YM155 (Sepantronium Bromide)

For research use only. Not for use in humans.

目录号:S1130

YM155 (Sepantronium Bromide) Chemical Structure

CAS No. 781661-94-7

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。

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
RMB 10401.3 现货
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客户使用Selleck生产的YM155 (Sepantronium Bromide)发表文献151篇:

产品安全说明书

Survivin抑制剂选择性比较

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 MljkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVW3NkBp M4HsOmROW09? NXi4UXpnUUN3ME2wMlAxQSEEsTCwMlAxODlizszN M3;tPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NkW5O|MyLz5{NU[1PVc{OTxxYU6=
M-07e Ml;rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorEO|IhcA>? NFjBenRFVVOR NV7jb2JSUUN3ME2wMlA1OCEEsTCwMlAyOyEQvF2= MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTZ3OUezNUc,OjV4NUm3N|E9N2F-
THP-1 M1HqTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYP2SpY5PzJiaB?= NGfJVnpFVVOR M2\YbmlEPTB;MD6wOVEhyrFiMD6wNVMh|ryP MoX5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV4NUm3N|EoRjJ3NkW5O|MyRC:jPh?=
CMK NIXwfZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXNO|IhcA>? MUfEUXNQ NEiwU4FKSzVyPUCuNFU{KMLzIECuNFA6KM7:TR?= NH\wc3c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NU[1PVc{OSd-MkW2OVk4OzF:L3G+
MV4-11 MmT6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\ZfmI4OiCq M2HofWROW09? NWnUe5RUUUN3ME2wMlA2PSEEsTCwMlAzQCEQvF2= MknrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV4NUm3N|EoRjJ3NkW5O|MyRC:jPh?=
AML-193 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXXO|IhcA>? NHrETYpFVVOR MVHJR|UxRTBwNE[yJOKyKDBwME[wJO69VQ>? NH\xcm89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NU[1PVc{OSd-MkW2OVk4OzF:L3G+
HL-60 Ml[wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjFO|IhcA>? MWTEUXNQ MWnJR|UxRTBwMECxJOKyKDBwMECwNkDPxE1? NGO2[I09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NU[1PVc{OSd-MkW2OVk4OzF:L3G+
ML-2 M1;rTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWW3NkBp Mn3iSG1UVw>? MlfCTWM2OD1yLkCwPUDDuSByLkCwNkDPxE1? MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTZ3OUezNUc,OjV4NUm3N|E9N2F-
OCI/AML3 NWLVRmJjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUi3NkBp M3jaWGROW09? M1rz[WlEPTB;MD6wNVEhyrFiMD6wNFIh|ryP MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTZ3OUezNUc,OjV4NUm3N|E9N2F-
HEL NWXGRoNXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV:2XGNGPzJiaB?= M2\3c2ROW09? MXjJR|UxRTBwNUW5JOKyKDBwMEO4JO69VQ>? MnvjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV4NUm3N|EoRjJ3NkW5O|MyRC:jPh?=
ME-1 NEjXUVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYi3NkBp NUjENXhWTE2VTx?= MV3JR|UxRTBwNki0JOKyKDBwMUe5JO69VQ>? MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTZ3OUezNUc,OjV4NUm3N|E9N2F-
THP-1 MV;BdI9xfG:|aYOgRZN{[Xl? MXKxxsDPxE1? M37hd|czKGh? M{HlOWROW09? MlPUbY5lfWOnczDhdI9xfG:|aYO= Mn7pQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV4NUm3N|EoRjJ3NkW5O|MyRC:jPh?=
M-07e NUHQWFFPTnWwY4Tpc44hSXO|YYm= NVrRVoFbOOLCk{JCpO69VQ>? NEHLU|Y4OiCq NYeySIl[TE2VTx?= MkXvbY5lfWOnczDkc5dvemWpdXzheIlwdiCxZjDTeZJ3cX[rbh?= M{T1eVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NkW5O|MyLz5{NU[1PVc{OTxxYU6=
THP-1 NIfxcFVHfW6ldHnvckBCe3OjeR?= Mo[1NQKBmzIEoN88US=> M4q2bVczKGh? MYLEUXNQ MYLpcoR2[2W|IHTve45z\We3bHH0bY9vKG:oIGP1dpZqfmmw NXL4b5RWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW2OVk4OzFpPkK1OlU6PzNzPD;hQi=>
CMK M{\EfmZ2dmO2aX;uJGF{e2G7 NEX0OZYx6oDVMdMg{txO MVy3NkBp MnPrSG1UVw>? MYXpcoR2[2W|IHTve45z\We3bHH0bY9vKG:oIGP1dpZqfmmw MmK5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV4NUm3N|EoRjJ3NkW5O|MyRC:jPh?=
AML-193 NY\QTGxWTnWwY4Tpc44hSXO|YYm= M2e4Z|DjiJNzwrFOwG0> NFfBbFE4OiCq MWHEUXNQ NHKxenJqdmS3Y3XzJIRwf26{ZXf1cIF1cW:wIH;mJHN2en[rdnnu MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTZ3OUezNUc,OjV4NUm3N|E9N2F-
Kasumi-1 NE\CPHNHfW6ldHnvckBCe3OjeR?= MkLNNQKBmzIEoN88US=> MWW3NkBp MlP6SG1UVw>? NHvrOIdqdmS3Y3XzJIRwf26{ZXf1cIF1cW:wIH;mJHN2en[rdnnu M4n3VlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NkW5O|MyLz5{NU[1PVc{OTxxYU6=
MV4-11 MWXGeY5kfGmxbjDBd5NigQ>? MXmw5qCUOcLizszN M{XIPFczKGh? NW\zc5ozTE2VTx?= MWfpcoR2[2W|IHTve45z\We3bHH0bY9vKG:oIGP1dpZqfmmw NVGxNHVtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW2OVk4OzFpPkK1OlU6PzNzPD;hQi=>
MUG-Chor  M3PvR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlzwNE02KM7:TR?= MWSyOE81QCCq NFjkNJZKSzVyPUeuNFXjiImwTTDmc5IhPDiq M3fTdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NkSwNVg2Lz5{NU[0NFE5PTxxYU6=
U-CH1  M1rZUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUi3bYk{OC13IN88US=> M{fVVlI1NzR6IHi= MWfJR|UxRTlwMERihKlvVSCob4KgOFhp MnnRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV4NECxPFUoRjJ3NkSwNVg2RC:jPh?=
KATOIII NH[4V5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvPb2gyOC9{MDDuUS=> MojZOFghcA>? MXzpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NGr1ZXI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NU[zOVA2PSd-MkW2N|UxPTV:L3G+
AGS  NUn0[XJzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFrQfWEyOC9{MDDuUS=> MlX6OFghcA>? Mn;zbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M3TpVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NkO1NFU2Lz5{NU[zOVA2PTxxYU6=
SACC-83 MYrGeY5kfGmxbjDBd5NigQ>? NHfwXY02KG6P MYW0PEBp NHTaUWpl\WO{ZXHz[ZMhdnWlbHXhdkBmgHC{ZYPzbY9vKG:oIFjJSk0y|rF? M3;lVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NEi1OlM2Lz5{NUS4OVY{PTxxYU6=
INA-6 M2LJNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHBNE02ODBibl2= MUm0PEBp M33RW4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M4rzcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mkm2PVc5Lz5{NUK5Olk4QDxxYU6=
U-266 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;pcpQxNTVyMDDuUS=> MW[0PEBp MYjpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NUe1UXRDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyPVY6PzhpPkK1Nlk3QTd6PD;hQi=>
MOLP-8 NH\YXY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NID3bY8xNTVyMDDuUS=> NXPQe|hIPDhiaB?= M3Lz[olvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M12ySVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mkm2PVc5Lz5{NUK5Olk4QDxxYU6=
HG-1 MmjaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7COWFXOC13MECgcm0> M3O4d|Q5KGh? MVfpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ7Nkm3PEc,OjV{OU[5O|g9N2F-
NCI-H929 NETrVpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoP3NE02ODBibl2= NUn2OJl3PDhiaB?= NYTjb|JicW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MoDIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{OU[5O|goRjJ3Mkm2PVc5RC:jPh?=
OPM-2 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvmR2pXOC13MECgcm0> NGqzdXc1QCCq Mo\IbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NVrPbWxERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyPVY6PzhpPkK1Nlk3QTd6PD;hQi=>
L-363 MoXJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXOwMVUxOCCwTR?= NHPvTVY1QCCq M4XSVYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MoK2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{OU[5O|goRjJ3Mkm2PVc5RC:jPh?=
MOLP-2 MmrlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnYW3AxNTVyMDDuUS=> MkjBOFghcA>? MVPpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NU\SWoVFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyPVY6PzhpPkK1Nlk3QTd6PD;hQi=>
KMS-12-BM NFzjcpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7Me4NqOC13MECgcm0> MUG0PEBp Mn21bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MoLIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{OU[5O|goRjJ3Mkm2PVc5RC:jPh?=
SK-MM-2 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DzZ|AuPTByIH7N MkLFOFghcA>? MofibY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ7Nkm3PEc,OjV{OU[5O|g9N2F-
U-266 Mk\kRZBweHSxc3nzJGF{e2G7 MWOwMVUxKG6P MXKyOEBp Mm\pbY5lfWOnczDhdI9xfG:|aYO= M2Lmd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mkm2PVc5Lz5{NUK5Olk4QDxxYU6=
INA-6  NXGybHpQSXCxcITvd4l{KEG|c3H5 NW\sWYYyOC13MDDuUS=> MUCyOEBp NHzyeY5qdmS3Y3XzJIFxd3C2b4Ppdy=> NYjTV3BURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyPVY6PzhpPkK1Nlk3QTd6PD;hQi=>
MCF7 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrsS4M4OiCq MUPJR|UxRTF|INMxJFYhdk1? M{DkU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkKwNlI2Lz5{NUKyNFIzPTxxYU6=
MCF7-TamR6 M{jXV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3Ke|A4OiCq MYHJR|UxRThiwsGgOkBvVQ>? Mn;PQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{MkCyNlUoRjJ3MkKwNlI2RC:jPh?=
MCF7-TamR7 NH3w[HVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fn[FczKGh? NUTIWYh5UUN3ME24JOKyKDNibl2= NHnsXnI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKyNFIzPSd-MkWyNlAzOjV:L3G+
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TC-71 NVzSd|NFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjkU|UxNjFvMUCwNEBvVQ>? MlL2SWM2OD13Lkegcm0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjl4MUe2N{c,OjJ7NkG3OlM9N2F-
SK-ES-1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\qOXcxNjFvMUCwNEBvVQ>? MnzRSWM2OD1{Lkigcm0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NHzzTnQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mkm2NVc3Oyd-MkK5OlE4PjN:L3G+
RD-ES MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHmeXlEOC5zLUGwNFAhdk1? NX\tfFluTUN3ME22MlIhdk1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M3PJUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OU[xO|Y{Lz5{Mkm2NVc3OzxxYU6=
HEK293 NUXKZWozT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUKwMlEuOTByMDDuUS=> MV\FR|UxRTJ|LkCgcm0tKGmwaHnibZR{KGOnbHyg[5Jwf3SqIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NH60V|I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mkm2NVc3Oyd-MkK5OlE4PjN:L3G+
M059J NHv2b45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;mNE02OCCwTR?= NI\CVZo1QCCq MorjbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjd5MEGxNEc,OjJ5N{CxNVA9N2F-
M059K M3TFUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHVeFcxNTVyIH7N Mn6yOFghcA>? NFHvSGxqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NYPrcodtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK3O|AyOTBpPkKyO|cxOTFyPD;hQi=>
M059J M{T6WGFxd3C2b4Ppd{BCe3OjeR?= NHHkSWo{OCCwTR?= MofQNlQhcA>? NF7jNINqdmS3Y3XzJIFxd3C2b4Ppdy=> NYS3Uok3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK3O|AyOTBpPkKyO|cxOTFyPD;hQi=>
M059K Ml\IRZBweHSxc3nzJGF{e2G7 NUTRelNLOzBibl2= NXi1S5BVOjRiaB?= M3SwfYlv\HWlZYOgZZBweHSxc3nz NYLFbXVSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK3O|AyOTBpPkKyO|cxOTFyPD;hQi=>
PANC-1 M4nKTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXHNE4xOS1zMECwJI5O NVvBTHR3PDhiaB?= MXXJR|UxRTNwNkmgcm0> NYrpeGFSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK3NlM5PzFpPkKyO|I{QDdzPD;hQi=>
MIAPaCa-2 NWnpXW1sT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\TeZoxNjBzLUGwNFAhdk1? Mn7aOFghcA>? MmLlTWM2OD1{OT6zOkBvVQ>? NHrnPGs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkeyN|g4OSd-MkK3NlM5PzF:L3G+
BxPC-3 NWHzPXFUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX6wMlAyNTFyMECgcm0> M37DSVQ5KGh? MlnoTWM2OD1|MD6yOkBvVQ>? Ml\iQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ5MkO4O|EoRjJ{N{KzPFcyRC:jPh?=
PANC-1 NUXobYZtTnWwY4Tpc44hSXO|YYm= MVuwMVExODBibl2= MmnONlQhcA>? NUjFZVNicW6mdXPld{Bld3ewcnXneYxifGmxbjDv[kBZUUGSIHHu[EB{fXK4aY\pckBmgHC{ZYPzbY9v MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjd{M{i3NUc,OjJ5MkO4O|E9N2F-
MIAPaCa-2 MVHGeY5kfGmxbjDBd5NigQ>? NEDhPYExNTFyMECgcm0> NHLVcIczPCCq MorkbY5lfWOnczDkc5dvemWpdXzheIlwdiCxZjDYTWFRKGGwZDDzeZJ3cX[rbjDlfJBz\XO|aX;u NYXkbZh1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK3NlM5PzFpPkKyO|I{QDdzPD;hQi=>
BxPC-3 NGC2TnFHfW6ldHnvckBCe3OjeR?= MlTVNE0yODByIH7N M3HpRlI1KGh? MkHIbY5lfWOnczDkc5dvemWpdXzheIlwdiCxZjDYTWFRKGGwZDDzeZJ3cX[rbjDlfJBz\XO|aX;u NFnL[|Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkeyN|g4OSd-MkK3NlM5PzF:L3G+
RPMI-7951 NXLTfXhyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fIcGdKPTB;Mz6yJI5O NInyT209[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUezO|UxOid-MkG3N|c2ODJ:L3G+
SK-MEL-5 NIO1UJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{PNdWdKPTB;ND6yJI5O M{XNOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzN{O3OVAzLz5{MUezO|UxOjxxYU6=
A375 NWfhXlVQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDHTVUxRTZwMzDuUS=> MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTd|N{WwNkc,OjF5M{e1NFI9N2F-
SK-MEL-28 M4TjeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\HTVUxRTdwNjDuUS=> MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTd|N{WwNkc,OjF5M{e1NFI9N2F-
SK-MEL-2 MnvBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\4fZNrT0l3ME2xNUBvVQ>? MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTd|N{WwNkc,OjF5M{e1NFI9N2F-
DB M3rSSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2foZlQ5yqCq NFfHb4FIUTVyPUOuOUBvVQ>? M1r4cFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzMkO3OVA5Lz5{MUKzO|UxQDxxYU6=
Pfeiffer MkfES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4O4PVQ5yqCq M3n5cWdKPTB;Mz65JI5O M1qzUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzMkO3OVA5Lz5{MUKzO|UxQDxxYU6=
SU-DHL-5 M1P0PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{TvUVQ5yqCq NVrRcJc2T0l3ME2wMlI{KG6P NHjZPZg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUKzO|UxQCd-MkGyN|c2ODh:L3G+
SU-DHL-8 MnTnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7uXm41QMLiaB?= NVPMb|JoT0l3ME2xMlQhdk1? MmLsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF{M{e1NFgoRjJzMkO3OVA5RC:jPh?=
WSU-DLCL-2 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HJNVQ5yqCq Mly3S2k2OD1zLkSgcm0> NHrRNYM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUKzO|UxQCd-MkGyN|c2ODh:L3G+
A549 MWLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUjHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDBOVQ6KGOnbHzzMEBKSzVyPUCuNFE{PM7:TR?= MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDhzNEO3OEc,Ojh6MUSzO|Q9N2F-
DU145 MYfDfZRwfG:6aXPpeJkh[XO|YYm= NH7iSWNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBFXTF2NTDj[YxteyCkeTDNWHQh[XO|YYmsJGVEPTB;MD6wNVM5|ryP MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDd5NESyOkc,Ojh5N{S0NlY9N2F-
PC3 NXjVclBvS3m2b4TvfIlkcXS7IHHzd4F6 NVvNRY9[S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWEN|IHPlcIx{KGK7IF3UWEBie3OjeTygSWM2OD1yLkC5Nu69VQ>? MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDd5NESyOkc,Ojh5N{S0NlY9N2F-
A549 M33UOmZ2dmO2aX;uJIF{e2G7 M1jpV2lvcGmkaYTpc44hd2ZiUFHLNUBqdiCqdX3hckBCPTR7IHPlcIx{NCCLQ{WwQVAvPc7:TR?= M135ZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OEG0N|c1Lz5{OEixOFM4PDxxYU6=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
Survivin / XIAP / Caspase-7 / Caspase-9 / Caspase-3 / Cleaved Caspase-8 / PARP; 

PubMed: 26771139     


YM155 treatment decreased survivin expression without affecting XIAP and induced cleavage of caspases. Protein expression (caspase-3, -7, -9, -8, PARP) was detected by Western Blot analysis. 

β-catenin / c-Myc / Cyclin D1 / CD44 ; 

PubMed: 26771139     


YM155 inhibited expression of CSC molecules. SGC-7901 cells were treated with YM155 at indicated doses for 24 hours. The protein levels of genes were determined by Western Blot.

p-STAT3 / STAT3 ; 

PubMed: 22723871     


Levels of phosphorylated STAT3 and expression of survivin were analyzed by Western blotting after a 24-hours treatment with YM155 and 48 hours after transfection of 40 nM siRNA.

26771139 22723871
Immunofluorescence
EGFR; 

PubMed: 22723871     


YM155 (10 nM) induced the nuclear EGFR accumulation. PANC-1 cells were stained with anti-EGFR, anti-Alexa Fluor 488, and DAPI after the YM155 treatment. Scale bars: 10 µm.

PARP-1 / PAR ; 

PubMed: 26090615     


A. Nuclear accumulation of active PARP-1 in KYSE410 cells after 12 h of YM155 treatment was evaluated using immunofluorescent analysis. Nuclei were stained with DAPI, as shown in blue. Scale bars: 10 μm. C. Accumulation of the poly-ADP polymer in KYSE410 was evaluated using immunofluorescent analysis after YM155 treatment for 12 h. Nuclei were stained with DAPI, as shown in blue. Scale bars: 10 μm. 

22723871 26090615
Growth inhibition assay
Cell viability; 

PubMed: 29636860     


Cells were grown in 96-well plates for 24 h and treated with the indicated concentrations of YM155 or docetaxel for 72 h, and cell survival was determined by MTT assay.

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]

- 合并

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]

- 合并
  • 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。


    (Only for Reference)
动物实验:

[1]

- 合并
  • 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。
    (Only for Reference)

溶解度 (25°C)

体外 Water 89 mg/mL (200.77 mM)
DMSO 55 mg/mL (124.07 mM)
Ethanol 6 mg/mL (13.53 mM)
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 粉状
溶于溶剂
别名 N/A

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
NCT01023386 Completed Drug: YM155 Cancer Astellas Pharma Inc November 2009 Phase 1

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操作手册

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID