。
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  MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUm3SIo3OC5yMT2xNEDPxE1? MWHEUXNQ MkPaTWM2OD16OTDuUS=> M{TTWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NEi0NFA3Lz5{M{S4OFAxPjxxYU6=
SNU-5  NYHmcmVmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRSBzOTDuUS=> Ml75QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF7Mk[xPVEoRjJzOUK2NVkyRC:jPh?=
Hs746T  NWTLfWJLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rWUGlEPTB;OT65JI5O MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTl{NkG5NUc,OjF7Mk[xPVE9N2F-
SNU-1  MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLpTWM2OD13MkKzJI5O NYe1cYZYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG5NlYyQTFpPkKxPVI3OTlzPD;hQi=>
SNU-16 MkLQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTFzNEmgcm0> NXX2SIRURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG5NlYyQTFpPkKxPVI3OTlzPD;hQi=>
MDA-MB-231 MnXDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFGxUGtKSzVyPTC2OFIyKG6P NF:4RZg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUmyOlE6OSd-MkG5NlYyQTF:L3G+
U87MG NGfCbZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGXUR29KSzVyPUG4OVEhdk1? NXnFNnBLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG5NlYyQTFpPkKxPVI3OTlzPD;hQi=>
H441  NGrET5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\FNHNsUUN3ME2yNVcxOCCwTR?= Ml:1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF7Mk[xPVEoRjJzOUK2NVkyRC:jPh?=
H69 Mn74S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;ESIJKSzVyPUKwNlAxKG6P NIi0b2I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUmyOlE6OSd-MkG5NlYyQTF:L3G+
PC3 MoHyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTFyOECwJI5O NEDxSHo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUmyOlE6OSd-MkG5NlYyQTF:L3G+
MTC-TT MlHIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLETWM2OD1yLkC0JEshOC5yMzFOwG0> Mne1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF2N{C5PVUoRjJzNEewPVk2RC:jPh?=
MZ-CRC NVzONY5RT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHhRoNKSzVyPjC1JO69VQ>? NYXTO5hrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG0O|A6QTVpPkKxOFcxQTl3PD;hQi=>
TPC-1 NVHlPFZwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfUZYdKSzVyPUCuNFYhMyByLkCyJO69VQ>? M4X2N|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNEewPVk2Lz5{MUS3NFk6PTxxYU6=
NIH-3T3/TPR-Met M3K3W2Z2dmO2aX;uJIF{e2G7 MlnHTY5pcWKrdHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25iaX6gcY92e2ViTlnIMVNVOy:WUGKtUYV1KGOnbHzzMEBKSzVyIE2gNUDPxE1w M4fGVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUm2NVQ1Lz5{NEm5OlE1PDxxYU6=
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BaF3 M2fqeGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmL5OFghcHK| MlrUTY5pcWKrdHnvckBw\iCWRVyt[pV{\WRiUnX0JHM5QTGDIH31eIFvfCBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDtc5V{\SCEYV[zJINmdGy|IHHzd4V{e2WmIHHzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiR1m1NEA:KDBwMEGg{txONg>? M3\HXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NkWyPFYxLz5{Nk[1Nlg3ODxxYU6=
BA/F3 NGW4WodIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3fOcFQ5KGi{cx?= NV2zTWZwUW6qaXLpeIlwdiCxZjD3bYxlKHS7cHWgWGVNNW[3c3XkJHJGXCBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDtc5V{\SCEQT;GN{Bk\WyuczDhd5Nme3OnZDDhd{Bk\WyuIHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFfJOVAhRSByLkC1JO69VS5? NX70cYd5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[2OVI5PjBpPkK2OlUzQDZyPD;hQi=>
TT Mo\qS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGS2cGcyOCCmYYnz NXj1UXZ2UW6qaXLpeIlwdiCxZjDSSXQhSzZ|NGegcZV1[W62IHnuJIh2dWGwIGTUJINmdGy|IHHzd4V{e2WmIHHzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhOTBiZHH5d{BjgSCPVGSgZZN{[XluIFfJOVAhRSByLkGyJO69VS5? NEDqb2o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nk[1Nlg3OCd-Mk[2OVI5PjB:L3G+
BA/F3 NHPOfIZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnvvOFghcHK| M3fMRWlvcGmkaYTpc44hd2ZiVFXMMYZ2e2WmIGLleEBXQDB2TTDteZRidnRiKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gcY92e2ViQlGvSlMh[2WubIOgZZN{\XO|ZXSgZZMh[2WubDDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDHTVUxKD1iMD64PUDPxE1w MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjZ3Mki2NEc,OjZ4NUK4OlA9N2F-
BaF3 M{ntR2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYrzc49CPDhiaILz M2raT2lvcGmkaYTpc44hd2ZiVFXMMYZ2e2WmIGLleEBXQDB2TDDteZRidnRiKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gcY92e2ViQnHGN{Bk\WyuczDhd5Nme3OnZDDhd{Bk\WyuIHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFfJOVAhRSByLkmxJO69VS5? NGDPOXo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nk[1Nlg3OCd-Mk[2OVI5PjB:L3G+
Nthy-ori 3-1 MUPDfZRwfG:6aXPpeJkh[XO|YYm= MkLMNVAh\GG7cx?= NGXkVJpEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBPfGi7LX;ybUA{NTFiY3XscJMh[W[2ZYKgNVAh\GG7czDifUBOXFRiYYPzZZktKEeLNUCgQUA1Njl|IN88UU4> NGO2dYc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nk[1Nlg3OCd-Mk[2OVI5PjB:L3G+
BAF3 MoHXSpVv[3Srb36gZZN{[Xl? NVHKNoFkOC5yMTD0c{AyOCC3TR?= NV;NZpI2OSCqch?= Mn\VTY5pcWKrdHnvckBw\iCWRVyt[pV{\WRid3ns[EB1gXCnIGLleEApfW6tbn;3ckBwemmpaX6pJJBpd3OyaH;yfYxifGmxbjDheEB[OTB4Mj;ZPVA2KGW6cILld5Nm\CCrbjDtc5V{\SCEQV[zJINmdGy|IHH0JFAvODFidH:gNVAhfU1iYX\0[ZIhOSCqcjDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? M4nUTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NkWyPFYxLz5{Nk[1Nlg3ODxxYU6=
TT NIXyTWxHfW6ldHnvckBie3OjeR?= NXnUe2g4PCCqcoO= MnHBTY5pcWKrdHnvckBw\iCjdYTvdIhwe3Cqb4L5cIF1cW:wIH;mJHJGXCCFNkO0W{BufXSjboSgZZQhYTlyNTDpckBpfW2jbjDUWEBk\WyuczDheEAyKHWPIHHmeIVzKDRiaILzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?= MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjZ3Mki2NEc,OjZ4NUK4OlA9N2F-
BAF3 NU\4SoNsTnWwY4Tpc44h[XO|YYm= M4XOWFAvODFidH:gNVAhfU1? NGDYVo0yKGi{ MWTJcohq[mm2aX;uJI9nKFSHTD3meZNm\CCUZYSgV|g6OUFibYX0ZY51KCi3bnvuc5dvKG:{aXfpckkheGixc4Doc5J6dGG2aX;uJIF1KFlzME[yM3k6ODViZYjwdoV{e2WmIHnuJI1wfXOnIFLBSlMh[2WubIOgZZQhOC5yMTD0c{AyOCC3TTDh[pRmeiBzIHjyJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?= MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjZ3Mki2NEc,OjZ4NUK4OlA9N2F-
BAF3 NFLL[XZHfW6ldHnvckBie3OjeR?= NFrHO5ExNjBzIITvJFExKHWP Mk[0NUBpeg>? NV;nSHA5UW6qaXLpeIlwdiCxZjDUSWwu\nW|ZXSgVoV1KFN6OUHBJI12fGGwdDCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBud3W|ZTDCRWY{KGOnbHzzJIF{e2W|c3XkJIF{KHO3cIDy[ZN{cW:wIH;mJJBpd3OyaH;yfYxifGmxbjDv[kBRVEOpYX3tZUBifCC\N{izJIF1KDBwMEGgeI8hOTBidV2gZYZ1\XJiMTDodkBjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= NUnHNpp4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[2OVI5PjBpPkK2OlUzQDZyPD;hQi=>
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OHS-50 MkPwdWhVWyCjc4PhfS=> NXK3O|JveUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF;IV{02OCClZXzsdy=> NFnEOmQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
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A673 MmTadWhVWyCjc4PhfS=> M1rlU5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJGE3PzNiY3XscJMq MoX3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
U-2 OS MoTidWhVWyCjc4PhfS=> NYe5SXRTeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhXS1{IF;TJINmdGy| NIjJdG89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
OHS-50 M4rOTpFJXFNiYYPzZZk> NF\jcHNyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBQUFNvNUCgZ4VtdHN? MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
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LAN-5 NFPGeolyUFSVIHHzd4F6 NWHie3Y3eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFzBUk02KGOnbHzz MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
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SJ-GBM2 M4m3[JFJXFNiYYPzZZk> NInIN5JyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBUUi2JQl2yJINmdGy| M2fWdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
TC32 NGPifmtyUFSVIHHzd4F6 NWXvWYQ2eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhXEN|MjDj[Yxtew>? M1PBU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Saos-2 M2\GUJFJXFNiYYPzZZk> MkjLdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgV4Fwey1{IHPlcIx{ NVLkcYxURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
EBC1 NY\L[WppSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NGLTNJY4OiCqcoO= M1\mdmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iRVLDNUBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxKD1iMD6wNFQ5KM7:TT6= NVHvTHpGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyOFg3PTRpPkOwNlQ5PjV2PD;hQi=>
MKN45 NEfTfZpCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M2TqXVczKGi{cx?= NXnOT|FJSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNT241PSClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyIE2gNE4xODZ7IN88UU4> MoXqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{NEi2OVQoRjNyMkS4OlU1RC:jPh?=
SNU5 M4rB[GFvfGmycn;sbYZmemG2aY\lJIF{e2G7 M1PXc|czKGi{cx?= M2nL[2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU17VOUBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxKD1iMD6wNVIyKM7:TT6= M3r2WFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkS4OlU1Lz5|MEK0PFY2PDxxYU6=
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NCI-H460 Mm[yRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MnTxO|IhcHK| MkjIRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mtTFQ3OCClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyIE2gNE4xPDBzIN88UU4> MkTEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{NEi2OVQoRjNyMkS4OlU1RC:jPh?=
MGHU3 MoO1RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MVK3NkBpenN? M4P2VmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVfIWVMh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8h[XO|YYm= NWXCeI8{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CzNFk3PzFpPkOwN|A6PjdzPD;hQi=>
RT112 M{m4T2FvfGmycn;sbYZmemG2aY\lJIF{e2G7 M4fJbFczKGi{cx?= NUWxd4kySW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDSWFEyOiClZXzsd{Bi\nSncjC3NkBpenNiYomgR4VtdFSrdHXyMWdtdyCjc4PhfS=> MkjpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB|MEm2O|EoRjNyM{C5OlcyRC:jPh?=

