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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Cited by 29 Publications

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 M{Cx[GtqdmG|ZTDBd5NigQ>? MX:xM|UwOTBizszN M1jyXVAvPSCq NVLwSGhETE2VTx?= M3fxTpJm\HWlZYOgR2szKGurbnHz[UBi[3Srdnn0fUBidmRicHzheIVt\XRiYXfndoVo[XSrb36= NGXZ[3kzPjN6MUSzOy=>
HDMEC MonyT4lv[XOnIFHzd4F6 MVOwMlI2NzBwNT:xJO69VQ>? NYH5dmlFOjRiaB?= NV3zbIZSTE2VTx?= MnXqdoVlfWOnczDDT|Ihc2mwYYPlJIFkfGm4aYT5MEB3X0ZiZYjwdoV{e2mxbjDhcoQhe2WlcnX0bY9v MnSyNlY{QDF2M{e=
HDMEC M3\0NGZ2dmO2aX;uJGF{e2G7 MVuwMlI2NzBwNT:xJO69VQ>? M4Dp[lI1KGh? M3TLeGROW09? M1j4[5Jm\HWlZYOg[ZhxemW|c3nvckBw\iCYQ1HNMVEh[nW2IH7veEBKS0GPLUG= NV;6Wph{OjZ|OEG0N|c>
HDMEC MXPGeY5kfGmxbjDBd5NigQ>? M1TV[lEh|ryP NGLE[4UzPCCq NFXMcYVFVVOR M2[xZoFn\mWldIOgd5Vj[2WubIXsZZIhdG:lYXzpfoF1cW:wIH;mJG5HSVSlMTDhcoQheGixc4Doc{1xPjV? MnXsNlY{QDF2M{e=
A549  M3r6d2Z2dmO2aX;uJGF{e2G7 MnOyN{8yOMLizszN NFPORWc1QCCq M2PsRpN2eHC{ZYPz[ZMhfGinIH3pZ5JweGmubHHyMYlv\HWlZXSg[ZhxemW|c3nvckBw\iCyLV\BTy=> M3HpNFI3OzF6OECw
HDMEC M2HTTmtqdmG|ZTDBd5NigQ>? M1zsblEuPTBizszN M1LNR|UhcA>? Ml:2SG1UVw>? M3fwWYRm[3KnYYPld{BEUzJia3nuZZNmKGGldHn2bZR6KHerdHjveZQh[W[oZXP0bY5oKGOnbHygeoli[mmuaYT5 MUCyOlE5QTV6Nh?=
HDMEC M1jFOWZ2dmO2aX;uJGF{e2G7 NVXHXnRtPTBizszN Mn;kNU82KGh? NILoN|JFVVOR NGjmVJll\WO{ZXHz[ZMhfGinIH71Z4xm[XJic3nncoFtKG:oIIDoc5NxcG:{eXzheIVlKHB4NTDpckBVVkZvzsGtd5RqdXWuYYTl[EBJTE2HQ9Mg MWiyOlE5QTV6Nh?=
HEK293 MVnLbY5ie2ViQYPzZZk> NYnP[nFWOC53wrFOwG0> NWC1WotjOTVibXnu MWnEUXNQ MnLFdoVlfWOnczDDT|Ihc2mwYYPlJIFkfGm4aYT5 NImxbWozPTh6N{[yOi=>
Hela NWDoNWNVU2mwYYPlJGF{e2G7 MW[wMlXDqM7:TR?= NXroflRJOTVibXnu NF7wRlBFVVOR NVi1VXplemWmdXPld{BEUzJia3nuZZNmKGGldHn2bZR6 MYWyOVg5PzZ{Nh?=
LAMA84 NFHCbG9McW6jc3WgRZN{[Xl? MUWwMlXDqM7:TR?= MlLaNVUhdWmw MofsSG1UVw>? NHrqWY5z\WS3Y3XzJGNMOiCtaX7hd4Uh[WO2aY\peJk> MlHBNlU5QDd4Mk[=
HEK293 MmCwSpVv[3Srb36gRZN{[Xl? MnnLN{DPxE1? NX[xW4NRPSCq MmjnSG1UVw>? MVfDT|IheGixc4Doc5J6dGG2ZYOg[WlHO2piYYSgV4VzOTJ5 NEXmTlAzPTh6N{[yOi=>
UM-SCC1 NXG0fZdRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HGWlAvOS1|MDFOwG0> MkjMNU02KGR? NGD2doJKSzVyPUSuNUDPxE1? Ml24NlU4QThyNkG=
UM-SCC46 NX7DUG5zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3XnNVAvOS1|MDFOwG0> MlP2NU02KGR? MlzpTWM2OD1|LkSg{txO NV:1emdjOjV5OUiwOlE>
UM-SCC1 NIDSPXpHfW6ldHnvckBCe3OjeR?= M{naclAvPS92L{GwJO69VQ>? MoDnO|IhcA>? NEnJbFdld3ewLYLl[5Vt[XSnczD0bIUh\XiycnXzd4lwdiCxZjDOSk3FwEJuIFLjcE1ZVCCjbnSgeZAuemWpdXzheIV{KHSqZTDlfJBz\XO|aX;uJI9nKHB3MzygdFIyNCCDUD2xJIFv\CCLTD24JINwdmOnboTyZZRqd25iZHXw[Y5l\W62bIm= MUiyOVc6QDB4MR?=
UM-SCC46 NHPUOnZHfW6ldHnvckBCe3OjeR?= MV:wMlUwPC9zMDFOwG0> NX3ZZWYxPzJiaB?= MWfkc5dvNXKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCQRj5EvGItKEKlbD3YUEwheDV|LDDwNlEtKEGSLUGgZY5lKHWyLYLl[5Vt[XSnczD0bIUh\XiycnXzd4lwdiCLTD24JINwdmOnboTyZZRqd25iZHXw[Y5l\W62bIm= M2fOdFI2Pzl6ME[x
NU-DUL NWjJeGRET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVi1MVI2KM7:TR?= M2jnS|Q5KGh? M4\YO4lvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> MYWyOVc5QDJ4OR?=
Oci Ly 3 MnPRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PzUFUuOjVizszN MVe0PEBp NYjQTVBjcW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? NX\kRmNSOjV5OEiyOlk>
Oci Ly 10 MorSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY[1MVI2KM7:TR?= MWe0PEBp NV[2ZYNkcW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? MkfoNlU4QDh{Nkm=
Oci Ly 1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnuOU0zPSEQvF2= NW\K[VYyPDhiaB?= MmHwbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> MVqyOVc5QDJ4OR?=
Oci Ly 18 NGDiW45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjqOU0zPSEQvF2= MVq0PEBp NI\0PGFqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 MortNlU4QDh{Nkm=
Oci Ly 19  MoDkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;RXXp2PS1{NTFOwG0> M{DWN|Q5KGh? MUTpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 NWDDdG5zOjV5OEiyOlk>
Raji NIjVSHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYe1MVI2KM7:TR?= NY\rbW5pPDhiaB?= NEn0c|VqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 M1nCVFI2Pzh6Mk[5
H1299 Ml\2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rGW|EwPS9zMDFOwG0> Mln4O|IhcA>? NILL[mhqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 MmrDNlU4PTB|MEi=
Calu-1  NVnLVZd2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvWNU82NzFyIN88US=> M1y4NFczKGh? NHqyTW5qdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NIfDZVIzPTd3MEOwPC=>
H358 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3XlSlEwPS9zMDFOwG0> Ml\JO|IhcA>? NWXV[FVRcW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? NIPIe|czPTd3MEOwPC=>
