Silmitasertib (CX-4945)

目录号:S2248

Silmitasertib (CX-4945) Chemical Structure

Molecular Weight(MW): 349.77

Silmitasertib (CX-4945)是有效的,选择性CK2(casein kinase 2)抑制剂,无细胞试验中IC50为1 nM,对 Flt3, Pim1 和 CDK1作用效果稍弱(细胞试验中没有活性)。Phase 1/2。

规格 价格 库存 购买数量  
RMB 2381.77 现货
RMB 1418.29 现货
RMB 2604.97 现货
有超大折扣

今日订购,明日送达,全国免运费!

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

客户使用该产品的6个实验数据:

  • Nat Commun 2014 5, 3393. Silmitasertib (CX-4945) purchased from Selleck.

    (E) Pretreatment with CX4945 blocks TNF-induced phosphorylation of BRMS1. H157 cells were pretreated with CX4945 (30 µM) for 2 h, followed by stimulation with TNF (20 ng/mL) for an additional 1 h. Immunofluorescence assays were performed using antibodies against BRMS1 (pS30) (red)/CK2α' (green)/DAPI (blue).

    Cancer Res, 2016, 76(9):2675-86. Silmitasertib (CX-4945) purchased from Selleck.

  • Immunofluorescence analysis for Ser536 p-NF-κB cellular localization of RS4;11cells treated with CX-4945 (5 μM) and bortezomib (2.5 nM) either alone or in combination. Cells were treated, collected at 22 h and reacted with an antibody to Ser536 p-NF-κB which was revealed by a Cy3-conjugated secondary antibody. DAPI was used to label nuclei.

    Oncotarget, 2015, 51: S659-S660. Silmitasertib (CX-4945) purchased from Selleck.

    Cell Signal 2014 26(7), 1567-75. Silmitasertib (CX-4945) purchased from Selleck.

  • Cell Signal 2014 26(7), 1567-75. Silmitasertib (CX-4945) purchased from Selleck.

    (B and C) Jurkat cells were pretreated for 2 h with DES (3 μM) and CX-4945 (10 μM) individually or in combination, and were then treated with PMA (50 ng/mL) plus PHA (1 μg/mL) for 6 and 24 h. IL-2 mRNA expression was detected by qRT-PCR analysis (B) and the amounts of secreted IL-2 in the culture medium were measured by ELISA (C). #p < .01 (vs. the PMA/PHA, DES, and CX-4945 untreated cell population); *p < .01; **p < .001 (vs. the cell population treated with only PMA/PHA).

    Biomed Pharmacother, 2018, 98:357-363. Silmitasertib (CX-4945) purchased from Selleck.

产品安全说明书

Casein Kinase抑制剂选择性比较

生物活性

产品描述 Silmitasertib (CX-4945)是有效的,选择性CK2(casein kinase 2)抑制剂,无细胞试验中IC50为1 nM,对 Flt3, Pim1 和 CDK1作用效果稍弱(细胞试验中没有活性)。Phase 1/2。
特性 CX-4945是促进人类临床实验的CK2的第一个口服生物相容性小分子抑制剂。
靶点
CK2 [1]
(Cell-free assay)
1 nM
体外研究

CX-4945是CK2特异的抑制剂,它只抑制238种激酶中的7种并且在0.5 μM浓度时它的抑制率超过90%,这是CK2的IC50的500多倍。虽然在无细胞系统中CX-4945抑制FLT3, PIM1和CDK1的IC50分别为35 nM, 46 nM和56 nM,但是在细胞基础上的功能实验中10 μM的CX-4945对FLT3, PIM1和 CDK1抑制作用不强。CX-4945有广谱的抗恶性细胞增生活性。乳腺癌细胞系对CX-4945敏感性最广泛,其EC50为1.71-20.01 μM。CX-4945的抗恶性细胞增生活性与CK2α mRNA和蛋白水平对应,但是与CK2α'催化亚基、调整CK2β亚族和PI3K/Akt 或 PTEN突变状态无关。CX-4945通过抑制CK2直接阻断Akt第129位丝氨酸的磷酸化作用来抑制PI3K/Akt信号通路,而不是通过抑制激活的PTEN起作用。用CX-4945处理可以引起磷酸化p21 (T145)减少,而p21和p27整体水平则会升高,同时诱导caspase 3/7活性。用CX-4945处理会诱导BT-474细胞阻断在细胞周期的G2/M期和BxPC-3细胞阻断在G1期。CX-4945会抑制HUVEC的增殖、迁移及血管新生,其IC50分别是5.5 μM, 2 μM和4 μM。在含氧量低的情况下BT-474和BxPC-3细胞用CX-4945处理,能阻断p53和pVHL下调,降低HIF-1α的转录活性[1]。在Jurkat细胞中CX-4945能有效抑制内源细胞内的内源CK2的活性,其IC50是0.1 μM [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
platelets NYe1WIJnU2mwYYPlJGF{e2G7 MYixM|UwOTBizszN NWO3NpA1OC53IHi= NEn4copFVVOR M1[5RZJm\HWlZYOgR2szKGurbnHz[UBi[3Srdnn0fUBidmRicHzheIVt\XRiYXfndoVo[XSrb36= M{PSflI3OzhzNEO3
HDMEC MUjLbY5ie2ViQYPzZZk> M3rt[FAvOjVxMD61M|Eh|ryP MlHpNlQhcA>? MYPEUXNQ MnTHdoVlfWOnczDDT|Ihc2mwYYPlJIFkfGm4aYT5MEB3X0ZiZYjwdoV{e2mxbjDhcoQhe2WlcnX0bY9v NF[2PIwzPjN6MUSzOy=>
HDMEC NUjaWYNsTnWwY4Tpc44hSXO|YYm= NFfsRW4xNjJ3L{CuOU8yKM7:TR?= MWGyOEBp M3;6SGROW09? MlvsdoVlfWOnczDlfJBz\XO|aX;uJI9nKF[FQV2tNUBjfXRibn;0JGlESU1vMR?= MXWyOlM5OTR|Nx?=
HDMEC MX\GeY5kfGmxbjDBd5NigQ>? MkPnNUDPxE1? NUPpb4hROjRiaB?= Ml3tSG1UVw>? NYLTNWJI[W[oZXP0d{B{fWKlZXzseYxieiCub3PhcIl7[XSrb36gc4YhVk[DVHOxJIFv\CCyaH;zdIhwNXB4NR?= MV:yOlM5OTR|Nx?=
A549  M2XvbWZ2dmO2aX;uJGF{e2G7 NHj4NXQ{NzFywrFOwG0> M{fFcFQ5KGh? NGHaUIp{fXCycnXzd4V{KHSqZTDtbYNzd3CrbHzhdk1qdmS3Y3XkJIV5eHKnc4Ppc44hd2ZicD3GRWs> MkPWNlY{OTh6MEC=
HDMEC NUPZT404U2mwYYPlJGF{e2G7 MUGxMVUxKM7:TR?= Mn\WOUBp M2rSZWROW09? M3\yWoRm[3KnYYPld{BEUzJia3nuZZNmKGGldHn2bZR6KHerdHjveZQh[W[oZXP0bY5oKGOnbHygeoli[mmuaYT5 M3zWU|I3OTh7NUi2
HDMEC MknmSpVv[3Srb36gRZN{[Xl? MV[1NEDPxE1? NVXNUIxYOS93IHi= NIqzOppFVVOR NF\CXoxl\WO{ZXHz[ZMhfGinIH71Z4xm[XJic3nncoFtKG:oIIDoc5NxcG:{eXzheIVlKHB4NTDpckBVVkZvzsGtd5RqdXWuYYTl[EBJTE2HQ9Mg MoG5NlYyQDl3OE[=
HEK293 M{POPGtqdmG|ZTDBd5NigQ>? MVuwMlXDqM7:TR?= Mof3NVUhdWmw NHm0TY9FVVOR M{O2TJJm\HWlZYOgR2szKGurbnHz[UBi[3Srdnn0fS=> NGKyeYMzPTh6N{[yOi=>
Hela MX\LbY5ie2ViQYPzZZk> M33yVlAvPcLizszN NEn5W5AyPSCvaX6= NX[x[oNCTE2VTx?= MlLDdoVlfWOnczDDT|Ihc2mwYYPlJIFkfGm4aYT5 Mk\HNlU5QDd4Mk[=
LAMA84 Mo\NT4lv[XOnIFHzd4F6 MUCwMlXDqM7:TR?= NXjETYdGOTVibXnu MoXoSG1UVw>? NWjkSnJMemWmdXPld{BEUzJia3nuZZNmKGGldHn2bZR6 NX\Ec2lxOjV6OEe2NlY>
HEK293 NFXwWnZHfW6ldHnvckBCe3OjeR?= MUmzJO69VQ>? NFfrWGM2KGh? M1;lRWROW09? M2fzdGNMOiCyaH;zdIhwenmuYYTld{BmUUZ|ajDheEBU\XJzMke= M4\XS|I2QDh5NkK2
UM-SCC1 NFPRcphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYSwMlEuOzBizszN NEmx[GkyNTViZB?= MnXzTWM2OD12LkGg{txO MYOyOVc6QDB4MR?=
UM-SCC46 MnzIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3XqTFAvOS1|MDFOwG0> MYexMVUh\A>? MnLjTWM2OD1|LkSg{txO M{HpU|I2Pzl6ME[x
UM-SCC1 MmHmSpVv[3Srb36gRZN{[Xl? NX\MSoNEOC53L{SvNVAh|ryP MXu3NkBp NW\6dWZE\G:5bj3y[Yd2dGG2ZYOgeIhmKGW6cILld5Nqd25ib3[gUmYuzLiELDDCZ4wuYExiYX7kJJVxNXKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCyNUOsJJAzOSxiQWCtNUBidmRiSVytPEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 MX2yOVc6QDB4MR?=
UM-SCC46 NF;CRZBHfW6ldHnvckBCe3OjeR?= M3KzTlAvPS92L{GwJO69VQ>? MkKzO|IhcA>? MnXN[I94di2{ZXf1cIF1\XNidHjlJIV5eHKnc4Ppc44hd2ZiTl[tyNhDNCCEY3ytXGwtKHB3MzygdFIyNCCDUD2xJIFv\CC3cD3y[Yd2dGG2ZYOgeIhmKGW6cILld5Nqd25iSVytPEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 NHXaNXMzPTd7OEC2NS=>
NU-DUL MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmHnOU0zPSEQvF2= Mn7kOFghcA>? MYHpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 NITHfHIzPTd6OEK2PS=>
Oci Ly 3 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1n5WFUuOjVizszN MVe0PEBp Mn6wbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> NEfSR2ozPTd6OEK2PS=>
Oci Ly 10 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknJOU0zPSEQvF2= NYjs[Yt6PDhiaB?= NVvE[XYxcW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? MXyyOVc5QDJ4OR?=
Oci Ly 1 NHPa[4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYKxPYlyPS1{NTFOwG0> NFnOXWc1QCCq MnjmbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> NIKzUIwzPTd6OEK2PS=>
Oci Ly 18 M4XOeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVG1MVI2KM7:TR?= M1\MO|Q5KGh? NIjqcopqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NXn3T2FIOjV5OEiyOlk>
Oci Ly 19  MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLIOU0zPSEQvF2= MkfCOFghcA>? NHnmNGJqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NHPET|EzPTd6OEK2PS=>
Raji MkT4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljVOU0zPSEQvF2= MXW0PEBp MnrrbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> NHq1O4UzPTd6OEK2PS=>
H1299 MkH5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVKxM|UwOTBizszN MYK3NkBp MWrpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 MVqyOVc2ODNyOB?=
Calu-1  NYLDZ2F2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7oVZMyNzVxMUCg{txO NW\SS3p6PzJiaB?= M4qyPYlvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> MkLhNlU4PTB|MEi=
H358 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVexM|UwOTBizszN M4PhU|czKGh? NXHjU5lrcW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? MnjWNlU4PTB|MEi=
H1299 Ml61RZBweHSxc3nzJGF{e2G7 NYPhPY1jOTBizszN Mon5O|IhcA>? Ml;MbY5lfWOnczDhdI9xfG:|aYO= NEHDb5kzPTd3MEOwPC=>
Calu-1  MW\BdI9xfG:|aYOgRZN{[Xl? NV7hd3FrOTBizszN M4DI[|czKGh? MmDwbY5lfWOnczDhdI9xfG:|aYO= NWfUTY84OjV5NUCzNFg>
H358 NX;wOnVwSXCxcITvd4l{KEG|c3H5 NX3QeoVkOTBizszN MkDtO|IhcA>? MkTKbY5lfWOnczDhdI9xfG:|aYO= MojINlU4PTB|MEi=
PC9/GR NGL3cpdHfW6ldHnvckBCe3OjeR?= Mk\EOUDDvU1? MXq0PEBp NIrPeJhqdmS3Y3XzJIF2fG:yaHHnfS=> MUGyOVQ5PjRyOR?=
PC9/ER NGHhPFdHfW6ldHnvckBCe3OjeR?= NIr2TXg2KML3TR?= MWO0PEBp MXfpcoR2[2W|IHH1eI9xcGGpeR?= Mlu0NlU1QDZ2MEm=
H28 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknONE4xOS1|MDFOwG0> MXK3NkBp M1jEfWROW09? MmfJTWM2OD15LkKg{txO MoHwNlU1OjJyOEG=
H2052 MljmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1y0WlAvODFvM{Cg{txO NEXSZ|g4OiCq NXm0U|VYTE2VTx?= MlXtTWM2OD1{LkCg{txO MYOyOVQzOjB6MR?=
UM-SCC-1 MXvDcI9vd2enbnnjJGF{e2G7 MlTSNE42NTVizszN MYKxOEBl M1uwemROW09? Ml3YxsBqdmirYnn0d{BkdG:wb3flcolkKHO3co\peoFtKGGwZDDzdIhmemViZn;ycYF1cW:w M{LreVI2Ozd7MEG2
UM-SCC-46 NX7oNVhFS2yxbn;n[Y5q[yCDc4PhfS=> MViwMlUuPSEQvF2= NUnpXW9QOTRiZB?= MnyySG1UVw>? MnzLxsBqdmirYnn0d{BkdG:wb3flcolkKHO3co\peoFtKGGwZDDzdIhmemViZn;ycYF1cW:w NYW0cnU5OjV|N{mwNVY>
U87-MG Mn25S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnSNU82NzFyIN88US=> M1rVVVI1NzR6L{eyJIg> NVPGVopvTE2VTx?= MYTpcohq[mm2czDj[YxtKGe{b4f0bEBjd3SqIHPvcoNmdnS{YYTpc44h[W6mIITpcYUh\GWyZX7k[Y51dHl? NXy5UFRCOjV{NEG4PVc>
MDA-MB-231 NV;0ZXJVTnWwY4Tpc44hSXO|YYm= NHHDNlkzNzVxMUCg{txO NXH2[WJiPCCq NVzPS4NT\GWlcnXhd4V{KHSqZTDjc45{fGm2dYTpeoUheGixc4Doc5J6dGG2aX;uJI9nKGKxdHigJJAuWzV{OT3wOlUh[W6mIICtV|EzQS2Da4S= MnrlNlUyPTN5MkW=
MDA-MB-231 MlPtSpVv[3Srb36gRZN{[Xl? NYO3VZFXOi93L{GwJO69VQ>? Ml;nOEBp NVXCWXpKcW6qaXLpeJMhe2W{aX7lJFUzQSCyaH;zdIhwenmuYYTpc44h[W6mIITo[UBmgHC{ZYPzbY9vKG:oIFnMMVYtKEmOLUi= NFT1bJAzPTF3M{eyOS=>
ARPE-19 MVnLbY5ie2ViQYPzZZk> NID3XFg2NzFyL{KwJO69VQ>? MoniNlQwPDhiaB?= MXzpcohq[mm2czDDT|Ihc2mwYYPlJIFkfGm4aYT5JIF1KGFiY3;uZ4VvfHKjdHnvckBw\iB3wrFOwG0> MlqwNlQ3QDZyOEC=
ARPE-19 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLvOVN[OTBizszN NV;vNYFLOjRvOU[gbC=> MlfLSG1UVw>? NXHid5o1cW6qaXLpeJMh[2WubDDndo94fGhidHnt[UBl\XCnbnTlcpRtgQ>? MVGyOFY5PjB6MB?=
HCT116  MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY[xNEDPxE1? NV;6OFFYOjRvOU[gbC=> M1TTbGROW09? MYHpcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 MmXRNlQ3QDZyOEC=
ARPE-19 MkXXSpVv[3Srb36gRZN{[Xl? NUDFVnEyOTBizszN MkLYOEBp NXjJWJA6TE2VTx?= NH62R2Jk[XW|ZYOgSXIue3S{ZYPzJJJme3CxboPlJI93\XJidHjlJJAu\UmIMt8xJIJz[W6laDygZpV1KGSxZYOgco91KGmwZIXj[UBEUE:SwrC= Ml20NlQ3QDZyOEC=
HCT116  MnvESpVv[3Srb36gRZN{[Xl? NVPQSWMxOTBizszN NWTNZmI1PCCq M4DDWmROW09? MlTWZ4F2e2W|IFXSMZN1emW|czDy[ZNxd26|ZTDveoVzKHSqZTDwMYVKTjMQsTDidoFv[2huIHL1eEBld2W|IH7veEBqdmS3Y3WgR2hQWMLi MWWyOFY5PjB6MB?=
HCT116  MVvBdI9xfG:|aYOgRZN{[Xl? MlXxNVAh|ryP MoG2NlQwPDhiaB?= NWDnOWV6TE2VTx?= MXXpcoR2[2W|IHHwc5B1d3Orcx?= MUiyOFY5PjB6MB?=
Nalm6  NX3V[IF[TnWwY4Tpc44hSXO|YYm= MU[xNE8zOCEQvF2= NWjkOVEyOjRiaB?= NGXZbllz\XO3bITzJIlvKGSnY4LlZZNm\CCSVFXOJJBpd3OyaH;yfYxifGmxbjDheEB1cGViQ1uyJJRiemendDDy[ZNq\HWnIGOzPFAh[W6mIHPvcoNwdWm2YX70JIRwf26{ZXf1cIF1cW:wIH;mJHBVTU5icILveIVqdiCneIDy[ZN{cW:w MY[yOFU3OTd7Mh?=
SUP-B15 MmGxSpVv[3Srb36gRZN{[Xl? M3\1OlExNzJyIN88US=> NGLOXZozPCCq NWD4R2xIemW|dXz0d{BqdiCmZXPy[YF{\WRiUGTFUkBxcG:|cHjvdplt[XSrb36gZZQhfGinIFPLNkB1[XKpZYSgdoV{cWS3ZTDTN|gxKGGwZDDjc45kd22rdHHueEBld3ewcnXneYxifGmxbjDv[kBRXEWQIIDyc5RmcW5iZYjwdoV{e2mxbh?= MnvYNlQ2PjF5OUK=
Nalm6  M4PmVGFxd3C2b4Ppd{BCe3OjeR?= MV:2M|ExKM7:TR?= MX60PEBp M2\WPYlv\HWlZYOgZZBweHSxc3nz NFT4d2QzPDV4MUe5Ni=>
SUP-B15 NVzWdmpLSXCxcITvd4l{KEG|c3H5 NFTafZU3NzFyIN88US=> NH;5dII1QCCq NFjpV49qdmS3Y3XzJIFxd3C2b4Ppdy=> M3fsb|I1PTZzN{my
C2C12 MVzGeY5kfGmxbjDBd5NigQ>? Mo\PN{DPxE1? M4rY[|EzNzJ2L{S4JIg> MUHpcohq[mm2czD0bIUh\XiycnXzd4lwdiCxZjDvd5Rmd2OuYYP0JIRq\m[ncnXueIlifGmxbjDtZZJs\XK|IHHu[EBCc3RicHjvd5Bpd3K7bHH0bY9v Mn\iNlQzQTNyMUG=
Jurkat MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LjOFEuOTBizszN NH3LOnQ1QCCq M2X6UWlEPTB;ND65JO69VQ>? NGHWPZYzPDJ3M{CyOC=>
CEM-R MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1T2UFEuOTBizszN M2X5WVQ5KGh? NFj1PVFKSzVyPUSg{txO NWPRWWMxOjR{NUOwNlQ>
CEM-S M4\iUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfSelEyNTFyIN88US=> NEnJc201QCCq NGjlXYRKSzVyPUSuOkDPxE1? MUWyOFI2OzB{NB?=
MOLT-4 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3OydFEuOTBizszN MXK0PEBp MnTmTWM2OD13Lkeg{txO NWjDPFFsOjR{NUOwNlQ>
PF-382 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGKybnUyNTFyIN88US=> MWW0PEBp MlzlTWM2OD12LkWg{txO MVeyOFI2OzB{NB?=
ALL-SIL NEnRbVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVuxMVExKM7:TR?= NHnUUI01QCCq M3vqe2lEPTB;NT63JO69VQ>? NVX3N5BUOjR{NUOwNlQ>
HPB-ALL MlTWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHJO3gyNTFyIN88US=> MV:0PEBp M2j1OWlEPTB;Nj6xJO69VQ>? MYiyOFI2OzB{NB?=
DND-41 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVT6ZW9wOS1zMDFOwG0> M2fVNFQ5KGh? M2e4fmlEPTB;OTFOwG0> MlzkNlQzPTNyMkS=
ALL-SIL M2PDb2Fxd3C2b4Ppd{BCe3OjeR?= M{PFeFUh|ryP MV6yOE81QCCq Ml3SbY5lfWOnczDhdI9xfG:|aYO= M1fWWlI1OjV|MEK0
DND-41 NUSzUIU2SXCxcITvd4l{KEG|c3H5 Ml2yOUDPxE1? MoXXNlQwPDhiaB?= NHrQT2ZqdmS3Y3XzJIFxd3C2b4Ppdy=> MoSwNlQzPTNyMkS=
MOLT-4 NYTod5BrSXCxcITvd4l{KEG|c3H5 NHntVlY2KM7:TR?= NX23NWdzOjRxNEigbC=> M13Meolv\HWlZYOgZZBweHSxc3nz NF7ZPI8zPDJ3M{CyOC=>
U-266 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX6wMVQxKM7:TR?= NXnqbmhvPDhiaB?= NYDx[GlXUUN3ME2xPU45KML3TdMg NIjwVFQzPDB6NkS5OC=>
INA-6 NVTaOFdqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWOwMVQxKM7:TR?= NVzKXGZ7PDhiaB?= Mlr1TWM2OD1{LkSyJOK2VQ>? NUfZUHh3OjRyOE[0PVQ>
Jeko-1 MoDrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\uTnVzOC12MDFOwG0> MWm0PEBp M{TiN2lEPTB;Mj60JOK2VcLi MnPsNlQxQDZ2OUS=
Rec-1 M3;Q[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zxclAuPDBizszN MlnIOFghcA>? MXzJR|UxRTFwNE[gxtVOyqB? M2nQOFI1ODh4NEm0
A549 M2CzfmZ2dmO2aX;uJGF{e2G7 MoTPNVAh|ryP MmjKNVIwOjRxNEigbC=> NGH1TnRqdmirYnn0d{BVT0ZvzsKxMYlv\HWlZXSgcYloemG2aX;uJIFv\CCrbo\hd4lwdg>? NIjCO2YzPDB{M{mzPC=>
A549 NYTXWohuTnWwY4Tpc44hSXO|YYm= NV3hXYRyOyEQvF2= M2fPZlQ5KGh? NWPHZXRDcW6qaXLpeJMhXEeILd8yNU1qdmS3Y3XkJIFkfGm4YYTpc44hd2ZiU33h[EBidmRiZYjwdoV{e2mxbjDv[kBUdmGrbDDhcoQhXHerc4S= NYTpRYZSOjRyMkO5N|g>
S-LAMA84 NIHVS4ZHfW6ldHnvckBCe3OjeR?= M3;ReFPDqM7:TR?= NGPtPIwzPCCq MlqwSG1UVw>? MmXrdoVlfWOnczDDT|Ih[WO2aY\peJk> NF\CO2kzPDBzMkGwPS=>
R-LAMA84 MkHKSpVv[3Srb36gRZN{[Xl? NHvJSFA{yqEQvF2= NGj0ZW4zPCCq NYLm[JZmTE2VTx?= NXPu[|NxemWmdXPld{BEUzJiYXP0bZZqfHl? MmfTNlQxOTJzMEm=
S-LAMA84 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUCyMlUuOTBizszN NU\kNVY{PDhiaB?= M{TnSGROW09? MWHpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 NEP2XYMzPDBzMkGwPS=>
R-LAMA84 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1XPflIvPS1zMDFOwG0> NHPNTm01QCCq Mn;ISG1UVw>? M17BcIlvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> Mn:2NlQxOTJzMEm=
A549 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HkeVAuOzBizszN NVLLPFMyPzJiaB?= M4noSGROW09? NGPJPFdKSzVyPUSuNVUh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 NXXXdlJ[OjN4NUG0OFM>
H1299 M2nVWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4iyRlAuOzBizszN Mo\zO|IhcA>? MmK3SG1UVw>? NF;a[oRKSzVyPUGuPFAh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 NEDsSIszOzZ3MUS0Ny=>
A549 MXjGeY5kfGmxbjDBd5NigQ>? MoexNU8yOCEQvF2= MoflOFghcA>? M1y1RWROW09? NWjLNosxdGWjZIOgeI8h[SCmb4PlMYRmeGWwZHXueEBl\WO{ZXHz[UBqdiCQb4TjbEBz\XCxcoTldkBi[3Srdnn0fS=> MW[yN|Y2OTR2Mx?=
LNCap MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI[zbY8xNTNyIN88US=> NF7rVHg1KGR? M2HseWlEPTB;ND61PeKh|ryP M4\TfFIzQDN{M{G2
A431  MmnsSpVv[3Srb36gRZN{[Xl? NIfBdIQyOCEQvF2= M1HOTFMxKG2rbh?= MkjyZZR1\W63YYTld{BRUTONLVHreE1uXE:UIIPp[45idGmwZx?= NVfPd|lROjJ|OEe5PFg>
H2170  MWrGeY5kfGmxbjDBd5NigQ>? Mnf0NVAh|ryP NGe2bXE{OCCvaX6= MlHiZZR1\W63YYTld{BRUTONLVHreE1uXE:UIIPp[45idGmwZx?= NXHGe4pWOjJ|OEe5PFg>
A431  MXPGeY5kfGmxbjDBd5NigQ>? MUmxNEDPxE1? NV7hdmZsPC1{NDDo MVPlcohidmOnczDhdI9xfG:|aYOge4l1cCCncnzveIlvcWJ? M2jLVlIzOzh5OUi4
H2170  Ml;LSpVv[3Srb36gRZN{[Xl? M{j0NVExKM7:TR?= M176elQuOjRiaB?= MXLlcohidmOnczDhdI9xfG:|aYOge4l1cCCncnzveIlvcWJ? MVWyNlM5Pzl6OB?=

