Silmitasertib (CX-4945)

For research use only. Not for use in humans.

目录号:S2248

Silmitasertib (CX-4945) Chemical Structure

CAS No. 1009820-21-6

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)。Silmitasertib可诱导自噬并促进细胞凋亡。Phase 1/2。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 2381.77 现货
RMB 1040.13 现货
RMB 1418.29 现货
RMB 2604.97 现货
RMB 7289.1 现货
RMB 10401.33 现货
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客户使用Selleck生产的Silmitasertib (CX-4945)发表文献67篇:

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)。Silmitasertib可诱导自噬并促进细胞凋亡。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 MU\LbY5ie2ViQYPzZZk> NHrr[HYyNzVxMUCg{txO MYiwMlUhcA>? M3\1S2ROW09? MoPqdoVlfWOnczDDT|Ihc2mwYYPlJIFkfGm4aYT5JIFv\CCybHH0[YxmfCCjZ3fy[YdifGmxbh?= NXn2NJVrOjZ|OEG0N|c>
HDMEC NILmOGFMcW6jc3WgRZN{[Xl? NEXEcWoxNjJ3L{CuOU8yKM7:TR?= NUHIcoViOjRiaB?= NUPPeIk1TE2VTx?= M4W3VJJm\HWlZYOgR2szKGurbnHz[UBi[3Srdnn0fUwhfleIIHX4dJJme3Orb36gZY5lKHOnY4LleIlwdg>? NEjPXYMzPjN6MUSzOy=>
HDMEC NHfofItHfW6ldHnvckBCe3OjeR?= MWewMlI2NzBwNT:xJO69VQ>? MlrvNlQhcA>? M4D4WmROW09? MXny[YR2[2W|IHX4dJJme3Orb36gc4YhXkODTT2xJIJ2fCCwb4SgTWNCVS1z M4rZSVI3OzhzNEO3
HDMEC MWTGeY5kfGmxbjDBd5NigQ>? MkS5NUDPxE1? NYjPXo9KOjRiaB?= NXLtUJRxTE2VTx?= M4[xVYFn\mWldIOgd5Vj[2WubIXsZZIhdG:lYXzpfoF1cW:wIH;mJG5HSVSlMTDhcoQheGixc4Doc{1xPjV? NFnRZoozPjN6MUSzOy=>
A549  M1X5eGZ2dmO2aX;uJGF{e2G7 MknjN{8yOMLizszN NWPsVYxCPDhiaB?= NEWxU2R{fXCycnXzd4V{KHSqZTDtbYNzd3CrbHzhdk1qdmS3Y3XkJIV5eHKnc4Ppc44hd2ZicD3GRWs> NFL1TVEzPjNzOEiwNC=>
HDMEC MXzLbY5ie2ViQYPzZZk> NFjkcW4yNTVyIN88US=> M4fj[VUhcA>? NGTleZBFVVOR MWLk[YNz\WG|ZYOgR2szKGurbnHz[UBi[3Srdnn0fUB4cXSqb4X0JIFn\mWldHnu[{Bk\WyuII\pZYJqdGm2eR?= NX7CT|IxOjZzOEm1PFY>
HDMEC MW\GeY5kfGmxbjDBd5NigQ>? NW\BTHhFPTBizszN MUmxM|UhcA>? NXTzSnFOTE2VTx?= Mnq5[IVkemWjc3XzJJRp\SCwdXPs[YFzKHOrZ37hcEBw\iCyaH;zdIhwenmuYYTl[EBxPjViaX6gWG5HNc7zLYP0bY12dGG2ZXSgTGROTUQEoB?= NHyyeGMzPjF6OUW4Oi=>
HEK293 NH\CV4hMcW6jc3WgRZN{[Xl? NEDuOlUxNjYEoN88US=> NUXYfm53OTVibXnu MWjEUXNQ M2jxSZJm\HWlZYOgR2szKGurbnHz[UBi[3Srdnn0fS=> NYXEeZFEOjV6OEe2NlY>
Hela M2DxNmtqdmG|ZTDBd5NigQ>? MYewMlXDqM7:TR?= NYD1T2x5OTVibXnu Ml;YSG1UVw>? MnXQdoVlfWOnczDDT|Ihc2mwYYPlJIFkfGm4aYT5 MY[yOVg5PzZ{Nh?=