... 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; 

PubMed: 29188469     


MET kinase inhibitors but not emibetuzumab inhibited MET signaling pathway in Hs746t cells in vitro by western blot analysis. Hs746t cells were treated for 24 h with 133 nM (20 μg/ml) or 667 nM (100 μg/ml) emibetuzumab or MET kinase inhibitors (merestinib, PF04217903, crizotinib, cabozantinib) at 15.6, 62.5, 250 or 1000 nM.

p-MET / p-ERK / p-AKT; 

PubMed: 29520051     


Western blot analysis of cellular pathways modifications after CBZ 5 μM treatment in HOS, MG-63, Saos-2 and U-2 OS cells; (A) CBZ 5 μM inhibits c-MET phosphorilation after 1 hour of treatment; downstream ERK activation kinetic adopts a sigmoidal shape in all OS cell lines, whereas AKT activation is strongly inhibited in HOS, Saos-2 and U-2OS, but not in MG-63 cells.

29188469 29520051
Immunofluorescence
α-tubulin; 

PubMed: 29520051     


Immunostaining of mitotic spindle in control and CBZ 5 μM treated HOS cells using a monoclonal antibody against α-tubulin (in green); white arrows indicate the mitotic spindle poles; control cells show normal bipolar spindles during metaphase formation, whereas treated cells show tripolar spindles during prometaphase (II), metaphase (III) and anaphase (IV); bar scale = 10 μm.

29520051
Growth inhibition assay
Cell viability; 

PubMed: 23661005     


Cells were left untreated or were treated with 5, 7.5 or 10 μM cabozantinib (XL184). Seventy-two hours later viability was detected by MTT-assay and apoptosis by staining with annexinV-FITC followed by FACS-analysis.

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]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验: [2]
- 合并
  • 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。
    (Only for Reference)
动物实验:[1]
- 合并
  • 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
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 100 mg/mL (199.39 mM)
Water Insoluble
Ethanol Insoluble
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
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 粉状
溶于溶剂
别名 XL184

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 ul 动物数量
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
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04957160 Not yet recruiting -- Advanced Renal Cell Carcinoma (aRCC) Ipsen September 4 2021 --
NCT04868773 Recruiting Drug: Cabozantinib|Drug: TAS-102 Colorectal Cancer|Colorectal Carcinoma|Metastatic Cancer|CRC University of California Irvine July 2021 Phase 1
NCT04893785 Not yet recruiting Drug: Cabozantinib and Temozolomide Lung Neuroendocrine Neoplasm|GEP Neuroendocrine Tumor National Cancer Institute Naples June 2021 Phase 2
NCT04804813 Recruiting Drug: Cabozantinib Renal Cell Carcinoma Takeda March 29 2021 --
NCT04631744 Recruiting Drug: Cabozantinib Prostate Cancer Weill Medical College of Cornell University|Exelixis March 3 2021 Phase 2
NCT04300140 Recruiting Drug: AVB-S6-500|Drug: Cabozantinib (Cabo) Clear Cell Renal Cell Carcinoma Aravive Inc. February 26 2021 Phase 1|Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID