YM155 (Sepantronium Bromide)

目录号:S1130

仅限科研使用

YM155 (Sepantronium Bromide)是一种有效的survivin抑制药,通过抑制Survivin启动子活性而发挥作用,在HeLa-SURP-luc 和 CHO-SV40-luc细胞中IC50为0.54 nM;对SV40启动子活性抑制作用不显著,能够轻微抑制Survivin与XIAP相互作用。YM155 在乳腺癌细胞中可下调 survivinXIAP、调节自噬并诱导自噬依赖的DNA损伤。Phase 2。

YM155 (Sepantronium Bromide) Chemical Structure

CAS: 781661-94-7

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 918.45 现货
RMB 568.29 现货
RMB 2214.29 现货
RMB 6310.26 现货
大包装 有超大折扣
大剂量询单有大折扣!

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YM155 (Sepantronium Bromide)发表文献158篇:

产品安全说明书

Survivin抑制剂选择性比较

相关Survivin产品

生物活性

产品描述 YM155 (Sepantronium Bromide)是一种有效的survivin抑制药,通过抑制Survivin启动子活性而发挥作用,在HeLa-SURP-luc 和 CHO-SV40-luc细胞中IC50为0.54 nM;对SV40启动子活性抑制作用不显著,能够轻微抑制Survivin与XIAP相互作用。YM155 在乳腺癌细胞中可下调 survivinXIAP、调节自噬并诱导自噬依赖的DNA损伤。Phase 2。
靶点
Survivin [1]
(HeLa-SURP-luc, CHO-SV40-luc cells)
0.54 nM
体外研究

YM155 30 μM时对SV40作用效果也不大。在p53缺陷的PC-3和PPC-1 人类HRPC细胞中,通过抑制 survivin基因启动子的转录,YM155显著抑制内源性survivin的表达。相反,YM155 100 nM时对c-IAP2, XIAP, Bcl-2, Bcl-xL, Bad, α-actin,及β-tubulin的蛋白表达仍没抑制效果。YM155作用于人类癌细胞系包括PC-3和PPC-1,使细胞发生凋亡,伴随着caspase-3活性上升。YM155有效抑制人类癌细胞系(突变p53或短小p53) 包括PC-3, PPC-1, DU145, TSU-Pr1, 22Rv1, SK-MEL-5及A375 ,IC50值为2.3到11 nM。[1]另外,YM155增强NSCLC细胞对γ-射线的敏感性。YM155和γ-射线联用,增强凋亡细胞数和caspase-3活性。 YM155推迟修复放射诱导核DNA断裂的双链。[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Kasumi-1 M36yV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlLCO|IhcA>? NIPSPIVFVVOR M2LvXWlEPTB;MD6wNFkhyrFiMD6wNFA6KM7:TR?= MorxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV4NUm3N|EoRjJ3NkW5O|MyRC:jPh?=
M-07e NWDEd5hoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX64RXdTPzJiaB?= M3PkZmROW09? MXLJR|UxRTBwMESwJOKyKDBwMEGzJO69VQ>? NEHEfo49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NU[1PVc{OSd-MkW2OVk4OzF:L3G+
THP-1 NGjnT29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVS3NkBp Ml\0SG1UVw>? NFX2eoRKSzVyPUCuNFUyKMLzIECuNFE{KM7:TR?= NXq1b2lMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW2OVk4OzFpPkK1OlU6PzNzPD;hQi=>
CMK NV7YS5ZuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NInVOlI4OiCq NVeyUJB7TE2VTx?= NWi0[oFYUUN3ME2wMlA2OyEEsTCwMlAxQSEQvF2= MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTZ3OUezNUc,OjV4NUm3N|E9N2F-
MV4-11 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3nHUVczKGh? Ml6ySG1UVw>? NX;mWW5tUUN3ME2wMlA2PSEEsTCwMlAzQCEQvF2= NVHBbHJ[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW2OVk4OzFpPkK1OlU6PzNzPD;hQi=>
AML-193 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHG2WpY4OiCq M1XGbGROW09? NIfTR5lKSzVyPUCuOFYzKMLzIECuNFYxKM7:TR?= NUX2XmZ[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW2OVk4OzFpPkK1OlU6PzNzPD;hQi=>
HL-60 NV2yUYt7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1m1eVczKGh? M1rWe2ROW09? NVfLb5N3UUN3ME2wMlAxOSEEsTCwMlAxODJizszN MmTOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV4NUm3N|EoRjJ3NkW5O|MyRC:jPh?=
ML-2 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPWRoE6PzJiaB?= MXPEUXNQ NVzSW2JHUUN3ME2wMlAxQSEEsTCwMlAxOiEQvF2= M3zBW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NkW5O|MyLz5{NU[1PVc{OTxxYU6=
OCI/AML3 NH2zbFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzGUng4OiCq NV3GeZp6TE2VTx?= NUXyU5FtUUN3ME2wMlAyOSEEsTCwMlAxOiEQvF2= NY\zRmNnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW2OVk4OzFpPkK1OlU6PzNzPD;hQi=>
HEL Mnu4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmnhO|IhcA>? M{fhbmROW09? M4DkdmlEPTB;MD61OVkhyrFiMD6wN|gh|ryP M4PDclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NkW5O|MyLz5{NU[1PVc{OTxxYU6=
ME-1 NEO2ZWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXNO|IhcA>? NWPGbYJ6TE2VTx?= M2mxXWlEPTB;MD62PFQhyrFiMD6xO|kh|ryP M1H6WFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NkW5O|MyLz5{NU[1PVc{OTxxYU6=
THP-1 M3vtS2Fxd3C2b4Ppd{BCe3OjeR?= MUSxxsDPxE1? NGH1dWo4OiCq NWK1c4JYTE2VTx?= M2q1U4lv\HWlZYOgZZBweHSxc3nz Mki5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV4NUm3N|EoRjJ3NkW5O|MyRC:jPh?=
M-07e M2j4UWZ2dmO2aX;uJGF{e2G7 NITsbpox6oDVMdMg{txO M{S0d|czKGh? MUXEUXNQ NHP4e5NqdmS3Y3XzJIRwf26{ZXf1cIF1cW:wIH;mJHN2en[rdnnu MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTZ3OUezNUc,OjV4NUm3N|E9N2F-
THP-1 NXTkVIpJTnWwY4Tpc44hSXO|YYm= NV2xU2VJOOLCk{JCpO69VQ>? Mof1O|IhcA>? NXXZZ2wxTE2VTx?= M{LGRolv\HWlZYOg[I94dnKnZ4XsZZRqd25ib3[gV5Vzfmm4aX6= MkLJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV4NUm3N|EoRjJ3NkW5O|MyRC:jPh?=
CMK NWDtZZlQTnWwY4Tpc44hSXO|YYm= M1vVZlDjiJNzwrFOwG0> NGqxTVE4OiCq Ml:wSG1UVw>? NHfnb|NqdmS3Y3XzJIRwf26{ZXf1cIF1cW:wIH;mJHN2en[rdnnu M3;YdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NkW5O|MyLz5{NU[1PVc{OTxxYU6=
AML-193 MXjGeY5kfGmxbjDBd5NigQ>? MYqw5qCUOcLizszN NITRfIQ4OiCq MVPEUXNQ M1XM[olv\HWlZYOg[I94dnKnZ4XsZZRqd25ib3[gV5Vzfmm4aX6= MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTZ3OUezNUc,OjV4NUm3N|E9N2F-
Kasumi-1 NHPPVndHfW6ldHnvckBCe3OjeR?= M3;vSlDjiJNzwrFOwG0> NIixOnY4OiCq NUfYZ3luTE2VTx?= NWDUSm5DcW6mdXPld{Bld3ewcnXneYxifGmxbjDv[kBUfXK4aY\pci=> Mn\iQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV4NUm3N|EoRjJ3NkW5O|MyRC:jPh?=