LAMA84 NVHZdpNXU2mwYYPlJGF{e2G7 NWnwPFRDOC53wrFOwG0> NV3hSG8yOTVibXnu MoDpSG1UVw>? MYfy[YR2[2W|IFPLNkBscW6jc3WgZYN1cX[rdIm= M2PZXVI2QDh5NkK2
HEK293 NWDHSGQxTnWwY4Tpc44hSXO|YYm= M1j3blMh|ryP NVnWXpRNPSCq M4PmfGROW09? NV;iUWZNS0t{IIDoc5NxcG:{eXzheIV{KGWLRkPqJIF1KFOnckGyOy=> NVHXO2FUOjV6OEe2NlY>
UM-SCC1 MnvrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUGwMlEuOzBizszN NWjMNmdwOS13IHS= MlfnTWM2OD12LkGg{txO M2ntTVI2Pzl6ME[x
UM-SCC46 M3X5cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIL0XZkxNjFvM{Cg{txO MV6xMVUh\A>? NYDLbVJvUUN3ME2zMlQh|ryP NWrFcYc6OjV5OUiwOlE>
UM-SCC1 NVztO5FMTnWwY4Tpc44hSXO|YYm= M1n3Z|AvPS92L{GwJO69VQ>? MmK5O|IhcA>? MYrkc5dvNXKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCQRj5EvGItKEKlbD3YUEBidmRidYCtdoVofWyjdHXzJJRp\SCneIDy[ZN{cW:wIH;mJJA2OyxicEKxMEBCWC1zIHHu[EBKVC16IHPvcoNmdnS{YYTpc44h\GWyZX7k[Y51dHl? NVq1ZWg1OjV5OUiwOlE>
UM-SCC46 Ml\JSpVv[3Srb36gRZN{[Xl? NH3PSFcxNjVxND:xNEDPxE1? NX;HdoJFPzJiaB?= M{jKbIRwf25vcnXneYxifGW|IITo[UBmgHC{ZYPzbY9vKG:oIF7GMeS5SixiQnPsMXhNNCCyNUOsJJAzOSxiQWCtNUBidmRidYCtdoVofWyjdHXzJJRp\SCneIDy[ZN{cW:wIFnMMVgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> NFPzNlMzPTd7OEC2NS=>
NU-DUL M36yPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfWbFN7PS1{NTFOwG0> M2fM[FQ5KGh? NGXUZ|lqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 MXWyOVc5QDJ4OR?=
Oci Ly 3 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\W[Y02NTJ3IN88US=> NIjkWms1QCCq Mo[2bY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> MVWyOVc5QDJ4OR?=
Oci Ly 10 NFzTVWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2qz[|UuOjVizszN NWTReZhEPDhiaB?= M2XhN4lvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> MofFNlU4QDh{Nkm=
Oci Ly 1 MoDaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13LNVUuOjVizszN MmLUOFghcA>? M2j4colvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> NWe3bVVGOjV5OEiyOlk>
Oci Ly 18 M3z1dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XwOlUuOjVizszN MV20PEBp MmfIbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> NIPIdHIzPTd6OEK2PS=>
Oci Ly 19  M3v2dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPtOU0zPSEQvF2= NHTwdXg1QCCq NFrWZW9qdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 MojWNlU4QDh{Nkm=
Raji MkLWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnXeWUxPS1{NTFOwG0> MnPHOFghcA>? NHPxeXVqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NFXaTm8zPTd6OEK2PS=>
H1299 NYfRXG1MT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmHwNU82NzFyIN88US=> NYLIOJptPzJiaB?= M{P2UIlvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> MnP4NlU4PTB|MEi=
Calu-1  MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1f0U|EwPS9zMDFOwG0> MmfGO|IhcA>? NVX5[FhGcW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? Mnr4NlU4PTB|MEi=
H358 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlrlNU82NzFyIN88US=> M3S0ZlczKGh? NV7y[o5bcW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? NUH1enU3OjV5NUCzNFg>
H1299 MVnBdI9xfG:|aYOgRZN{[Xl? MXqxNEDPxE1? M4L1W|czKGh? MVHpcoR2[2W|IHHwc5B1d3Orcx?= NWHYZ5B[OjV5NUCzNFg>
Calu-1  NFewRZdCeG:ydH;zbZMhSXO|YYm= MlX2NVAh|ryP M1rzfVczKGh? MYTpcoR2[2W|IHHwc5B1d3Orcx?= NX7yNJh6OjV5NUCzNFg>
H358 MYPBdI9xfG:|aYOgRZN{[Xl? NEDoU3AyOCEQvF2= M3jhfFczKGh? Mn3UbY5lfWOnczDhdI9xfG:|aYO= MXuyOVc2ODNyOB?=
PC9/GR Mk\ESpVv[3Srb36gRZN{[Xl? MoS4OUDDvU1? NYjHV|IyPDhiaB?= MV\pcoR2[2W|IHH1eI9xcGGpeR?= M4Xwb|I2PDh4NEC5
PC9/ER MljBSpVv[3Srb36gRZN{[Xl? NHX1XHU2KML3TR?= NULuNG1WPDhiaB?= M3vvVIlv\HWlZYOgZZV1d3CqYXf5 MVKyOVQ5PjRyOR?=
H28 NXXtUJdWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXXtfpl2OC5yMT2zNEDPxE1? NHHEcXo4OiCq NHTUN4VFVVOR MVXJR|UxRTdwMjFOwG0> M{XTRlI2PDJ{MEix
H2052 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYr0OHhSOC5yMT2zNEDPxE1? MlfHO|IhcA>? M1L3e2ROW09? NFPGcGZKSzVyPUKuNEDPxE1? MlHqNlU1OjJyOEG=
UM-SCC-1 MknGR4xwdm:pZX7pZ{BCe3OjeR?= MWewMlUuPSEQvF2= M4nmbVE1KGR? MVHEUXNQ NYPVVVUxyqCrbnjpZol1eyClbH;uc4dmdmmlIIP1dpZqfmGuIHHu[EB{eGincnWg[o9zdWG2aX;u MWqyOVM4QTBzNh?=
UM-SCC-46 M3jKe2Ntd26xZ3XubYMhSXO|YYm= MX:wMlUuPSEQvF2= NUfNVWVZOTRiZB?= NUXoWol[TE2VTx?= M4\pT:KhcW6qaXLpeJMh[2yxbn;n[Y5q[yC|dYL2bZZidCCjbnSgd5Bp\XKnIH\vdo1ifGmxbh?= MVuyOVM4QTBzNh?=
U87-MG Mn7LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrFT2NZOS93L{GwJO69VQ>? M{fzdlI1NzR6L{eyJIg> NHvZWXhFVVOR NF\HZXJqdmirYnn0d{Bk\WyuIHfyc5d1cCCkb4ToJINwdmOnboTyZZRqd25iYX7kJJRqdWViZHXw[Y5l\W62bIm= MWqyOVI1OTh7Nx?=
MDA-MB-231 MY\GeY5kfGmxbjDBd5NigQ>? M3HZW|IwPS9zMDFOwG0> MmXGOEBp MUjk[YNz\WG|ZYOgeIhmKGOxboP0bZR2fGm4ZTDwbI9{eGixconsZZRqd25ib3[gZo91cCBicD3TOVI6NXB4NTDhcoQheC2VMUK5MWFsfA>? MlPtNlUyPTN5MkW=
MDA-MB-231 NX:4Z2tXTnWwY4Tpc44hSXO|YYm= NI\6ZlYzNzVxMUCg{txO NYPvOHUzPCCq NIn3XVNqdmirYnn0d{B{\XKrbnWgOVI6KHCqb4PwbI9zgWyjdHnvckBidmRidHjlJIV5eHKnc4Ppc44hd2ZiSVytOkwhUUxvOB?= M3f2UVI2OTV|N{K1
ARPE-19 NV;xXJhFU2mwYYPlJGF{e2G7 Mki4OU8yOC9{MDFOwG0> MVWyOE81QCCq NYH4R|dGcW6qaXLpeJMhS0t{IHvpcoF{\SCjY4Tpeol1gSCjdDDhJINwdmOnboTyZZRqd25ib3[gOeKh|ryP NHnIS48zPDZ6NkC4NC=>
ARPE-19 NW\USXYxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1PqdVExKM7:TR?= M3jKSVI1NTl4IHi= MoXvSG1UVw>? NUDabXh4cW6qaXLpeJMh[2WubDDndo94fGhidHnt[UBl\XCnbnTlcpRtgQ>? NXP6UolmOjR4OE[wPFA>
HCT116  MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWr1fo15OTBizszN NV;2bpRSOjRvOU[gbC=> M3zoNGROW09? M4nwcolvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk> NXnieWk1OjR4OE[wPFA>
ARPE-19 M1;IbGZ2dmO2aX;uJGF{e2G7 NUDYO4JCOTBizszN NWXkfFBVPCCq M1v1NWROW09? NWntdlZW[2G3c3XzJGVTNXO2cnXzd{Bz\XOyb37z[UBwfmW{IITo[UBxNWWLRkNOtUBjemGwY3isJIJ2fCCmb3XzJI5wfCCrbnT1Z4UhS0iRUNMg NHjORWMzPDZ6NkC4NC=>
HCT116  MVnGeY5kfGmxbjDBd5NigQ>? M1[wSlExKM7:TR?= M3H5S|QhcA>? MULEUXNQ MmXQZ4F2e2W|IFXSMZN1emW|czDy[ZNxd26|ZTDveoVzKHSqZTDwMYVKTjMQsTDidoFv[2huIHL1eEBld2W|IH7veEBqdmS3Y3WgR2hQWMLi MYCyOFY5PjB6MB?=
HCT116  NXLuPWs2SXCxcITvd4l{KEG|c3H5 MlH1NVAh|ryP MUmyOE81QCCq NXKwemJCTE2VTx?= MlvobY5lfWOnczDhdI9xfG:|aYO= NVfyRZVJOjR4OE[wPFA>
Nalm6  M1;Tc2Z2dmO2aX;uJGF{e2G7 M1mxblExNzJyIN88US=> MXKyOEBp M1nEfpJme3WudIOgbY4h\GWlcnXhd4VlKFCWRV6gdIhwe3Cqb4L5cIF1cW:wIHH0JJRp\SCFS{KgeIFz\2W2IILld4llfWViU{O4NEBidmRiY3;uZ49ucXSjboSg[I94dnKnZ4XsZZRqd25ib3[gVHRGViCycn;0[YlvKGW6cILld5Nqd25? MWKyOFU3OTd7Mh?=
SUP-B15 NX[1[IlZTnWwY4Tpc44hSXO|YYm= MX[xNE8zOCEQvF2= NWPPVGF4OjRiaB?= MlvEdoV{fWy2czDpckBl\WO{ZXHz[YQhWFSHTjDwbI9{eGixconsZZRqd25iYYSgeIhmKEONMjD0ZZJo\XRicnXzbYR2\SCVM{iwJIFv\CClb37jc41qfGGwdDDkc5dvemWpdXzheIlwdiCxZjDQWGVPKHC{b4TlbY4h\XiycnXzd4lwdg>? MnPYNlQ2PjF5OUK=
Nalm6  NFX1c3dCeG:ydH;zbZMhSXO|YYm= M2\NPVYwOTBizszN M2\HOFQ5KGh? NVr0e|J[cW6mdXPld{BieG:ydH;zbZM> NWHlXHpwOjR3NkG3PVI>
SUP-B15 M37LNGFxd3C2b4Ppd{BCe3OjeR?= MmjpOk8yOCEQvF2= MXK0PEBp MXjpcoR2[2W|IHHwc5B1d3Orcx?= M4LOelI1PTZzN{my
C2C12 M4HGdGZ2dmO2aX;uJGF{e2G7 MojpN{DPxE1? M1fzV|EzNzJ2L{S4JIg> NHnDUHBqdmirYnn0d{B1cGViZYjwdoV{e2mxbjDv[kBwe3Snb3PsZZN1KGSrZn\ldoVvfGmjdHnvckBu[XKtZYLzJIFv\CCDa4SgdIhwe3Cqb4L5cIF1cW:w M{jlXFI1Ojl|MEGx
Jurkat MmXNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFy2OWQyNTFyIN88US=> NXS2SlNYPDhiaB?= M3rjemlEPTB;ND65JO69VQ>? NYT0TWpKOjR{NUOwNlQ>
CEM-R M3HxNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4fhSVEuOTBizszN MWq0PEBp MojQTWM2OD12IN88US=> MVmyOFI2OzB{NB?=
CEM-S M{HqO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV7CWpdtOS1zMDFOwG0> Mn3FOFghcA>? M1nCe2lEPTB;ND62JO69VQ>? NFzSTG0zPDJ3M{CyOC=>
MOLT-4 Mk\aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HYWlEuOTBizszN M{[yR|Q5KGh? M3;2[mlEPTB;NT63JO69VQ>? M13FbVI1OjV|MEK0
PF-382 M4Xuemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHO4fWcyNTFyIN88US=> NUXiUpF6PDhiaB?= MmLyTWM2OD12LkWg{txO MnfrNlQzPTNyMkS=
ALL-SIL NWXE[FdkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrUcowyNTFyIN88US=> NUnmRolbPDhiaB?= M4rDTmlEPTB;NT63JO69VQ>? M2X4WVI1OjV|MEK0
HPB-ALL NGPvc3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PCXlEuOTBizszN NHHsWGc1QCCq NEntXo1KSzVyPU[uNUDPxE1? NXzQd21YOjR{NUOwNlQ>
DND-41 Mon2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknoNU0yOCEQvF2= M4iyUlQ5KGh? NFzUXG1KSzVyPUmg{txO M3rHXVI1OjV|MEK0
ALL-SIL M2HaVWFxd3C2b4Ppd{BCe3OjeR?= NUG0dZduPSEQvF2= NX24ToRoOjRxNEigbC=> NV20b5JrcW6mdXPld{BieG:ydH;zbZM> MYeyOFI2OzB{NB?=
DND-41 NWnlfGs{SXCxcITvd4l{KEG|c3H5 NWjDSnp{PSEQvF2= M{HuO|I1NzR6IHi= MX\pcoR2[2W|IHHwc5B1d3Orcx?= M4f4dVI1OjV|MEK0
MOLT-4 MnLXRZBweHSxc3nzJGF{e2G7 MWK1JO69VQ>? NYXjRlF[OjRxNEigbC=> NYLYcFlmcW6mdXPld{BieG:ydH;zbZM> MonoNlQzPTNyMkS=
U-266 M4nuNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\2VXkxNTRyIN88US=> M4XTSFQ5KGh? NGP3WolKSzVyPUG5MlghyrWPwrC= MnKxNlQxQDZ2OUS=
INA-6 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUTDNYpMOC12MDFOwG0> MkDCOFghcA>? MnPKTWM2OD1{LkSyJOK2VQ>? MXiyOFA5PjR7NB?=
Jeko-1 NF7IfY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3WweFAuPDBizszN MVe0PEBp Mn20TWM2OD1{LkSgxtVOyqB? M1PWTFI1ODh4NEm0
Rec-1 M2j4fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\DN|ExNTRyIN88US=> MUe0PEBp M1W0WmlEPTB;MT60OkDDvU4EoB?= MUOyOFA5PjR7NB?=
A549 MVrGeY5kfGmxbjDBd5NigQ>? M1zPUFExKM7:TR?= MnG3NVIwOjRxNEigbC=> MkjxbY5pcWKrdIOgWGdHNc7{MT3pcoR2[2WmIH3p[5JifGmxbjDhcoQhcW64YYPpc44> M3TQSFI1ODJ|OUO4
A549 MlTaSpVv[3Srb36gRZN{[Xl? MXGzJO69VQ>? MXq0PEBp MUjpcohq[mm2czDUS2Yu|rJzLXnu[JVk\WRiYXP0bZZifGmxbjDv[kBUdWGmIHHu[EBmgHC{ZYPzbY9vKG:oIGPuZYltKGGwZDDUe4l{fA>? NHTGU3gzPDB{M{mzPC=>
S-LAMA84 NVTudoZWTnWwY4Tpc44hSXO|YYm= NIqyNYM{yqEQvF2= NHLTe2gzPCCq MXvEUXNQ NEjicFFz\WS3Y3XzJGNMOiCjY4Tpeol1gQ>? NEPCbo8zPDBzMkGwPS=>
R-LAMA84 NU[x[FMyTnWwY4Tpc44hSXO|YYm= MnPnN:Kh|ryP NH[1bo4zPCCq MV3EUXNQ M33peJJm\HWlZYOgR2szKGGldHn2bZR6 MkLuNlQxOTJzMEm=
S-LAMA84 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3UeHJROi53LUGwJO69VQ>? NH3UWXU1QCCq NVHvPXpKTE2VTx?= Mn\jbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> M{W3NlI1ODF{MUC5
R-LAMA84 NXLTR2M2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjXPIMzNjVvMUCg{txO M1HOcVQ5KGh? NF2xbFFFVVOR M2\NS4lvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> MViyOFAyOjFyOR?=
A549 NUPjR4l7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHNT3gxNTNyIN88US=> MkDPO|IhcA>? MonlSG1UVw>? MlHRTWM2OD12LkG1JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHigZ49v[2WwdILheIlwdiCmZYDlcoRmdnSueR?= NHvxdW4zOzZ3MUS0Ny=>
H1299 NYK1dHAyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrwXFIxNTNyIN88US=> NXvCU5lyPzJiaB?= NX35bGhxTE2VTx?= MXTJR|UxRTFwOECg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDjc45k\W62cnH0bY9vKGSncHXu[IVvfGy7 NX70NplxOjN4NUG0OFM>
A549 MVnGeY5kfGmxbjDBd5NigQ>? MXqxM|ExKM7:TR?= NVXjb4dFPDhiaB?= NHHNWpJFVVOR Mn\zcIVi\HNidH:gZUBld3OnLXTldIVv\GWwdDDk[YNz\WG|ZTDpckBPd3SlaDDy[ZBwenSncjDhZ5Rqfmm2eR?= NUXlWWxSOjN4NUG0OFM>
LNCap MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfhOmVsOC1|MDFOwG0> MmGyOEBl M2PqVWlEPTB;ND61PeKh|ryP MnH2NlI5OzJ|MU[=
A431  NV2zRmdvTnWwY4Tpc44hSXO|YYm= NILkdpcyOCEQvF2= M3;pOlMxKG2rbh?= MoLMZZR1\W63YYTld{BRUTONLVHreE1uXE:UIIPp[45idGmwZx?= NIjKbJQzOjN6N{m4PC=>
H2170  M2WyNmZ2dmO2aX;uJGF{e2G7 MX6xNEDPxE1? NILncFY{OCCvaX6= M4KyU4F1fGWwdXH0[ZMhWEl|Sz3Bb5QudVSRUjDzbYdv[Wyrbne= NX;0NHRQOjJ|OEe5PFg>
A431  M4PBZWZ2dmO2aX;uJGF{e2G7 M3TQWFExKM7:TR?= NYruRVVRPC1{NDDo MlXC[Y5p[W6lZYOgZZBweHSxc3nzJJdqfGhiZYLsc5Rqdmmk MoLYNlI{QDd7OEi=
H2170  NVLt[HBvTnWwY4Tpc44hSXO|YYm= MVqxNEDPxE1? NXew[GlxPC1{NDDo MWjlcohidmOnczDhdI9xfG:|aYOge4l1cCCncnzveIlvcWJ? Mm\1NlI{QDd7OEi=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-S6K1(T389) / S6K1 / p-S6(S235/236) / S6; 

PubMed: 30683840     


DLD-1 cells were incubated with 25 μM silmitasertib for 16 h. The levels of the indicated proteins were analyzed by western blot.

p-AKT(S129) / p-AKT(T308) / p-AKT(S473) / AKT / p-ERK / ERK / TP53 / p-p21(Th145) / p21 / Bcl-xl; 

PubMed: 25798061     


CX-4945 altered PI3K/AKT/Bcl-XL, ERK/AP-1 and TP53/p21proteins in HNSCC. UM-SCC-1 (left) and UM-SCC-46 (right) cell lines were treated with 4 and 10 μM CX-4945, whole cell lysates were harvested 6 and 24 hours after treatment, and subjected to SDS-PAGE and Western blot of indicated proteins. β-action was used as a loading control.

p-Smad2 (Cytosol) / Smad2/3 (Cytosol) / Smad2/3 (Nucleus) / Twist / Snail; 

PubMed: 24023938     


The effect of CX-4945 on TGF-β1-induced activation of Smad and expression of Snail and Twist was evaluated using Western blot analysis. Briefly, after 24 h serum starvation, A549 cells were treated with TGF-β1 (5 ng/ml) alone or in combination with CX-4945 in media containing 0.1% FBS for 48 h. Cytosolic and Nuclear fractions were obtained. Actin and histone H3 were used as internal control of cytosolic and nuclear fraction, respectively. The relative, normalized ratio between p-Smad2 and actin was presented. 

30683840 25798061 24023938
Immunofluorescence
β-catenin; 

PubMed: 24023938     


Nuclear translocation of β-catenin and its inhibition by CX-4945 were confirmed by immunocytochemistry. Nuclei were counterstained with Hoechst 33342. All scale bars represent 20 µm.

E-cadherin / Vimentin; 

PubMed: 24023938     


The effect of CX-4945 on the TGF-β1-induced expression of epithelial and mesenchymal markers was evaluated by immunocytochemistry. Briefly, after 24 h serum starvation, A549 cells were treated with TGF-β1 (5 ng/ml) alone or in combination with CX-4945 in media containing 0.1% FBS for 72 h. All scale bars represent 200 µm.

24023938
Growth inhibition assay
Cell viability; 

PubMed: 30316146     


CX-4945 decreases cell viability of HuCCT1, EGI-1, and Liv27 CCA cell lines in dose-dependent manner (IC50of 7.3, 9.5, and 9.4 μM, respectively) (A)

30316146
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]
- 合并

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]
- 合并
  • 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]
- 合并
  • Animal Models: 注射了BxPC-3 或BT-474细胞的免疫缺陷的雌鼠
  • 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
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、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

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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID