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88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
A431  MVLGeY5kfGmxbjDBd5NigQ>? NIXDbXMyOCEQvF2= M33xbFMxKG2rbh?= NHK3d4ZifHSnboXheIV{KFCLM1utRYt1NW2WT2Kgd4lodmGuaX7n M2PTSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{i3PVg5Lz5{MkO4O|k5QDxxYU6=
H2170  NIficppHfW6ldHnvckBCe3OjeR?= MYOxNEDPxE1? MoDDN|AhdWmw NHLuVmFifHSnboXheIV{KFCLM1utRYt1NW2WT2Kgd4lodmGuaX7n NVzFenZpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzPFc6QDhpPkKyN|g4QTh6PD;hQi=>
A431  NHPaRlFHfW6ldHnvckBCe3OjeR?= MX2xNEDPxE1? NWfPfG1qPC1{NDDo NH3Sd|JmdmijbnPld{BieG:ydH;zbZMhf2m2aDDldoxwfGmwaXK= Ml2wQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|OEe5PFgoRjJ{M{i3PVg5RC:jPh?=
H2170  MlXsSpVv[3Srb36gRZN{[Xl? MofENVAh|ryP NF;ZU2Y1NTJ2IHi= MVPlcohidmOnczDhdI9xfG:|aYOge4l1cCCncnzveIlvcWJ? M2PkO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{i3PVg5Lz5{MkO4O|k5QDxxYU6=
LNCap MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTJOG9COC1|MDFOwG0> MYi0JIQ> MXjJR|UxRTRwNUpCpO69VQ>? M1vv[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OEOyN|E3Lz5{MkizNlMyPjxxYU6=
A549 NWTIPXp[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1PFZ|AuOzBizszN NGHZbXI4OiCq NVznUItFTE2VTx?= NYLWfHhnUUN3ME20MlE2KM7:TTygbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> NYXKRndrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2OVE1PDNpPkKzOlUyPDR|PD;hQi=>
H1299 NWntcHhjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3n1VFAuOzBizszN M3nOZ|czKGh? NUKwd4E{TE2VTx?= MoLTTWM2OD1zLkiwJO69VSxiaX7obYJqfHNiY3XscEBoem:5dHigZ49v[2WwdILheIlwdiCmZYDlcoRmdnSueR?= MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZ3MUS0N{c,OjN4NUG0OFM9N2F-
A549 NIfz[WFHfW6ldHnvckBCe3OjeR?= MXuxM|ExKM7:TR?= M2L2b|Q5KGh? MlTRSG1UVw>? M2jVeIxm[WS|IITvJIEh\G:|ZT3k[ZBmdmSnboSg[IVkemWjc3WgbY4hVm:2Y3igdoVxd3K2ZYKgZYN1cX[rdIm= NFvjfXg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[1NVQ1Oyd-MkO2OVE1PDN:L3G+
S-LAMA84 M1vOW2Z2dmO2aX;uJGF{e2G7 NWjYcVJiO8LizszN NYe2PGcyOjRiaB?= NYfxOYNuTE2VTx?= MnjudoVlfWOnczDDT|Ih[WO2aY\peJk> MlG5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMUKxNFkoRjJ2MEGyNVA6RC:jPh?=
R-LAMA84 NWH0RmhCTnWwY4Tpc44hSXO|YYm= NH;ZfWc{yqEQvF2= MVOyOEBp M2jBRmROW09? NXXtNYpOemWmdXPld{BEUzJiYXP0bZZqfHl? M33OO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEGyNVA6Lz5{NECxNlExQTxxYU6=
S-LAMA84 NUDCVHZTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWniXXQ5Oi53LUGwJO69VQ>? MWq0PEBp M17hXmROW09? NXvk[VB[cW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? MlzlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMUKxNFkoRjJ2MEGyNVA6RC:jPh?=
R-LAMA84 NXTjN4F4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NES4bGozNjVvMUCg{txO MnqzOFghcA>? MmO2SG1UVw>? NWr6ZZBOcW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? MkfPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMUKxNFkoRjJ2MEGyNVA6RC:jPh?=
A549 MUjGeY5kfGmxbjDBd5NigQ>? NYXBeVF2OTBizszN MlTtNVIwOjRxNEigbC=> MoLibY5pcWKrdIOgWGdHNc7{MT3pcoR2[2WmIH3p[5JifGmxbjDhcoQhcW64YYPpc44> NH:zbHo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECyN|k{QCd-MkSwNlM6Ozh:L3G+
A549 M{jYS2Z2dmO2aX;uJGF{e2G7 M4HoPFMh|ryP MmrnOFghcA>? MmrMbY5pcWKrdIOgWGdHNc7{MT3pcoR2[2WmIHHjeIl3[XSrb36gc4YhW22jZDDhcoQh\XiycnXzd4lwdiCxZjDTcoFqdCCjbnSgWJdqe3R? NIHzUWk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NECyN|k{QCd-MkSwNlM6Ozh:L3G+
U-266 MlSyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEjieFcxNTRyIN88US=> MlzDOFghcA>? NXjoRWtzUUN3ME2xPU45KML3TdMg NV3Qc4xqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwPFY1QTRpPkK0NFg3PDl2PD;hQi=>
INA-6 NHG2XHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HsWlAuPDBizszN Mk\BOFghcA>? NGXBXWNKSzVyPUKuOFIhyrWP NVHT[pFuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwPFY1QTRpPkK0NFg3PDl2PD;hQi=>
Jeko-1 M3S2d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HIZVAuPDBizszN NXHUfYdVPDhiaB?= M4Ts[GlEPTB;Mj60JOK2VcLi NE\kZmk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEC4OlQ6PCd-MkSwPFY1QTR:L3G+
Rec-1 NHW2cZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HWfFAuPDBizszN M3PHcFQ5KGh? NHXRR2NKSzVyPUGuOFYhyrWPwrC= M2rG[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEi2OFk1Lz5{NEC4OlQ6PDxxYU6=
Jurkat NFjFcYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPUNU0yOCEQvF2= Mnn2OFghcA>? MYDJR|UxRTRwOTFOwG0> NEDFZ5U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEK1N|AzPCd-MkSyOVMxOjR:L3G+
CEM-R M1TUcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVuxMVExKM7:TR?= MoPIOFghcA>? MWXJR|UxRTRizszN MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJ3M{CyOEc,OjR{NUOwNlQ9N2F-
CEM-S MoDuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfkNU0yOCEQvF2= M4\wclQ5KGh? MXHJR|UxRTRwNjFOwG0> MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJ3M{CyOEc,OjR{NUOwNlQ9N2F-
MOLT-4 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PtZlEuOTBizszN NILGeGY1QCCq MnLqTWM2OD13Lkeg{txO NWjhfGtURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyOVMxOjRpPkK0NlU{ODJ2PD;hQi=>
PF-382 NH7Edm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVWxMVExKM7:TR?= M1vTXVQ5KGh? MmnXTWM2OD12LkWg{txO NIXuNng9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEK1N|AzPCd-MkSyOVMxOjR:L3G+
ALL-SIL M{fCbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUfJT483OS1zMDFOwG0> M2f5W|Q5KGh? M176W2lEPTB;NT63JO69VQ>? MoLuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR{NUOwNlQoRjJ2MkWzNFI1RC:jPh?=
HPB-ALL MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljHNU0yOCEQvF2= M13NdFQ5KGh? M1;NO2lEPTB;Nj6xJO69VQ>? MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJ3M{CyOEc,OjR{NUOwNlQ9N2F-
DND-41 MkXUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33qflEuOTBizszN NXfOd5JsPDhiaB?= MXfJR|UxRTlizszN MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJ3M{CyOEc,OjR{NUOwNlQ9N2F-
ALL-SIL MkTERZBweHSxc3nzJGF{e2G7 NFHJXoQ2KM7:TR?= NHTtSYMzPC92ODDo NV7C[mhMcW6mdXPld{BieG:ydH;zbZM> NYfsR5B1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyOVMxOjRpPkK0NlU{ODJ2PD;hQi=>
DND-41 MlXHRZBweHSxc3nzJGF{e2G7 NYDZS3FpPSEQvF2= NWWwUYc{OjRxNEigbC=> Ml3wbY5lfWOnczDhdI9xfG:|aYO= MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJ3M{CyOEc,OjR{NUOwNlQ9N2F-
MOLT-4 M3XzPGFxd3C2b4Ppd{BCe3OjeR?= NYfhV3dNPSEQvF2= NFOwWoczPC92ODDo MYnpcoR2[2W|IHHwc5B1d3Orcx?= NIXjNZM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEK1N|AzPCd-MkSyOVMxOjR:L3G+
C2C12 M4rjOmZ2dmO2aX;uJGF{e2G7 M3O0NFMh|ryP MlrtNVIwOjRxNEigbC=> MnS1bY5pcWKrdIOgeIhmKGW6cILld5Nqd25ib3[gc5N1\W:lbHHzeEBlcW[oZYLlcpRq[XSrb36gcYFzc2W{czDhcoQhSWu2IIDoc5NxcG:{eXzheIlwdg>? M2T4V|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MkmzNFEyLz5{NEK5N|AyOTxxYU6=
Nalm6  NGjkdFVHfW6ldHnvckBCe3OjeR?= NWH1[4pFOTBxMkCg{txO MofGNlQhcA>? NXvHUW4zemW|dXz0d{BqdiCmZXPy[YF{\WRiUGTFUkBxcG:|cHjvdplt[XSrb36gZZQhfGinIFPLNkB1[XKpZYSgdoV{cWS3ZTDTN|gxKGGwZDDjc45kd22rdHHueEBld3ewcnXneYxifGmxbjDv[kBRXEWQIIDyc5RmcW5iZYjwdoV{e2mxbh?= MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV4MUe5Nkc,OjR3NkG3PVI9N2F-
SUP-B15 M3TLVGZ2dmO2aX;uJGF{e2G7 MXqxNE8zOCEQvF2= NFXOSVIzPCCq MoS2doV{fWy2czDpckBl\WO{ZXHz[YQhWFSHTjDwbI9{eGixconsZZRqd25iYYSgeIhmKEONMjD0ZZJo\XRicnXzbYR2\SCVM{iwJIFv\CClb37jc41qfGGwdDDkc5dvemWpdXzheIlwdiCxZjDQWGVPKHC{b4TlbY4h\XiycnXzd4lwdg>? NX3TfoMxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1OlE4QTJpPkK0OVYyPzl{PD;hQi=>
Nalm6  MlPXRZBweHSxc3nzJGF{e2G7 MonyOk8yOCEQvF2= M{nGVFQ5KGh? MVjpcoR2[2W|IHHwc5B1d3Orcx?= MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV4MUe5Nkc,OjR3NkG3PVI9N2F-
SUP-B15 M1fi[2Fxd3C2b4Ppd{BCe3OjeR?= NFzXUXY3NzFyIN88US=> NYXhOIRDPDhiaB?= NIP6XXlqdmS3Y3XzJIFxd3C2b4Ppdy=> NWLrO4ZORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS1OlE4QTJpPkK0OVYyPzl{PD;hQi=>
ARPE-19 NVPVZY8yU2mwYYPlJGF{e2G7 MU[1M|ExNzJyIN88US=> MUOyOE81QCCq MkTabY5pcWKrdIOgR2szKGurbnHz[UBi[3Srdnn0fUBifCCjIHPvcoNmdnS{YYTpc44hd2ZiNdMg{txO NHrpTo49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[4OlA5OCd-MkS2PFYxQDB:L3G+
ARPE-19 M{TzN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUj1Z|BWOTBizszN NV7LVI9kOjRvOU[gbC=> M{H5OWROW09? Mnv4bY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> NEj0Sog9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[4OlA5OCd-MkS2PFYxQDB:L3G+
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ARPE-19 NXP5SHRETnWwY4Tpc44hSXO|YYm= NIHPSmMyOCEQvF2= NX60VHB{PCCq MoG5SG1UVw>? MXTjZZV{\XNiRWKtd5Rz\XO|IILld5BwdnOnIH;2[ZIhfGinIICt[WlHOs7zIHLyZY5kcCxiYoX0JIRw\XNibn;0JIlv\HWlZTDDTG9RyqB? M1;YVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2Nki2NFgxLz5{NE[4OlA5ODxxYU6=
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A673 NHexS|FyUFSVIHHzd4F6 M4jDepFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCDNkezJINmdGy| Mk\EQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
DAOY NYKybpNDeUiWUzDhd5NigQ>? NV3BXI9VeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFTBU3kh[2WubIO= M3fQ[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Saos-2 MV3xTHRUKGG|c3H5 Ml\PdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOjb4OtNkBk\Wyucx?= M2HVTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
BT-37 NIX5dlRyUFSVIHHzd4F6 MVnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSlRvM{egZ4VtdHN? M2H2ZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
RD M2i4ZpFJXFNiYYPzZZk> MXzxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWkRiY3XscJM> NXnENJBmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-SH NEL4VIdyUFSVIHHzd4F6 M1PMPZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMXNJKGOnbHzz MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
BT-12 MYnxTHRUKGG|c3H5 MYrxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSlRvMUKgZ4VtdHN? NYq5XZNPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
MG 63 (6-TG R) NYjZPHJNeUiWUzDhd5NigQ>? MULxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVUdiNkOgLFYuXEdiUjmgZ4VtdHN? NULVU25LRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB1643 NEnpWlRyUFSVIHHzd4F6 NH;1OWhyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKxOlQ{KGOnbHzz M2rlOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
OHS-50 MnPxdWhVWyCjc4PhfS=> NEXzdGZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiT1jTMVUxKGOnbHzz NInzOZI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Rh41 MkHadWhVWyCjc4PhfS=> NXy0PGlLeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGLoOFEh[2WubIO= MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SJ-GBM2 MVvxTHRUKGG|c3H5 NF\2R45yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1qtS2JOOiClZXzsdy=> MmDtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SK-N-MC NWrzN2RHeUiWUzDhd5NigQ>? NIS5W4tyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1OSyClZXzsdy=> M4m3d|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB-EBc1 MonJdWhVWyCjc4PhfS=> NUfF[lJGeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF7CMWVD[zFiY3XscJM> NXuweFZMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
LAN-5 MXHxTHRUKGG|c3H5 NILlOolyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTFHOMVUh[2WubIO= MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Rh18 MWfxTHRUKGG|c3H5 NFzRfJFyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUnixPEBk\Wyucx?= M4rUSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=

... 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

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04668209 Recruiting Drug: Silmitasertib Coronavirus University of Arizona|Senhwa Biosciences Inc. January 1 2021 Phase 2
NCT04663737 Recruiting Drug: Silmitasertib|Drug: SOC Covid19 Chris Recknor MD|Senhwa Biosciences Inc. December 3 2020 Phase 2
NCT03904862 Recruiting Drug: CX 4945 Medulloblastoma Childhood Pediatric Brain Tumor Consortium|St. Jude Children''s Research Hospital|National Cancer Institute (NCI) March 18 2019 Phase 1|Phase 2
NCT02128282 Active not recruiting Drug: CX-4945|Drug: Cisplatin|Drug: Gemcitabine Cholangiocarcinoma Senhwa Biosciences Inc. June 2014 Phase 1|Phase 2

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