Ispinesib (SB-715992)

目录号:S1452 别名: CK0238273 中文名称:伊斯平斯

仅限科研使用

Ispinesib (SB-715992, CK0238273)是一种有效的,特异性的,可逆kinesin spindle protein (KSP)抑制剂,无细胞试验中Kiapp为1.7 nM,对CENP-E, RabK6, MCAK, MKLP1,KHC和Kif1A没有抑制作用。Ispinesib可诱导有丝分裂阻滞和细胞的凋亡。Phase 2。

Ispinesib (SB-715992) Chemical Structure

CAS: 336113-53-2

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 3457.54 现货
RMB 2621.56 现货
RMB 7941.69 现货
大包装 有超大折扣

今日订购,明日送达 全国免运费 分装免费 分装成小规格产品(单支最小为1mg)
如1支10mg产品可分装为10支1mg产品

全国免费电话:400-668-6834   |   Email:info@selleck.cn

客户使用Selleck生产的Ispinesib (SB-715992)发表文献23篇:

产品安全说明书

Kinesin抑制剂选择性比较

相关Kinesin产品

生物活性

产品描述 Ispinesib (SB-715992, CK0238273)是一种有效的,特异性的,可逆kinesin spindle protein (KSP)抑制剂,无细胞试验中Kiapp为1.7 nM,对CENP-E, RabK6, MCAK, MKLP1,KHC和Kif1A没有抑制作用。Ispinesib可诱导有丝分裂阻滞和细胞的凋亡。Phase 2。
特性 Ispinesib是一种有效可逆的特定有丝分裂驱动蛋白(KSP)变构抑制剂。
靶点
KSP (HsEg5) [1]
(Cell-free assay)
1.7 nM(Ki app)
体外研究

Ispinesib 是有效可逆的特定KSP变构抑制剂,KSP与微管的结合性能,通过抑制ADP释放而不改变微管中KSP-ADP复合体的释放,而扰乱KSP的运动。[1] Ispinesib作用于一系列肿瘤细胞系, 包括Colo205, Colo201, HT-29, M5076, Madison-109,和MX-1, IC50为1.2 nM 到 9.5 nM,具有很强细胞毒性。[2] 15 nM 和 30 nM Ispinesib作用于PC-3前列腺癌细胞, 通过调节控制凋亡,细胞增殖,细胞周期,和信号的基因表达水平,如EGFR, p27, p15, 和IL-11,而抑制细胞增殖和诱导凋亡。[3] 7.4 nM–600 nM Ispinesib 作用于一组53种乳腺癌细胞系,具有广谱抑制活性。150 nM Ispinesib 作用于BT-474 和MDA-MB-468细胞,诱导凋亡, 提高凋亡细胞比例,降低抗凋亡的Bcl-XL水平,和提高促凋亡的Bax和Bid 水平。[4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HCT116 MmLkRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MXK3NkBpenN? MYPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczDh[pRmeiB5MjDodpMh[nliQXzhcYFzKGKudXWgZZN{[XluIFfJOVA:OC5yMkZOwG0> NFe2[Zc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkK0PFI3Oid-MkKyOFgzPjJ:L3G+
hTERT-HME1 NYnMOmdqSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NI\1TFU4OiCqcoO= NIrBZm5CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIHjUSXJVNUiPRUGgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KEGuYX3hdkBjdHWnIHHzd4F6NCCJSUWwQVAvODN{zszN M2XZSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MkS4NlYzLz5{MkK0PFI3OjxxYU6=
K562 NEDVW3FCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NEXGNWs4OiCqcoO= Mn\6RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCNNU[yJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCDbHHtZZIh[my3ZTDhd5NigSxiR1m1NF0xNjB5Md88US=> M1HGcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MkS4NlYzLz5{MkK0PFI3OjxxYU6=
BxPC3 NX3ZUmNwSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M2H0d|czKGi{cx?= MlPqRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCEeGDDN{Bk\WyuczDh[pRmeiB5MjDodpMh[nliQXzhcYFzKGKudXWgZZN{[XluIFfJOVA:OC5yON88US=> NXnMRlZFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyOFgzPjJpPkKyNlQ5OjZ{PD;hQi=>
NCI-H1299 NWjndohsSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M3vS[VczKGi{cx?= M2jzOGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWgyOjl7IHPlcIx{KGGodHXyJFczKGi{czDifUBCdGGvYYKgZox2\SCjc4PhfUwhT0l3ME2wMlA5Os7:TR?= M3TiPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MkS4NlYzLz5{MkK0PFI3OjxxYU6=
LNCAP MknLS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MY[3NkBpenN? M3zmOWdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJGxPS0GSIHPlcIx{KGGodHXyJFczKGi{czDifUBCdGGvYYKgZox2\SCjc4PhfUwhT0l3ME2wMlAzOs7:TR?= MoXtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|OUSxPFAoRjJ|M{m0NVgxRC:jPh?=
HCT116 M1vveWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mmf1O|IhcHK| MWTHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDIR3QyOTZiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JGFt[W2jcjDicJVmKGG|c3H5MEBIUTVyPUCuNFI2|ryP M4LZbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{m0NVgxLz5{M{O5OFE5ODxxYU6=
PC3 MmnrS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXvpeFM5PzJiaILz NVywfmJWT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hWEN|IHPlcIx{KGGodHXyJFczKGi{czDifUBCdGGvYYKgZox2\SCjc4PhfUwhT0l3ME2wMlA2|ryP NYDVSHFMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzPVQyQDBpPkKzN|k1OThyPD;hQi=>
BxPC3 MVnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWO3NkBpenN? M1jjcGdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJGJ5WEN|IHPlcIx{KGGodHXyJFczKGi{czDifUBCdGGvYYKgZox2\SCjc4PhfUwhT0l3ME2wMlA5|ryP MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN7NEG4NEc,OjN|OUSxPFA9N2F-
NCI-H1299 M13mfWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2L2SlczKGi{cx?= NXnKSJZoT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVixNlk6KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDBcIFu[XJiYnz1[UBie3OjeTygS2k2OD1yLkC4Nu69VQ>? MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN7NEG4NEc,OjN|OUSxPFA9N2F-
LXFS 538 MUnBcpRqfHWvb4KgZZN{[Xl? MlztOkBu\y:tZx?= MoHERY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTGjGV{A2OzhiY3XscJMhgGWwb3fyZYZ1\WRiaX6gUm1TUSCwdT;ueUBud3W|ZTDhd5Nme3OnZDDhd{B1fW2xcjDy[Ydz\XO|aX;uJIF1KDZibXevb4ctKGmyIH3lZZN2emWmIH;uJIRigSBzMx?= M13DSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{m0NVgxLz5{M{O5OFE5ODxxYU6=
HeLa NIr1dHVCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NXzmXm46PDhiaILz MnPNRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKZVzhJINmdGy|IHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:Oc7:TR?= NULNd4dZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxPFQ4PzZpPkK0NVg1Pzd4PD;hQi=>
MCF7 MojyRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NIfobos1QCCqcoO= M1nkcGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTFwM988US=> MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDF6NEe3Okc,OjRzOES3O|Y9N2F-
HCT116 NYLYVpRQT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkHZO|IhcHK| NV\jNVlCT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hUEOWMUG2JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGOgZZN{[XluIFnDOVA:OC5yMEGx{txO MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN7Nk[4PEc,OjZ|OU[2PFg9N2F-
TC32 Ml35dWhVWyCjc4PhfS=> MUfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhXEN|MjDj[Yxtew>? M3LLS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
DAOY MWrxTHRUKGG|c3H5 MoTrdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKESDT2mgZ4VtdHN? NFfQW|k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SJ-GBM2 NHPFXWdyUFSVIHHzd4F6 NEnY[HFyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1qtS2JOOiClZXzsdy=> NV;2VG5TRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
A673 M4nVdpFJXFNiYYPzZZk> MWjxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSTZ5MzDj[Yxtew>? NIjqe2k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SK-N-MC MkOydWhVWyCjc4PhfS=> MkXFdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tUWMh[2WubIO= NYO0RoY1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB-EBc1 MmP6dWhVWyCjc4PhfS=> MX7xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJvRVLjNUBk\Wyucx?= NWfWN5lLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Saos-2 NWq0THh6eUiWUzDhd5NigQ>? MYPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW2Gxcz2yJINmdGy| M1\lZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
LAN-5 NH;lR3FyUFSVIHHzd4F6 MnLIdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEyDTj21JINmdGy| M3jCZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
BT-12 MkfsdWhVWyCjc4PhfS=> M4nnUJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCEVD2xNkBk\Wyucx?= NUfUbIJIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
OHS-50 M2raV5FJXFNiYYPzZZk> NYS2TllOeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF;IV{02OCClZXzsdy=> M2nKNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
A673 NHTS[3hyUFSVIHHzd4F6 MY\xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDBOlc{KGOnbHzzLS=> MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-MC MofhdWhVWyCjc4PhfS=> NXzIVmx{eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?= M2noflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
BT-12 MmC3dWhVWyCjc4PhfS=> MoDNdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgRnQuOTJiY3XscJM> NFe2Ro89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
DAOY MV7xTHRUKGG|c3H5 MnjidWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgSGFQYSClZXzsdy=> MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
BT-37 M4rMeJFJXFNiYYPzZZk> MUnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDCWE0{PyClZXzsdy=> NH\tSGY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
TC32 M4TUOZFJXFNiYYPzZZk> MXjxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDUR|MzKGOnbHzz MoLUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
MG 63 (6-TG R) MkSzdWhVWyCjc4PhfS=> NXTYcHVWeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhVUdiNkOgLFYuXEdiUjmgZ4VtdHN? Mo[xQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
U-2 OS NHHxcI5yUFSVIHHzd4F6 M2i3OpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHUuOiCRUzDj[Yxtew>? MkXwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
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RD NGf1PXdyUFSVIHHzd4F6 MXnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDSSEBk\Wyucx?= MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Rh30 MofDdWhVWyCjc4PhfS=> NFWxWWZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBTcDNyIHPlcIx{ M2GyVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Saos-2 M1rOOJFJXFNiYYPzZZk> MkXGdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgV4Fwey1{IHPlcIx{ NYj0Wmt[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-SH MnrIdWhVWyCjc4PhfS=> MnztdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgV2suVi2VSDDj[Yxtew>? MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
体内研究 Ispinesib按4.5 mg/kg-15 mg/kg剂量作用于携带移植瘤的小鼠模型,有效抑制Colo205, Colo201, HT-29细胞,但是不抑制MX-1细胞。SB-715992按6 mg/kg-10 mg/kg剂量处理,也抑制小鼠实体瘤,包括 Madison 109 肺癌, M5076肉瘤,及L1210和P388白血病。[2] Ispinesib 按8 mg/kg-10 mg/kg剂量作用于携带乳腺癌细胞MCF-7, HCC1954, MDA-MB-468,和KPL4移植瘤的小鼠,抑制肿瘤生长。[4]

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)

激酶实验:[1]
  • 人类KSP ATP酶活性和Ispinesib抑制的稳定动力学分析:

    使用丙酮酸激酶-乳酸脱氢酶检测体系进行驱动蛋白的特异性分析,伴随着NADH氧化产生ADP。在340 nm处检测吸光度的变化。使用纳摩尔浓度KSP进行稳态研究, 使用一个敏感的荧光为基础的检测系统,利用丙酮酸激酶,丙酮酸氧化酶,辣根过氧化物酶(HRP)耦合的检测体系, 伴随着Amplex红色荧光试剂氧化为试卤灵而生成ADP。通过荧光检测产生的试卤灵。在含10 µM paclitaxel紫杉醇的PEM25 buffer [25 mM Pipes-K+ (pH 6.8), 2 mM MgCl2, 1 mM EGTA]中进行稳态生化试验。在含500 µM ATP, 5 µM 微管,和1 nM KSP的PEM25 buffer中测定抑制稳定的IC50值。通过剂量-反应曲线获得Ispinesib的Ki app(明显的抑制剂解离常数)值, 通过使用Morrison方程明确纠正酶浓度。在稳态情况下测定抑制剂形态(竞争性,非竞争性,无竞争力的,或者混合生物)。

细胞实验:[4]
  • Cell lines: Breast 乳腺癌细胞,包括MCF-7, HCC1954, MDA-MB-468,和KPL4
  • Concentrations: 0.085 nM-33 μM
  • Incubation Time: 72小时
  • Method: 指数生长期细胞接种在96孔板上,用Ispinesib处理72小时。然后使用CellTiter-Glo测量细胞生长, 并使用BioTek FLx800测定荧光值。分析数据,计算IC50值。
动物实验:[4]
  • Animal Models: 携带MCF7, KPL4,和HCC1954细胞的(nu/nu)裸鼠模型,携带MDA-MB-468 细胞的SCID小鼠模型
  • Dosages: 10 mg/kg作用于裸鼠,8 mg/kg作用于SCID 鼠
  • Administration: 3倍剂量腹腔注射,每隔四天进行一次

溶解度(25°C)

体外

* 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 517.06
化学式

C30H33ClN4O2

CAS号 336113-53-2
储存条件 3年 -20°C 粉状
2年 -80°C 溶于溶剂

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)

mg/kg g μL

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,: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: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: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

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00607841 Terminated Drug: Ispinesib Breast Neoplasms Cytokinetics December 2007 Phase 1
NCT00354250 Completed Drug: ispinesib Recurrent Renal Cell Cancer|Stage III Renal Cell Cancer|Stage IV Renal Cell Cancer National Cancer Institute (NCI) May 2006 Phase 2
NCT00097409 Completed Drug: Ispinesib Ovarian Cancer GlaxoSmithKline December 2004 Phase 2
NCT00119171 Completed Drug: Ispinesib|Drug: Capecitabine Solid Tumor Cancer GlaxoSmithKline November 2004 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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