... Click to View More Cell Line Experimental Data

体内研究 在BT-474模型中,一天两次口服25 mg/kg或75 mg/kg的CX-4945,具有强效的抗癌活性,TGI分别为88% 和97%,每组实验动物9只中有2只其肿瘤的体积大小比初期的要减少50%。在BxPC-3模型中,一天两次用75 mg/kg的CX-4945处理,TGI为93%,在治疗期结束时,有3只动物没发现还有残留的肿瘤[1]。在PC3异种移植的模型中,用25 mg/kg, 50 mg/kg或 75 mg/kg的CX-4945处理,能抑制肿瘤生长,TGI分别为19%, 40%和86%[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:[2]
+ 展开

CK2激酶实验:

将10 μL稀释缓冲液(ADB; 20 mM MOPS, pH 7.2, 25 mM β-磷酸甘油, 5 mM EGTA, 1 mM原钒酸钠和 1 mM 二硫苏糖醇),10 μL多肽底物(RRRDDDSDDD, 溶于ADB,浓度1mM)和10 μL重组的人源CK2(ααββ-全酶, 25 ng溶于ADB)混合,加入10 μL CX-4945。加入10μLATP溶液(90% 75 mM MgCl 2, 75 μM ATP (终浓度15 μM)溶于ADB; 10% [γ-33P]ATP (储存1 mCi/100 μL; 3000 Ci/mM起始反应,30 ℃反应10分钟。用100 μL的0.75%的磷酸终止反应,然后转移到磷酸纤维素滤板上过滤。每个孔用0.75%磷酸洗5次,真空抽干5分钟,再每孔加入15 μL闪烁液,然后用Wallac荧光计数器检测残留的放射性。通过对0.0001 μM 到1 μM的8个浓度的CX-4945实验结果的检测,计算出IC50。
细胞实验:[1]
+ 展开
  • Cell lines: SKBr3, MDA-MB-453, BT-474, ZR-75-1, MDA-MB-231, MDA-MB-468, T47D, MCF 7, Hs578T, MDA-MB-361, UACC-812, 等等
  • Concentrations: 溶于 DMSO, 终浓度 ~100 μM
  • Incubation Time: 4 天
  • Method: 在用药处理前,在合适的培养基中按每孔3000个细胞的浓度接种细胞培养24小时,然后用不同浓度的CX-4945处理细胞。接种悬浮细胞并处理相同的天数。接着孵育4天,加入Alamar Blue (20 μL, 体积比每孔10%),然后于37℃孵育4-5小时。检测荧光,激发光为530-560 nm,放射光为590 nm。
    (Only for Reference)
动物实验:[1]
+ 展开
  • Animal Models: 注射了BxPC-3 或BT-474细胞的免疫缺陷的雌鼠
  • Formulation: 溶于DMSO, 用PBS稀释
  • Dosages: 25或75 mg/kg
  • Administration: 每日两次口服
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 16 mg/mL (45.74 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):
1% CMC Na
30mg/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 349.77
化学式

C19H12ClN3O2

CAS号 1009820-21-6
稳定性 powder
in solvent
别名 N/A

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 (g) = 浓度 (mol/L) x 体积 (L) 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、MSDS / 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、MSDS / 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 Conditions Sponsor/Collaborators Start Date Phases
NCT02128282 Recruiting Cholangiocarcinoma Senhwa Biosciences Inc. June 2014 Phase 1|Phase 2
NCT01199718 Unknown status Multiple Myeloma Cylene Pharmaceuticals September 2010 Phase 1
NCT00891280 Unknown status Advanced Solid Tumors|Breast Cancer|Inflammatory Breast Cancer|Castleman''s Disease|Multiple Myeloma Cylene Pharmaceuticals February 2009 Phase 1

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1:

    How to reconstitute the compound (S2248) for in vivo uses?

  • 回答:

    For injection, CX-4945 can be dissolved in 2% DMSO+30% PEG 300+2% Tween 80+ddH2O at 5mg/ml clearly. When making the solution, please dissolve the compound in DMSO clearly first. If it dissolves not readily, please sonicate and warm the solution in water bath at about 45-50℃. Then add PEG and Tween. After they mixed well, dilute with water. For oral gavage, CX-4945 can be dissolved in 1% CMC Na at 30mg/ml as a homogeneous suspension. This is a common formulation for oral gavage, and is convenience to prepare.

Tags: 购买Silmitasertib (CX-4945) | Silmitasertib (CX-4945)供应商 | 采购Silmitasertib (CX-4945) | Silmitasertib (CX-4945)价格 | Silmitasertib (CX-4945)生产 | 订购Silmitasertib (CX-4945) | Silmitasertib (CX-4945)代理商
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID