Silmitasertib (CX-4945)

Catalog No.S2248

Silmitasertib (CX-4945) Chemical Structure

Molecular Weight(MW): 349.77

Silmitasertib (CX-4945) is a potent and selective inhibitor of CK2 (casein kinase 2) with IC50 of 1 nM in a cell-free assay, less potent to Flt3, Pim1 and CDK1 (inactive in cell-based assay). Phase 1/2.

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In DMSO USD 291 In stock
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5 Customer Reviews

  • 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.

Purity & Quality Control

Choose Selective Casein Kinase Inhibitors

Biological Activity

Description Silmitasertib (CX-4945) is a potent and selective inhibitor of CK2 (casein kinase 2) with IC50 of 1 nM in a cell-free assay, less potent to Flt3, Pim1 and CDK1 (inactive in cell-based assay). Phase 1/2.
Features First clinical inhibitor of CK2.
Targets
CK2 [1]
(Cell-free assay)
1 nM
In vitro

CX-4945 is selective for CK2, as it only inhibits 7 of the 238 kinases by more than 90% at concentration of 0.5 μM, which is 500-fold greater than the IC50 of CK2. Although in cell-free systems CX-4945 inhibits FLT3, PIM1, and CDK1 with IC50 of 35 nM, 46 nM, and 56 nM, respectively, CX-4945 treatment at 10 μM is inactive against FLT3, PIM1, and CDK1 in cell-based functional assays. CX-4945 exhibits a broad spectrum of antiproliferative activity, and the breast cancer cell lines displays the widest range of sensitivity to CX-4945 with EC50 of 1.71-20.01 μM. The antiproliferative activity of CX-4945 correlates with CK2α mRNA and protein levels but not the CK2α' catalytic subunit, the regulatory CK2β subunit, and the PI3K/Akt or PTEN mutational status. CX-4945 inhibits PI3K/Akt signaling by directly blocking the phosphorylation of Akt at Serine 129 by CK2 rather than through activation of PTEN. CX-4945 treatment causes reduced phosphorylation of p21 (T145), increased levels of total p21 and p27, and induction of caspase 3/7 activity. CX-4945 treatment induces a G2/M cell-cycle arrest in BT-474 cells and a G1 arrest in BxPC-3 cells. CX-4945 inhibits HUVEC proliferation, migration, and tube formation with IC50 of 5.5 μM, 2 μM, and 4 μM, respectively. Under hypoxic conditions in BT-474 and BxPC-3 cells, CX-4945 treatment prevents downregulation of p53 and pVHL and reduces activation of HIF-1α transcription. [1] CX-4945 potently inhibits endogenous intracellular CK2 activity with IC50 of 0.1 μM in Jurkat cells. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
platelets NUHWZo4xU2mwYYPlJGF{e2G7 MYCxM|UwOTBizszN MX:wMlUhcA>? MkH6SG1UVw>? MYHy[YR2[2W|IFPLNkBscW6jc3WgZYN1cX[rdImgZY5lKHCuYYTlcIV1KGGpZ4Ll[4F1cW:w M1f5N|I3OzhzNEO3
HDMEC MmTOT4lv[XOnIFHzd4F6 M1r6fVAvOjVxMD61M|Eh|ryP M2e5TFI1KGh? M1;QfGROW09? MYHy[YR2[2W|IFPLNkBscW6jc3WgZYN1cX[rdImsJJZYTiCneIDy[ZN{cW:wIHHu[EB{\WO{ZYTpc44> MXyyOlM5OTR|Nx?=
HDMEC MV3GeY5kfGmxbjDBd5NigQ>? MWKwMlI2NzBwNT:xJO69VQ>? NYjweHFXOjRiaB?= MmP5SG1UVw>? MkLCdoVlfWOnczDlfJBz\XO|aX;uJI9nKF[FQV2tNUBjfXRibn;0JGlESU1vMR?= M2DUZVI3OzhzNEO3
HDMEC MYnGeY5kfGmxbjDBd5NigQ>? MWWxJO69VQ>? Mnv6NlQhcA>? MYHEUXNQ NGTrSXZi\m[nY4TzJJN2[mOnbHz1cIFzKGyxY3HsbZpifGmxbjDv[kBPTkGWY{GgZY5lKHCqb4PwbI8ueDZ3 NV\KdHpiOjZ|OEG0N|c>
A549  M37oUmZ2dmO2aX;uJGF{e2G7 M3O3S|MwOTEEoN88US=> NX3FVo1tPDhiaB?= MXXzeZBxemW|c3XzJJRp\SCvaXPyc5BqdGyjcj3pcoR2[2WmIHX4dJJme3Orb36gc4YheC2IQVu= MWGyOlMyQDhyMB?=
HDMEC NF32WphMcW6jc3WgRZN{[Xl? MWWxMVUxKM7:TR?= NUfaUWdJPSCq MVzEUXNQ M3LMcYRm[3KnYYPld{BEUzJia3nuZZNmKGGldHn2bZR6KHerdHjveZQh[W[oZXP0bY5oKGOnbHygeoli[mmuaYT5 NGfEPJIzPjF6OUW4Oi=>
HDMEC NIDEfVFHfW6ldHnvckBCe3OjeR?= NGfXb3Q2OCEQvF2= NE\0NlMyNzViaB?= M1fFV2ROW09? MkL6[IVkemWjc3XzJJRp\SCwdXPs[YFzKHOrZ37hcEBw\iCyaH;zdIhwenmuYYTl[EBxPjViaX6gWG5HNc7zLYP0bY12dGG2ZXSgTGROTUQEoB?= MknENlYyQDl3OE[=
HEK293 NU\TSotvU2mwYYPlJGF{e2G7 NFOzOmQxNjYEoN88US=> NHL6b40yPSCvaX6= M4HVe2ROW09? MYjy[YR2[2W|IFPLNkBscW6jc3WgZYN1cX[rdIm= M1jYUFI2QDh5NkK2
Hela MoTKT4lv[XOnIFHzd4F6 NX3jT3J4OC53wrFOwG0> NIHZfHcyPSCvaX6= MXvEUXNQ M1r3bpJm\HWlZYOgR2szKGurbnHz[UBi[3Srdnn0fS=> MkS1NlU5QDd4Mk[=
LAMA84 NULkco5TU2mwYYPlJGF{e2G7 NVnmPVN4OC53wrFOwG0> NV\le3JFOTVibXnu MnT6SG1UVw>? NISyR4pz\WS3Y3XzJGNMOiCtaX7hd4Uh[WO2aY\peJk> MYqyOVg5PzZ{Nh?=
HEK293 MoDDSpVv[3Srb36gRZN{[Xl? MoHON{DPxE1? NVHBSXE2PSCq NYDJfGpyTE2VTx?= Mn7CR2szKHCqb4PwbI9zgWyjdHXzJIVKTjOsIHH0JHNmejF{Nx?= MWmyOVg5PzZ{Nh?=
UM-SCC1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\DVYoxNjFvM{Cg{txO MVuxMVUh\A>? NHrabY5KSzVyPUSuNUDPxE1? MV6yOVc6QDB4MR?=
UM-SCC46 NFzIOIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPCXHYxNjFvM{Cg{txO NFn0eJIyNTViZB?= MWDJR|UxRTNwNDFOwG0> NXfMOotZOjV5OUiwOlE>
UM-SCC1 NHrXfVhHfW6ldHnvckBCe3OjeR?= NHjwPY8xNjVxND:xNEDPxE1? NYK3cI5ZPzJiaB?= NFW3TYxld3ewLYLl[5Vt[XSnczD0bIUh\XiycnXzd4lwdiCxZjDOSk3FwEJuIFLjcE1ZVCCjbnSgeZAuemWpdXzheIV{KHSqZTDlfJBz\XO|aX;uJI9nKHB3MzygdFIyNCCDUD2xJIFv\CCLTD24JINwdmOnboTyZZRqd25iZHXw[Y5l\W62bIm= MWiyOVc6QDB4MR?=
UM-SCC46 MofNSpVv[3Srb36gRZN{[Xl? MlLHNE42NzRxMUCg{txO NYPkb3B6PzJiaB?= M1nFTIRwf25vcnXneYxifGW|IITo[UBmgHC{ZYPzbY9vKG:oIF7GMeS5SixiQnPsMXhNNCCyNUOsJJAzOSxiQWCtNUBidmRidYCtdoVofWyjdHXzJJRp\SCneIDy[ZN{cW:wIFnMMVgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> Mnf6NlU4QThyNkG=
NU-DUL NIHZXmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHydlc2NTJ3IN88US=> M2TFT|Q5KGh? M3r6UIlvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> NFfvfVkzPTd6OEK2PS=>
Oci Ly 3 NVTLdI1DT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfJOU0zPSEQvF2= NH7jb2k1QCCq M{fpWIlvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> M1nHW|I2Pzh6Mk[5
Oci Ly 10 MnnmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jSdVUuOjVizszN MWG0PEBp M{PFbolvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> MkW5NlU4QDh{Nkm=
Oci Ly 1 NVPJVWRFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXm1MVI2KM7:TR?= NVHlb49NPDhiaB?= Mon2bY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> NYPkUnQ2OjV5OEiyOlk>
Oci Ly 18 NWj6fmpZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjz[2Q2NTJ3IN88US=> MoHnOFghcA>? M37COolvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> MYeyOVc5QDJ4OR?=
Oci Ly 19  M{XScGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XqdlUuOjVizszN MVK0PEBp Mlq1bY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> M1u0e|I2Pzh6Mk[5
Raji M4joTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHe4cmY2NTJ3IN88US=> NXuyUZhQPDhiaB?= MkfmbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> NEKw[HkzPTd6OEK2PS=>
H1299 MnrmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rHXVEwPS9zMDFOwG0> MVG3NkBp NGnUdFhqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NFn5[o0zPTd3MEOwPC=>
Calu-1  NHXITItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7WNU82NzFyIN88US=> NYD4NFVlPzJiaB?= NH7iWHZqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 MViyOVc2ODNyOB?=
H358 Mm\3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVixM|UwOTBizszN M{HtXVczKGh? MmribY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> MVeyOVc2ODNyOB?=
H1299 NX\GcY4ySXCxcITvd4l{KEG|c3H5 MnrqNVAh|ryP MUm3NkBp M1fNUolv\HWlZYOgZZBweHSxc3nz M1H5[VI2PzVyM{C4
Calu-1  NInUSGJCeG:ydH;zbZMhSXO|YYm= MXSxNEDPxE1? NHnDUnE4OiCq M4TRXolv\HWlZYOgZZBweHSxc3nz MoHYNlU4PTB|MEi=
H358 MknKRZBweHSxc3nzJGF{e2G7 Ml;LNVAh|ryP MXy3NkBp MV\pcoR2[2W|IHHwc5B1d3Orcx?= Mki5NlU4PTB|MEi=
PC9/GR NXXaNo51TnWwY4Tpc44hSXO|YYm= NF\FXpA2KML3TR?= M16yeVQ5KGh? M1HWNolv\HWlZYOgZZV1d3CqYXf5 NVTxVm5POjV2OE[0NFk>
PC9/ER NVy0TohwTnWwY4Tpc44hSXO|YYm= M{\G[VUhyrWP MWS0PEBp MlHVbY5lfWOnczDheZRweGijZ4m= NU[xeJBuOjV2OE[0NFk>
H28 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjvSpdrOC5yMT2zNEDPxE1? M1XpW|czKGh? MX3EUXNQ MoDUTWM2OD15LkKg{txO NYn3Z3pPOjV2MkKwPFE>
H2052 NGT1SYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUWwMlAyNTNyIN88US=> Mo\iO|IhcA>? NIj4SYVFVVOR NFe4XWFKSzVyPUKuNEDPxE1? M2PZVlI2PDJ{MEix
UM-SCC-1 MVLDcI9vd2enbnnjJGF{e2G7 NGDDdm4xNjVvNTFOwG0> NH\kT3QyPCCm MnjzSG1UVw>? NV7uZ3V1yqCrbnjpZol1eyClbH;uc4dmdmmlIIP1dpZqfmGuIHHu[EB{eGincnWg[o9zdWG2aX;u MonFNlU{PzlyMU[=
UM-SCC-46 M3G1XWNtd26xZ3XubYMhSXO|YYm= NETzbnMxNjVvNTFOwG0> NGLwbFQyPCCm M3nqN2ROW09? NGn6b2vDqGmwaHnibZR{KGOub37v[4VvcWNic4Xyeol3[WxiYX7kJJNxcGW{ZTDmc5Ju[XSrb36= MkDvNlU{PzlyMU[=
U87-MG MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLw[Fd5OS93L{GwJO69VQ>? M4SzVlI1NzR6L{eyJIg> Mk\USG1UVw>? MYHpcohq[mm2czDj[YxtKGe{b4f0bEBjd3SqIHPvcoNmdnS{YYTpc44h[W6mIITpcYUh\GWyZX7k[Y51dHl? M2rQOVI2OjRzOEm3
MDA-MB-231 MoizSpVv[3Srb36gRZN{[Xl? M2jkdlIwPS9zMDFOwG0> MoHiOEBp MXvk[YNz\WG|ZYOgeIhmKGOxboP0bZR2fGm4ZTDwbI9{eGixconsZZRqd25ib3[gZo91cCBicD3TOVI6NXB4NTDhcoQheC2VMUK5MWFsfA>? MXyyOVE2Ozd{NR?=
MDA-MB-231 NVTWbFZiTnWwY4Tpc44hSXO|YYm= NUK1[2xWOi93L{GwJO69VQ>? NYSzWWlNPCCq M3PDOIlvcGmkaYTzJJNmemmwZTC1NlkheGixc4Doc5J6dGG2aX;uJIFv\CC2aHWg[ZhxemW|c3nvckBw\iCLTD22MEBKVC16 MmnqNlUyPTN5MkW=
ARPE-19 NYjSempUU2mwYYPlJGF{e2G7 NXH5U2t[PS9zMD:yNEDPxE1? MV[yOE81QCCq NYXOT2J1cW6qaXLpeJMhS0t{IHvpcoF{\SCjY4Tpeol1gSCjdDDhJINwdmOnboTyZZRqd25ib3[gOeKh|ryP MX:yOFY5PjB6MB?=
ARPE-19 MmrNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGLm[mQyOCEQvF2= M3:x[|I1NTl4IHi= MYrEUXNQ NXzGTJhycW6qaXLpeJMh[2WubDDndo94fGhidHnt[UBl\XCnbnTlcpRtgQ>? NX;mUJdjOjR4OE[wPFA>
HCT116  M3n4TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml2zNVAh|ryP MWCyOE06PiCq MW\EUXNQ NFLrSWVqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 NGSwN40zPDZ6NkC4NC=>
ARPE-19 M1;MZmZ2dmO2aX;uJGF{e2G7 M{TlUVExKM7:TR?= NVWwZ|R7PCCq M2rhU2ROW09? MmPNZ4F2e2W|IFXSMZN1emW|czDy[ZNxd26|ZTDveoVzKHSqZTDwMYVKTjMQsTDidoFv[2huIHL1eEBld2W|IH7veEBqdmS3Y3WgR2hQWMLi M{S1ZlI1Pjh4MEiw
HCT116  MmixSpVv[3Srb36gRZN{[Xl? NWTKSHBZOTBizszN MX:0JIg> MnLhSG1UVw>? NFXSS4Rk[XW|ZYOgSXIue3S{ZYPzJJJme3CxboPlJI93\XJidHjlJJAu\UmIMt8xJIJz[W6laDygZpV1KGSxZYOgco91KGmwZIXj[UBEUE:SwrC= MVmyOFY5PjB6MB?=
HCT116  MV\BdI9xfG:|aYOgRZN{[Xl? NWXCVm1rOTBizszN M1rWelI1NzR6IHi= MVnEUXNQ NY\VTFZ5cW6mdXPld{BieG:ydH;zbZM> MVSyOFY5PjB6MB?=
Nalm6  MV7GeY5kfGmxbjDBd5NigQ>? MUSxNE8zOCEQvF2= MlLtNlQhcA>? M17s[ZJme3WudIOgbY4h\GWlcnXhd4VlKFCWRV6gdIhwe3Cqb4L5cIF1cW:wIHH0JJRp\SCFS{KgeIFz\2W2IILld4llfWViU{O4NEBidmRiY3;uZ49ucXSjboSg[I94dnKnZ4XsZZRqd25ib3[gVHRGViCycn;0[YlvKGW6cILld5Nqd25? MYCyOFU3OTd7Mh?=
SUP-B15 MWDGeY5kfGmxbjDBd5NigQ>? NYXYNZh{OTBxMkCg{txO M1L1T|I1KGh? NVPH[4dvemW|dXz0d{BqdiCmZXPy[YF{\WRiUGTFUkBxcG:|cHjvdplt[XSrb36gZZQhfGinIFPLNkB1[XKpZYSgdoV{cWS3ZTDTN|gxKGGwZDDjc45kd22rdHHueEBld3ewcnXneYxifGmxbjDv[kBRXEWQIIDyc5RmcW5iZYjwdoV{e2mxbh?= MmX6NlQ2PjF5OUK=
Nalm6  NXPufW5NSXCxcITvd4l{KEG|c3H5 NUDBRoZOPi9zMDFOwG0> NVHhbI84PDhiaB?= MX;pcoR2[2W|IHHwc5B1d3Orcx?= MWiyOFU3OTd7Mh?=
SUP-B15 NEWxWohCeG:ydH;zbZMhSXO|YYm= MVG2M|ExKM7:TR?= MYq0PEBp NWPVOZBUcW6mdXPld{BieG:ydH;zbZM> M1XzXlI1PTZzN{my
C2C12 Ml;hSpVv[3Srb36gRZN{[Xl? Mkn0N{DPxE1? M3yy[|EzNzJ2L{S4JIg> NEnpdnBqdmirYnn0d{B1cGViZYjwdoV{e2mxbjDv[kBwe3Snb3PsZZN1KGSrZn\ldoVvfGmjdHnvckBu[XKtZYLzJIFv\CCDa4SgdIhwe3Cqb4L5cIF1cW:w NWnKWYtDOjR{OUOwNVE>
Jurkat M2H4PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHO3RYgyNTFyIN88US=> NVHLbHZIPDhiaB?= NUHtNnVzUUN3ME20Mlkh|ryP M4TpclI1OjV|MEK0
CEM-R NYriTHpNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXRZ5VKOS1zMDFOwG0> NHPBVHc1QCCq MnfSTWM2OD12IN88US=> NFfuW5czPDJ3M{CyOC=>
CEM-S NVHSN2RbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWrXdVNNOS1zMDFOwG0> MmnQOFghcA>? MV3JR|UxRTRwNjFOwG0> NFyzZZUzPDJ3M{CyOC=>
MOLT-4 NHnRXY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWSxMVExKM7:TR?= NGDXfog1QCCq Mk[0TWM2OD13Lkeg{txO NX7Pd45zOjR{NUOwNlQ>
PF-382 M1XvSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW[xMVExKM7:TR?= NHz5RXE1QCCq M3XyfWlEPTB;ND61JO69VQ>? NUG0SY9YOjR{NUOwNlQ>
ALL-SIL MmT5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLsVnYyNTFyIN88US=> M{PhXVQ5KGh? NXfhV2c4UUN3ME21Mlch|ryP M2jxNlI1OjV|MEK0
HPB-ALL M2TBbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjp[FkyNTFyIN88US=> MV60PEBp MlnvTWM2OD14LkGg{txO NXrxNnYxOjR{NUOwNlQ>
DND-41 M1jpN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHP2d3kyNTFyIN88US=> NVvjfHB5PDhiaB?= MnHGTWM2OD17IN88US=> Ml7UNlQzPTNyMkS=
ALL-SIL MVfBdI9xfG:|aYOgRZN{[Xl? MlHHOUDPxE1? NEjHPXgzPC92ODDo MYjpcoR2[2W|IHHwc5B1d3Orcx?= NGDZO5MzPDJ3M{CyOC=>
DND-41 MWfBdI9xfG:|aYOgRZN{[Xl? NY\mR3ptPSEQvF2= NFfWfHMzPC92ODDo MUTpcoR2[2W|IHHwc5B1d3Orcx?= M{KwOlI1OjV|MEK0
MOLT-4 MlrSRZBweHSxc3nzJGF{e2G7 NILoOVY2KM7:TR?= NF3CS2wzPC92ODDo NWHYRoVIcW6mdXPld{BieG:ydH;zbZM> NH3pcGozPDJ3M{CyOC=>
U-266 NHHJVHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYKwMVQxKM7:TR?= NVXyNml4PDhiaB?= Ml;NTWM2OD1zOT64JOK2VcLi NFviUZAzPDB6NkS5OC=>
INA-6 NH3PcIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUGwMVQxKM7:TR?= M2PhfVQ5KGh? NHHoTGlKSzVyPUKuOFIhyrWP MUiyOFA5PjR7NB?=
Jeko-1 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml7lNE01OCEQvF2= NF\LNYQ1QCCq NYfrOolWUUN3ME2yMlQhyrWPwrC= MlfqNlQxQDZ2OUS=
Rec-1 Ml;rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWSwMVQxKM7:TR?= MXO0PEBp MlTJTWM2OD1zLkS2JOK2VcLi NXvRU4NROjRyOE[0PVQ>
A549 MmLCSpVv[3Srb36gRZN{[Xl? MY[xNEDPxE1? NF25ZngyOi9{ND:0PEBp MWjpcohq[mm2czDUS2Yu|rJzLXnu[JVk\WRibXnndoF1cW:wIHHu[EBqdn[jc3nvci=> MViyOFAzOzl|OB?=
A549 NIjPTWtHfW6ldHnvckBCe3OjeR?= Ml3GN{DPxE1? MV[0PEBp NVrHRWFEcW6qaXLpeJMhXEeILd8yNU1qdmS3Y3XkJIFkfGm4YYTpc44hd2ZiU33h[EBidmRiZYjwdoV{e2mxbjDv[kBUdmGrbDDhcoQhXHerc4S= NWfrNpNNOjRyMkO5N|g>
S-LAMA84 MVjGeY5kfGmxbjDBd5NigQ>? M2Do[VPDqM7:TR?= NFTwUm4zPCCq MXLEUXNQ M1TKcJJm\HWlZYOgR2szKGGldHn2bZR6 M37DblI1ODF{MUC5
R-LAMA84 MoXRSpVv[3Srb36gRZN{[Xl? NWfIUZo1O8LizszN NV2yPFR5OjRiaB?= Mn3NSG1UVw>? MWDy[YR2[2W|IFPLNkBi[3Srdnn0fS=> NWDiUYNtOjRyMUKxNFk>
S-LAMA84 M4TqZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEP1NWkzNjVvMUCg{txO M3ruT|Q5KGh? M2n2NGROW09? NFHMeWpqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 MmrFNlQxOTJzMEm=
R-LAMA84 NELqdIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TIbFIvPS1zMDFOwG0> NYrRNpd[PDhiaB?= NYDueZB7TE2VTx?= NVP2VnJ3cW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? M33UZlI1ODF{MUC5
A549 M4jUS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HM[lAuOzBizszN NILtWoQ4OiCq NE\Be2NFVVOR MWHJR|UxRTRwMUWg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDjc45k\W62cnH0bY9vKGSncHXu[IVvfGy7 MknaNlM3PTF2NEO=
H1299 NXXjWndyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFy1eZMxNTNyIN88US=> MVK3NkBp MmLWSG1UVw>? NX7tWYJpUUN3ME2xMlgxKM7:TTygbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> NEHpPGgzOzZ3MUS0Ny=>
A549 Ml7BSpVv[3Srb36gRZN{[Xl? M1\OeFEwOTBizszN M2Toc|Q5KGh? NHvSSFhFVVOR MXfs[YFleyC2bzDhJIRwe2VvZHXw[Y5l\W62IHTlZ5Jm[XOnIHnuJG5wfGOqIILldI9zfGW{IHHjeIl3cXS7 MlX5NlM3PTF2NEO=
LNCap NV[yV2VnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXjNE0{OCEQvF2= NX7OO4tpPCCm MXXJR|UxRTRwNUpCpO69VQ>? MVmyNlg{OjNzNh?=
A431  MV3GeY5kfGmxbjDBd5NigQ>? NWDIcVF3OTBizszN MV:zNEBucW5? MkjIZZR1\W63YYTld{BRUTONLVHreE1uXE:UIIPp[45idGmwZx?= MVeyNlM5Pzl6OB?=
H2170  NVnJVWN1TnWwY4Tpc44hSXO|YYm= NU[5dIFYOTBizszN M2DOXVMxKG2rbh?= MVLheJRmdnWjdHXzJHBKO0tvQXv0MY1VV1Jic3nncoFtcW6p M1izR|IzOzh5OUi4
A431  MlXqSpVv[3Srb36gRZN{[Xl? NUDvZmNoOTBizszN MnXtOE0zPCCq NILIcoVmdmijbnPld{BieG:ydH;zbZMhf2m2aDDldoxwfGmwaXK= M4XiTFIzOzh5OUi4
H2170  M17qcmZ2dmO2aX;uJGF{e2G7 NET4OVQyOCEQvF2= NEn5OoQ1NTJ2IHi= NVTiSFBF\W6qYX7j[ZMh[XCxcITvd4l{KHerdHig[ZJtd3Srbnni Mn31NlI{QDd7OEi=

... Click to View More Cell Line Experimental Data

In vivo Oral administration of CX-4945 at 25 mg/kg or 75 mg/kg twice daily displays potent antitumor activity in the BT-474 model, with TGI of 88% and 97%, respectively, and 2 of 9 animals in each group showing more than 50% reduction in tumor size compared with the initial tumor volume. In the BxPC-3 model, CX-4945 treatment at 75 mg/kg twice daily shows 93% TGI with 3 animals having no evidence of tumor remaining at the end of the treatment period. [1] In PC3 xenograft model, administration of CX-4945 at 25 mg/kg, 50 mg/kg, or 75 mg/kg causes tumor growth inhibition with TGI of 19%, 40%, and 86%, respectively. [2]

Protocol

Kinase Assay:[2]
+ Expand

CK2 Kinase Assay:

CX-4945 is added at a volume of 10 μL to a reaction mixture comprising 10 μL of assay dilution buffer (ADB; 20 mM MOPS, pH 7.2, 25 mM β-glycerolphosphate, 5 mM EGTA, 1 mM sodium orthovanadate, and 1 mM dithiothreitol), 10 μL of substrate peptide (RRRDDDSDDD, dissolved in ADB at a concentration of 1 mM), 10 μL of recombinant human CK2 (ααββ-holoenzyme, 25 ng dissolved in ADB). Reactions are initiated by the addition of 10 μL of ATP solution (90% 75 mM MgCl2, 75 μM ATP (final ATP concentration=15 μM) dissolved in ADB; 10% [γ-33P]ATP (stock 1 mCi/100 μL; 3000 Ci/mM and maintained for 10 minutes at 30 °C. The reactions are quenched with 100 μL of 0.75% phosphoric acid and then transferred to and filtered through a phosphocellulose filter plate. After washing each well five times with 0.75% phosphoric acid, the plate is dried under vacuum for 5 minutes and, following the addition of 15 μL of scintillation fluid to each well, the residual radioactivity is measured using a Wallac luminescence counter. The IC50 values are derived from eight concentrations of CX-4945 over a range of 0.0001 μM to 1 μM.
Cell Research:[1]
+ Expand
  • 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, et al.
  • Concentrations: Dissolved in DMSO, final concentrations ~100 μM
  • Incubation Time: 4 days
  • Method: Cells are seeded at a density of 3,000 cells per well 24 hours prior to treatment, in appropriate media, and then treated with various concentrations of CX-4945. Suspensions cells are seeded and treated on the same day. Following 4 days of incubation, Alamar Blue (20 μL, 10% of volume per well) is added and the cells are further incubated at 37 °C for 4-5 hours. Fluorescence with excitation wavelength at 530-560 nm and emission wavelength at 590 nm is measured.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: Female immunocompromised mice CrTac:Ncr-Foxn1nu injected with BxPC-3 or BT-474 cells
  • Formulation: Dissolved in DMSO, and diluted in PBS
  • Dosages: 25 or 75 mg/kg
  • Administration: Oral gavage twice daily
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 16 mg/mL (45.74 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order:
1% CMC Na
For best results, use promptly after mixing.
30mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 349.77
Formula

C19H12ClN3O2

CAS No. 1009820-21-6
Storage powder
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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    C2
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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • 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):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

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|Castlemans Disease|Multiple Myeloma Cylene Pharmaceuticals February 2009 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Frequently Asked Questions

  • Question 1:

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

  • Answer:

    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