H1299 M125[2Fxd3C2b4Ppd{BCe3OjeR?= NXfrfZZOOTBizszN MXW3NkBp M2O5Solv\HWlZYOgZZBweHSxc3nz MmnjNlU4PTB|MEi=
Calu-1  M{jrZWFxd3C2b4Ppd{BCe3OjeR?= M1ToT|ExKM7:TR?= MWq3NkBp MmjVbY5lfWOnczDhdI9xfG:|aYO= MWGyOVc2ODNyOB?=
H358 M1fx[GFxd3C2b4Ppd{BCe3OjeR?= M1POdVExKM7:TR?= NXLI[IU1PzJiaB?= NHSyNWxqdmS3Y3XzJIFxd3C2b4Ppdy=> NEf0dnozPTd3MEOwPC=>
PC9/GR NHrGWZpHfW6ldHnvckBCe3OjeR?= NGCyZ282KML3TR?= NIDLRYo1QCCq MUPpcoR2[2W|IHH1eI9xcGGpeR?= M4rTRVI2PDh4NEC5
PC9/ER NXqwfY1TTnWwY4Tpc44hSXO|YYm= Mn:zOUDDvU1? Mn6yOFghcA>? NVnXW|E4cW6mdXPld{BifXSxcHjh[5k> Moj1NlU1QDZ2MEm=
H28 NUXyTpJZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mli5NE4xOS1|MDFOwG0> MWW3NkBp NVP2[Vh{TE2VTx?= Ml7wTWM2OD15LkKg{txO MUCyOVQzOjB6MR?=
H2052 Mli2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;uU|AvODFvM{Cg{txO NHLKTIc4OiCq M3LuO2ROW09? M1PzXWlEPTB;Mj6wJO69VQ>? M4XUNFI2PDJ{MEix
UM-SCC-1 NX7RTIRNS2yxbn;n[Y5q[yCDc4PhfS=> Ml;QNE42NTVizszN NWPGe3JKOTRiZB?= MVHEUXNQ NYXxUlAzyqCrbnjpZol1eyClbH;uc4dmdmmlIIP1dpZqfmGuIHHu[EB{eGincnWg[o9zdWG2aX;u M2f5WFI2Ozd7MEG2
UM-SCC-46 NIrBT3JEdG:wb3flcolkKEG|c3H5 NHvLW4ExNjVvNTFOwG0> MXqxOEBl NV7MO3F2TE2VTx?= MVxCpIlvcGmkaYTzJINtd26xZ3XubYMhe3W{dnn2ZYwh[W6mIIPwbIVz\SCob4LtZZRqd25? M3PMdFI2Ozd7MEG2
U87-MG MojqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVixM|UwOTBizszN MkDDNlQwPDhxN{KgbC=> NFTsd29FVVOR MofjbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[m:2aDDjc45k\W62cnH0bY9vKGGwZDD0bY1mKGSncHXu[IVvfGy7 NHzidI0zPTJ2MUi5Oy=>
MDA-MB-231 NXrsUpV[TnWwY4Tpc44hSXO|YYm= NFS2[FgzNzVxMUCg{txO NV25RWVOPCCq NYnGO|Rv\GWlcnXhd4V{KHSqZTDjc45{fGm2dYTpeoUheGixc4Doc5J6dGG2aX;uJI9nKGKxdHigJJAuWzV{OT3wOlUh[W6mIICtV|EzQS2Da4S= MkDtNlUyPTN5MkW=
MDA-MB-231 NFXRcW1HfW6ldHnvckBCe3OjeR?= M1HGeFIwPS9zMDFOwG0> MUK0JIg> NGXyfphqdmirYnn0d{B{\XKrbnWgOVI6KHCqb4PwbI9zgWyjdHnvckBidmRidHjlJIV5eHKnc4Ppc44hd2ZiSVytOkwhUUxvOB?= MWGyOVE2Ozd{NR?=
ARPE-19 NXH0W3B7U2mwYYPlJGF{e2G7 MlvpOU8yOC9{MDFOwG0> MV6yOE81QCCq NFfwWGFqdmirYnn0d{BEUzJia3nuZZNmKGGldHn2bZR6KGG2IHGgZ49v[2WwdILheIlwdiCxZjC1xsDPxE1? MWiyOFY5PjB6MB?=
ARPE-19 MoDkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGfCT5QyOCEQvF2= NGntO2ozPC17NjDo M4TWUGROW09? NIGyVphqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 NF7ZNIkzPDZ6NkC4NC=>
HCT116  MnTIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvPS3cyOCEQvF2= Ml3tNlQuQTZiaB?= NWrxVY1kTE2VTx?= NGC0ZpBqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 NFrXRVUzPDZ6NkC4NC=>
ARPE-19 MnmxSpVv[3Srb36gRZN{[Xl? M3\Pe|ExKM7:TR?= M4niOlQhcA>? M4DTWWROW09? NELQUZZk[XW|ZYOgSXIue3S{ZYPzJJJme3CxboPlJI93\XJidHjlJJAu\UmIMt8xJIJz[W6laDygZpV1KGSxZYOgco91KGmwZIXj[UBEUE:SwrC= NIHkc3QzPDZ6NkC4NC=>
HCT116  M3rSS2Z2dmO2aX;uJGF{e2G7 MWGxNEDPxE1? MknZOEBp NYjCb4NqTE2VTx?= NYHUNlhj[2G3c3XzJGVTNXO2cnXzd{Bz\XOyb37z[UBwfmW{IITo[UBxNWWLRkNOtUBjemGwY3isJIJ2fCCmb3XzJI5wfCCrbnT1Z4UhS0iRUNMg NXTGc3RCOjR4OE[wPFA>
HCT116  M1H2RmFxd3C2b4Ppd{BCe3OjeR?= MY[xNEDPxE1? NYCwcW5pOjRxNEigbC=> NULDRXJqTE2VTx?= NVjmOG5PcW6mdXPld{BieG:ydH;zbZM> NI\zcIQzPDZ6NkC4NC=>
Nalm6  MlPJSpVv[3Srb36gRZN{[Xl? MUKxNE8zOCEQvF2= M{TOfFI1KGh? MnrmdoV{fWy2czDpckBl\WO{ZXHz[YQhWFSHTjDwbI9{eGixconsZZRqd25iYYSgeIhmKEONMjD0ZZJo\XRicnXzbYR2\SCVM{iwJIFv\CClb37jc41qfGGwdDDkc5dvemWpdXzheIlwdiCxZjDQWGVPKHC{b4TlbY4h\XiycnXzd4lwdg>? NI\rbJIzPDV4MUe5Ni=>
SUP-B15 MlvHSpVv[3Srb36gRZN{[Xl? M3HNVFExNzJyIN88US=> M1vGW|I1KGh? NUXSem5HemW|dXz0d{BqdiCmZXPy[YF{\WRiUGTFUkBxcG:|cHjvdplt[XSrb36gZZQhfGinIFPLNkB1[XKpZYSgdoV{cWS3ZTDTN|gxKGGwZDDjc45kd22rdHHueEBld3ewcnXneYxifGmxbjDv[kBRXEWQIIDyc5RmcW5iZYjwdoV{e2mxbh?= NVvnN40yOjR3NkG3PVI>
Nalm6  NGK4O3dCeG:ydH;zbZMhSXO|YYm= MVe2M|ExKM7:TR?= MmC4OFghcA>? Mor5bY5lfWOnczDhdI9xfG:|aYO= NEPLXpgzPDV4MUe5Ni=>
SUP-B15 NYL1RVM1SXCxcITvd4l{KEG|c3H5 NWfYdnFjPi9zMDFOwG0> NV7SZY1SPDhiaB?= MljvbY5lfWOnczDhdI9xfG:|aYO= NVPEPVhtOjR3NkG3PVI>
C2C12 NELPPJlHfW6ldHnvckBCe3OjeR?= MmflN{DPxE1? M3ixOlEzNzJ2L{S4JIg> MYfpcohq[mm2czD0bIUh\XiycnXzd4lwdiCxZjDvd5Rmd2OuYYP0JIRq\m[ncnXueIlifGmxbjDtZZJs\XK|IHHu[EBCc3RicHjvd5Bpd3K7bHH0bY9v MXyyOFI6OzBzMR?=
Jurkat MonPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2GzNlEuOTBizszN NUXvR4ZNPDhiaB?= MW\JR|UxRTRwOTFOwG0> MnLnNlQzPTNyMkS=
CEM-R NEXTUm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3OwZ|EuOTBizszN NHW1OXg1QCCq M1TIS2lEPTB;NDFOwG0> MmL5NlQzPTNyMkS=
CEM-S NXLVO5AyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnq4NU0yOCEQvF2= MnmzOFghcA>? M2XFd2lEPTB;ND62JO69VQ>? MX[yOFI2OzB{NB?=
MOLT-4 Mn[wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrPSpU4OS1zMDFOwG0> NEm3Rnk1QCCq NIe3[pBKSzVyPUWuO{DPxE1? NIG3eXMzPDJ3M{CyOC=>
PF-382 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUCyNpZDOS1zMDFOwG0> MUe0PEBp NIn0eWdKSzVyPUSuOUDPxE1? MYOyOFI2OzB{NB?=
ALL-SIL NFXTSHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\FOlZzOS1zMDFOwG0> NGL3SVI1QCCq NW\1clFvUUN3ME21Mlch|ryP M1HvU|I1OjV|MEK0
HPB-ALL NYCxdFRpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELWbHcyNTFyIN88US=> NFW4fnk1QCCq M2XrSWlEPTB;Nj6xJO69VQ>? MVmyOFI2OzB{NB?=
DND-41 M1fmV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLUeFhTOS1zMDFOwG0> NFLTPGo1QCCq MkfITWM2OD17IN88US=> MoKyNlQzPTNyMkS=
ALL-SIL Mnq3RZBweHSxc3nzJGF{e2G7 MYO1JO69VQ>? M3\iPFI1NzR6IHi= NWmxWmhqcW6mdXPld{BieG:ydH;zbZM> MkDaNlQzPTNyMkS=
DND-41 MWfBdI9xfG:|aYOgRZN{[Xl? NYn2U|F4PSEQvF2= MYiyOE81QCCq Mni5bY5lfWOnczDhdI9xfG:|aYO= NWLr[|BoOjR{NUOwNlQ>
MOLT-4 NV\pTlltSXCxcITvd4l{KEG|c3H5 NHP2PIE2KM7:TR?= Moi5NlQwPDhiaB?= M2ewSIlv\HWlZYOgZZBweHSxc3nz NUHTTWtJOjR{NUOwNlQ>
U-266 M1W3Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXmwMVQxKM7:TR?= NVG0fVJ5PDhiaB?= NITxNIpKSzVyPUG5MlghyrWPwrC= M3rCWlI1ODh4NEm0
INA-6 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWCwMVQxKM7:TR?= NV;CUFVUPDhiaB?= MV\JR|UxRTJwNEKgxtVO MVGyOFA5PjR7NB?=
Jeko-1 M3HaZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlWwNE01OCEQvF2= M4PWSlQ5KGh? M2DsNGlEPTB;Mj60JOK2VcLi Mmq1NlQxQDZ2OUS=
Rec-1 M3e4cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTFbGwxNTRyIN88US=> M{LQUlQ5KGh? M2H4bGlEPTB;MT60OkDDvU4EoB?= NHHYWpczPDB6NkS5OC=>
A549 NWLtRpZXTnWwY4Tpc44hSXO|YYm= NIH1fmUyOCEQvF2= MlzHNVIwOjRxNEigbC=> NYn2PIxpcW6qaXLpeJMhXEeILd8yNU1qdmS3Y3XkJI1q\3KjdHnvckBidmRiaX72ZZNqd25? MYGyOFAzOzl|OB?=
A549 MnW1SpVv[3Srb36gRZN{[Xl? Moi5N{DPxE1? MV60PEBp NUDRXI1TcW6qaXLpeJMhXEeILd8yNU1qdmS3Y3XkJIFkfGm4YYTpc44hd2ZiU33h[EBidmRiZYjwdoV{e2mxbjDv[kBUdmGrbDDhcoQhXHerc4S= NYL4[YVjOjRyMkO5N|g>
S-LAMA84 MUTGeY5kfGmxbjDBd5NigQ>? NETPV2o{yqEQvF2= M2jTfVI1KGh? M2HiNWROW09? M2P4fJJm\HWlZYOgR2szKGGldHn2bZR6 NHvSdWczPDBzMkGwPS=>
R-LAMA84 NUKz[pc3TnWwY4Tpc44hSXO|YYm= NHPXd3g{yqEQvF2= MXuyOEBp NInIZWRFVVOR MUjy[YR2[2W|IFPLNkBi[3Srdnn0fS=> NIPJZYozPDBzMkGwPS=>
S-LAMA84 MkLpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGfSUGMzNjVvMUCg{txO NV\MRYZVPDhiaB?= NETRVI5FVVOR NEjDdVVqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 MVyyOFAyOjFyOR?=
R-LAMA84 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHTO2diOi53LUGwJO69VQ>? MVG0PEBp MmPLSG1UVw>? MU\pcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 NV\iZYp5OjRyMUKxNFk>
A549 MkXxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLTcXl7OC1|MDFOwG0> NWjtO2doPzJiaB?= NGrQNItFVVOR MUfJR|UxRTRwMUWg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDjc45k\W62cnH0bY9vKGSncHXu[IVvfGy7 Mn\0NlM3PTF2NEO=
H1299 M4DuR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY[wMVMxKM7:TR?= MknnO|IhcA>? M{fNT2ROW09? M4\Fe2lEPTB;MT64NEDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJINwdmOnboTyZZRqd25iZHXw[Y5l\W62bIm= MW[yN|Y2OTR2Mx?=
A549 NUDXc3pPTnWwY4Tpc44hSXO|YYm= NIm4dZAyNzFyIN88US=> Mo\NOFghcA>? NEPUNXpFVVOR NIT3Xnpt\WGmczD0c{BiKGSxc3Wt[IVx\W6mZX70JIRm[3KnYYPlJIlvKE6xdHPoJJJmeG:{dHXyJIFkfGm4aYT5 NEXjRogzOzZ3MUS0Ny=>
LNCap NYfTbIpjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml[yNE0{OCEQvF2= NVjwNpNsPCCm M325SWlEPTB;ND61PeKh|ryP M4\5UVIzQDN{M{G2
A431  NU\5TVlNTnWwY4Tpc44hSXO|YYm= M4jtdlExKM7:TR?= MUmzNEBucW5? NYjCemhI[XS2ZX71ZZRmeyCSSUPLMWFsfC2vVF;SJJNq\26jbHnu[y=> M4nPXlIzOzh5OUi4
H2170  M2rKeGZ2dmO2aX;uJGF{e2G7 NEm3WWMyOCEQvF2= M4nTSFMxKG2rbh?= M4G2WIF1fGWwdXH0[ZMhWEl|Sz3Bb5QudVSRUjDzbYdv[Wyrbne= Mk\rNlI{QDd7OEi=
A431  NGHnSGxHfW6ldHnvckBCe3OjeR?= NHv6NWgyOCEQvF2= M4fUbVQuOjRiaB?= NIH4W3JmdmijbnPld{BieG:ydH;zbZMhf2m2aDDldoxwfGmwaXK= NV[xWGl6OjJ|OEe5PFg>
H2170  NWrlTpB{TnWwY4Tpc44hSXO|YYm= MWGxNEDPxE1? NVy5e4UxPC1{NDDo MX\lcohidmOnczDhdI9xfG:|aYOge4l1cCCncnzveIlvcWJ? NY[5SmprOjJ|OEe5PFg>

... 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
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(Data is from Selleck tests instead of citations):
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
in solvent
Synonyms N/A

Bio Calculators

Molarity Calculator

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

Mass (mg) = Concentration (mM) × Volume (mL) × 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

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

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

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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).

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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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)
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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