MV4-11 NHK3WmdHfW6ldHnvckBCe3OjeR?= Ml3TNQKBmzIEoN88US=> Moi1O|IhcA>? MVjEUXNQ MoS5bY5lfWOnczDkc5dvemWpdXzheIlwdiCxZjDTeZJ3cX[rbh?= M2XGNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NkW5O|MyLz5{NU[1PVc{OTxxYU6=
MUG-Chor  MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXmwMVUh|ryP MVOyOE81QCCq NVTDPWhbUUN3ME23MlA26oDLbl2g[o9zKDR6aB?= NFvselQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NU[0NFE5PSd-MkW2OFAyQDV:L3G+
U-CH1  MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLJNE02KM7:TR?= NFrmU2MzPC92ODDo MXXJR|UxRTlwMERihKlvVSCob4KgOFhp NVjDcG5YRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW2OFAyQDVpPkK1OlQxOTh3PD;hQi=>
KATOIII NWnzNXh{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLsNVAwOjBibl2= NVfaXFhCPDhiaB?= NGrleolqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NES3W3U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NU[zOVA2PSd-MkW2N|UxPTV:L3G+
AGS  M1vPbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fSTlExNzJyIH7N MofGOFghcA>? NHHaZ|JqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NUm5e2JbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW2N|UxPTVpPkK1OlM2ODV3PD;hQi=>
SACC-83 MmHNSpVv[3Srb36gRZN{[Xl? NHrvbok2KG6P M3fyV|Q5KGh? Mn3w[IVkemWjc3XzJI52[2ynYYKg[ZhxemW|c3nvckBw\iCKSV[tNe6y MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTR6NU[zOUc,OjV2OEW2N|U9N2F-
INA-6 NH;lc5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;GW|MxNTVyMDDuUS=> MnrZOFghcA>? M3yxfYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M4L6fVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mkm2PVc5Lz5{NUK5Olk4QDxxYU6=
U-266 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MViwMVUxOCCwTR?= MnvKOFghcA>? MVrpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MkLaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{OU[5O|goRjJ3Mkm2PVc5RC:jPh?=
MOLP-8 M1zWWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFvD[GUxNTVyMDDuUS=> NVq1c2drPDhiaB?= M3zMdYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M2\CRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mkm2PVc5Lz5{NUK5Olk4QDxxYU6=
HG-1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fMSlAuPTByIH7N M1\WPVQ5KGh? NWfFVJhocW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NGDGcWw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK5Olk4QCd-MkWyPVY6Pzh:L3G+
NCI-H929 NUP0Z3k1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\4bIgxNTVyMDDuUS=> MYq0PEBp NEf1Z3dqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ7Nkm3PEc,OjV{OU[5O|g9N2F-
OPM-2 NIfoTZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfHdYRTOC13MECgcm0> NFrjcok1QCCq M1f3eYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M2ryflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mkm2PVc5Lz5{NUK5Olk4QDxxYU6=
L-363 NETEcYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUOwMVUxOCCwTR?= Mlz6OFghcA>? NITPdG1qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M4jLcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mkm2PVc5Lz5{NUK5Olk4QDxxYU6=
MOLP-2 NUTHXY5pT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlKxNE02ODBibl2= NUPJWoNXPDhiaB?= NYLsPZVPcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M1jXb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mkm2PVc5Lz5{NUK5Olk4QDxxYU6=
KMS-12-BM MkDnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nlZlAuPTByIH7N MUm0PEBp MUnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NXzOdVA1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyPVY6PzhpPkK1Nlk3QTd6PD;hQi=>
SK-MM-2 NIe0eoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUmwMVUxOCCwTR?= NYLBOlRtPDhiaB?= NUjxOIxGcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ7Nkm3PEc,OjV{OU[5O|g9N2F-
U-266 MWLBdI9xfG:|aYOgRZN{[Xl? Mn;ENE02OCCwTR?= Mm[yNlQhcA>? MWXpcoR2[2W|IHHwc5B1d3Orcx?= MnnEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{OU[5O|goRjJ3Mkm2PVc5RC:jPh?=
INA-6  M2jIZ2Fxd3C2b4Ppd{BCe3OjeR?= MlfGNE02OCCwTR?= MVSyOEBp MnvZbY5lfWOnczDhdI9xfG:|aYO= NHrZNVg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK5Olk4QCd-MkWyPVY6Pzh:L3G+
MCF7 MnXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHYO|IhcA>? MoD2TWM2OD1zMzFCtUA3KG6P MoXRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{MkCyNlUoRjJ3MkKwNlI2RC:jPh?=
MCF7-TamR6 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU[3NkBp NX\DcnZkUUN3ME24JOKyKDZibl2= NXi2OpQ6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyNlAzOjVpPkK1NlIxOjJ3PD;hQi=>
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PANC-1 MWXGeY5kfGmxbjDBd5NigQ>? MUKwMVExODBibl2= MUiyOEBp Ml\6bY5lfWOnczDkc5dvemWpdXzheIlwdiCxZjDYTWFRKGGwZDDzeZJ3cX[rbjDlfJBz\XO|aX;u MoPEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ5MkO4O|EoRjJ{N{KzPFcyRC:jPh?=
MIAPaCa-2 M1jJTGZ2dmO2aX;uJGF{e2G7 MoK2NE0yODByIH7N MoT0NlQhcA>? MUHpcoR2[2W|IHTve45z\We3bHH0bY9vKG:oIGjJRXAh[W6mIIP1dpZqfmmwIHX4dJJme3Orb36= NGjLN2c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkeyN|g4OSd-MkK3NlM5PzF:L3G+
BxPC-3 NUK4ZlJyTnWwY4Tpc44hSXO|YYm= MnqyNE0yODByIH7N MnH6NlQhcA>? NHPNXmdqdmS3Y3XzJIRwf26{ZXf1cIF1cW:wIH;mJHhKSVBiYX7kJJN2en[rdnnuJIV5eHKnc4Ppc44> M3yzbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{N{KzPFcyLz5{MkeyN|g4OTxxYU6=
RPMI-7951 NXjsdJRsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1ewZWdKPTB;Mz6yJI5O M1K0PFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzN{O3OVAzLz5{MUezO|UxOjxxYU6=
SK-MEL-5 MlS2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfHTVUxRTRwMjDuUS=> NFz2bYw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUezO|UxOid-MkG3N|c2ODJ:L3G+
A375 MnnNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnHTVUxRTZwMzDuUS=> M3OwZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzN{O3OVAzLz5{MUezO|UxOjxxYU6=
SK-MEL-28 NXvicFVST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXHTVUxRTdwNjDuUS=> NIr3XW49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUezO|UxOid-MkG3N|c2ODJ:L3G+
SK-MEL-2 MoGzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTBcGhIUTVyPUGxJI5O NHj4cVU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUezO|UxOid-MkG3N|c2ODJ:L3G+
DB M{jXO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV[0POKhcA>? NVLhcmo6T0l3ME2zMlUhdk1? NVrPOndpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGyN|c2ODhpPkKxNlM4PTB6PD;hQi=>
Pfeiffer M4PRbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVi0POKhcA>? MknDS2k2OD1|Lkmgcm0> NFXXWnA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUKzO|UxQCd-MkGyN|c2ODh:L3G+
SU-DHL-5 NGnwfZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzlOFjDqGh? MWnHTVUxRTBwMkOgcm0> M2DDRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzMkO3OVA5Lz5{MUKzO|UxQDxxYU6=
SU-DHL-8 NFvtTXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\RUoU1QMLiaB?= NHP0SIhIUTVyPUGuOEBvVQ>? MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTJ|N{WwPEc,OjF{M{e1NFg9N2F-
WSU-DLCL-2 NHL3dndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjtcHM1QMLiaB?= M1KyR2dKPTB;MT60JI5O NUPJTW1vRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGyN|c2ODhpPkKxNlM4PTB6PD;hQi=>
A549 M13zbWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MX3Hdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDBOVQ6KGOnbHzzMEBKSzVyPUCuNFE{PM7:TR?= MmP5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh6MUSzO|QoRjJ6OEG0N|c1RC:jPh?=
DU145 M{T3bmN6fG:2b4jpZ4l1gSCjc4PhfS=> NUja[ZNJS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hTFVzNEWgZ4VtdHNiYomgUXRVKGG|c3H5MEBGSzVyPUCuNFE{QM7:TR?= M{DD[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6N{e0OFI3Lz5{OEe3OFQzPjxxYU6=
PC3 MYTDfZRwfG:6aXPpeJkh[XO|YYm= NFzmUnFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBRSzNiY3XscJMh[nliTWTUJIF{e2G7LDDFR|UxRTBwMEmy{txO MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDd5NESyOkc,Ojh5N{S0NlY9N2F-
A549 NULiRpRKTnWwY4Tpc44h[XO|YYm= MVXJcohq[mm2aX;uJI9nKFCDS{GgbY4hcHWvYX6gRVU1QSClZXzsd{whUUN3ME2wMlXPxE1? M3HPU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OEG0N|c1Lz5{OEixOFM4PDxxYU6=
Assay
Methods Test Index PMID
Western blot Survivin / XIAP / Caspase-7 / Caspase-9 / Caspase-3 / Cleaved Caspase-8 / PARP β-catenin / c-Myc / Cyclin D1 / CD44 p-STAT3 / STAT3 26771139 22723871
Immunofluorescence EGFR PARP-1 / PAR 22723871 26090615
Growth inhibition assay Cell viability 29636860
体内研究 YM155按3和10 mg/kg皮下注射前列腺移植瘤,结果显示YM155完全抑制PC-3的肿瘤生长,但是重量没有降低,血细胞数也没有下降。药物动力学分析显示YM155作用于肿瘤组织效果很明显。而且,YM155按5 mg/kg作用于PC-3常位移植瘤时肿瘤抑制率达80% 。[1]YM155和γ-射线联用作用于携带H460或Calu6 移植瘤的裸鼠,显示出强抗癌活性。[2]

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]

  • 启动子-荧光酶素报告实验:

    使用Pyrobest聚合酶和引物5’-GCGCGCTCGAGTCTAGACATGCGGATATATTC-3’和5’-GCGCGAA-GCTTTGGCGGTTAATGGCGCGC-3’, 从人类基因组DNA中分离2767个碱基对序列的人类survivin基因启动子。在pGL3-Basic质粒的XhoI/HindIII切除位点,内切酶XhoI/HindIII切除产生的PCR片段。产生的质粒称为pSUR-luc。通过DNA测序仪在所有增强序列处测定DNA序列。通过荧光酶素实验,使用短暂转染的HeLa-S3细胞,测定pSUR-luc的活力。使用的pGL3质粒含有SV40启动子和增强子序列。 pSUR-luc和pSV2bsr 质粒通过Lipofectamin2000稳定转染到HeLa细胞中。加入10 μg/mL灭瘟素,根据适当的荧光酶素信号和基因稳定性,筛选HeLa-SURP-luc单一群落。pGL3和pSV2bsr质粒稳定转染到CHO细胞中。加入10 μg/mL灭瘟素,根据适当的荧光酶素信号和基因稳定性,筛选CHO-SV40-luc单一群落。从HeLa-SURP-luc和CHO-SV40-luc群落中获得细胞用于化学筛选。细胞按每孔5×103接种在96孔板上,加入YM155(溶于DMSO中)。24小时后测定荧光酶素活性。通过回归分析计算IC50值。

细胞实验:

[1]

  • Cell lines: PC-3, PPC-1, DU145, TSU-Pr1, 22Rv1, SK-MEL-5,和A375细胞
  • Concentrations: ~ 100 nM
  • Incubation Time: 48小时
  • Method:

    PC-3, PPC-1, DU145, TSU-Pr1, 22Rv1, SK-MEL-5,及A375细胞系按5到40×103密度接种在96孔板上。YM155溶解在DMSO中,持续处理细胞48小时。通过sulforhodamine B试剂测定细胞数。

动物实验:

[1]

  • Animal Models: 皮下注射PC-3移植瘤的雄性裸鼠(BALB/c nu/nu)
  • Dosages: 5 mg/kg
  • Administration: 皮下注射,每周持续处理3天,处理3周。

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):
Saline

30 mg/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 443.29
化学式

C20H19BrN4O3

CAS号 781661-94-7
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
NCT01023386 Completed Drug: YM155 Cancer Astellas Pharma Inc November 2009 Phase 1

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

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