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 42 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 MnvKT4lv[XOnIFHzd4F6 MnrpNU82NzFyIN88US=> M1W3N|AvPSCq NFrHRZpFVVOR M4[zVpJm\HWlZYOgR2szKGurbnHz[UBi[3Srdnn0fUBidmRicHzheIVt\XRiYXfndoVo[XSrb36= MknUNlY{QDF2M{e=
HDMEC M1XqPWtqdmG|ZTDBd5NigQ>? M1vibFAvOjVxMD61M|Eh|ryP MnOwNlQhcA>? MmfnSG1UVw>? NGTtNWhz\WS3Y3XzJGNMOiCtaX7hd4Uh[WO2aY\peJktKH[ZRjDlfJBz\XO|aX;uJIFv\CC|ZXPy[ZRqd25? NXjkcGE2OjZ|OEG0N|c>
HDMEC NFu2eFZHfW6ldHnvckBCe3OjeR?= MlvINE4zPS9yLkWvNUDPxE1? MUeyOEBp M1vVWGROW09? NUiwVFJ4emWmdXPld{BmgHC{ZYPzbY9vKG:oIG\DRW0uOSCkdYSgco91KEmFQV2tNS=> NGHWSnYzPjN6MUSzOy=>
HDMEC MXLGeY5kfGmxbjDBd5NigQ>? MXexJO69VQ>? MWWyOEBp MWDEUXNQ NI\SPZFi\m[nY4TzJJN2[mOnbHz1cIFzKGyxY3HsbZpifGmxbjDv[kBPTkGWY{GgZY5lKHCqb4PwbI8ueDZ3 Ml;RNlY{QDF2M{e=
A549  MmnMSpVv[3Srb36gRZN{[Xl? NYm5NnRbOy9zMNMg{txO MkH6OFghcA>? NWfSRYN7e3WycILld5NmeyC2aHWgcYlkem:yaXzsZZIucW6mdXPl[EBmgHC{ZYPzbY9vKG:oIICtSmFM NHviWFIzPjNzOEiwNC=>
HDMEC NYnUN2ozU2mwYYPlJGF{e2G7 MXyxMVUxKM7:TR?= MlPrOUBp NHXZN5VFVVOR NWrJfW05\GWlcnXhd4V{KEONMjDrbY5ie2ViYXP0bZZqfHlid3n0bI92fCCjZn\lZ5RqdmdiY3XscEB3cWGkaXzpeJk> NWnKNGJtOjZzOEm1PFY>
HDMEC MmjDSpVv[3Srb36gRZN{[Xl? NFvyRYg2OCEQvF2= NWD3R|lrOS93IHi= NHrWTpJFVVOR NX7qcG5o\GWlcnXhd4V{KHSqZTDueYNt\WG{IIPp[45idCCxZjDwbI9{eGixconsZZRm\CCyNkWgbY4hXE6ILd8xMZN1cW23bHH0[YQhUESPRVRCpC=> M1z5NlI3OTh7NUi2
HEK293 MmHXT4lv[XOnIFHzd4F6 NF\QSVQxNjYEoN88US=> NHP4WosyPSCvaX6= M2jwc2ROW09? MW\y[YR2[2W|IFPLNkBscW6jc3WgZYN1cX[rdIm= NVLnSG81OjV6OEe2NlY>
Hela M1LRcWtqdmG|ZTDBd5NigQ>? MUKwMlXDqM7:TR?= NIDl[GkyPSCvaX6= M13CdmROW09? NYnUclU1emWmdXPld{BEUzJia3nuZZNmKGGldHn2bZR6 M3\qc|I2QDh5NkK2
LAMA84 M4LV[mtqdmG|ZTDBd5NigQ>? M{j1fVAvPcLizszN MUmxOUBucW5? MULEUXNQ NVLyTpZVemWmdXPld{BEUzJia3nuZZNmKGGldHn2bZR6 NHWxcowzPTh6N{[yOi=>
HEK293 NYf3[oNVTnWwY4Tpc44hSXO|YYm= Mmi4N{DPxE1? NWPQXFNvPSCq M1LjPGROW09? M1rCc2NMOiCyaH;zdIhwenmuYYTld{BmUUZ|ajDheEBU\XJzMke= MYWyOVg5PzZ{Nh?=
UM-SCC1 NUXRdZFYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlK2NE4yNTNyIN88US=> NGDGcGEyNTViZB?= NFTWOWVKSzVyPUSuNUDPxE1? MnzlNlU4QThyNkG=
UM-SCC46 NX\6XmJIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1T0WFAvOS1|MDFOwG0> MX6xMVUh\A>? Mn:zTWM2OD1|LkSg{txO NFH3NGozPTd7OEC2NS=>
UM-SCC1 NGrkZpNHfW6ldHnvckBCe3OjeR?= NYf3c4F7OC53L{SvNVAh|ryP M1\XR|czKGh? MU\kc5dvNXKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCQRj5EvGItKEKlbD3YUEBidmRidYCtdoVofWyjdHXzJJRp\SCneIDy[ZN{cW:wIH;mJJA2OyxicEKxMEBCWC1zIHHu[EBKVC16IHPvcoNmdnS{YYTpc44h\GWyZX7k[Y51dHl? MVuyOVc6QDB4MR?=
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NU-DUL NHnMNIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGThXpg2NTJ3IN88US=> M{HyOFQ5KGh? NGH5N2VqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NWe3O5FKOjV5OEiyOlk>
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Oci Ly 10 NV3CVIs3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\IdlUuOjVizszN MojXOFghcA>? MX7pcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 MXmyOVc5QDJ4OR?=
Oci Ly 1 NF;hXWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfWOU0zPSEQvF2= MY[0PEBp NVmxV|RjcW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? M3PMclI2Pzh6Mk[5
Oci Ly 18 M4PtRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLDOU0zPSEQvF2= NUDvS4NvPDhiaB?= MkPlbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> MW[yOVc5QDJ4OR?=
Oci Ly 19  NEjNelVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWW1MVI2KM7:TR?= NG\WS2E1QCCq NHPobGxqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 M1zKN|I2Pzh6Mk[5
Raji Mn3yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1qxO|UuOjVizszN MUK0PEBp MXHpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 NGH6S3QzPTd6OEK2PS=>
H1299 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTFcol5OS93L{GwJO69VQ>? M{PKfVczKGh? M3PhUolvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> M3;QZlI2PzVyM{C4
Calu-1  M3vTV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVKxM|UwOTBizszN M3fUSVczKGh? NH3sTXNqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NGfHUFAzPTd3MEOwPC=>
H358 NIf1fYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHfIfGEyNzVxMUCg{txO MVW3NkBp NHf0cndqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NGLWOo0zPTd3MEOwPC=>
H1299 NEPIT|RCeG:ydH;zbZMhSXO|YYm= M33mXFExKM7:TR?= MXi3NkBp NVv3PJlzcW6mdXPld{BieG:ydH;zbZM> NVvOZXlyOjV5NUCzNFg>
Calu-1  Mn76RZBweHSxc3nzJGF{e2G7 MlK4NVAh|ryP NIGz[4w4OiCq NF[zcVNqdmS3Y3XzJIFxd3C2b4Ppdy=> MojZNlU4PTB|MEi=
H358 NVvscGlmSXCxcITvd4l{KEG|c3H5 MVSxNEDPxE1? M17je|czKGh? MWTpcoR2[2W|IHHwc5B1d3Orcx?= NWjmVHFzOjV5NUCzNFg>
PC9/GR NWjkVpZ[TnWwY4Tpc44hSXO|YYm= NFzXbJc2KML3TR?= NEj2ZmE1QCCq MUXpcoR2[2W|IHH1eI9xcGGpeR?= MY[yOVQ5PjRyOR?=
PC9/ER NFHnXmxHfW6ldHnvckBCe3OjeR?= NFr5eWs2KML3TR?= MWO0PEBp NVLrUot2cW6mdXPld{BifXSxcHjh[5k> NFXCWIQzPTR6NkSwPS=>
H28 M4\TU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVOwMlAyNTNyIN88US=> NYXWfIF5PzJiaB?= NVPEe45ITE2VTx?= NF;qSGNKSzVyPUeuNkDPxE1? NGHzXI0zPTR{MkC4NS=>
H2052 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33JVFAvODFvM{Cg{txO MV:3NkBp MojNSG1UVw>? MU\JR|UxRTJwMDFOwG0> MkKzNlU1OjJyOEG=
UM-SCC-1 MmTpR4xwdm:pZX7pZ{BCe3OjeR?= MnHiNE42NTVizszN NF:yZlQyPCCm NU\BVZMxTE2VTx?= M{TOTOKhcW6qaXLpeJMh[2yxbn;n[Y5q[yC|dYL2bZZidCCjbnSgd5Bp\XKnIH\vdo1ifGmxbh?= NX\XeoU4OjV|N{mwNVY>
UM-SCC-46 NUnCN3Z1S2yxbn;n[Y5q[yCDc4PhfS=> M3:5TFAvPS13IN88US=> NHXQbm8yPCCm M1HBOmROW09? NWfjb3FPyqCrbnjpZol1eyClbH;uc4dmdmmlIIP1dpZqfmGuIHHu[EB{eGincnWg[o9zdWG2aX;u MoDmNlU{PzlyMU[=
U87-MG MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml[wNU82NzFyIN88US=> NH\DVoEzPC92OD:3NkBp MXrEUXNQ M3[yVYlvcGmkaYTzJINmdGxiZ4Lve5RpKGKxdHigZ49v[2WwdILheIlwdiCjbnSgeIlu\SCmZYDlcoRmdnSueR?= NYnqVoFLOjV{NEG4PVc>
MDA-MB-231 NIj1NVFHfW6ldHnvckBCe3OjeR?= NX[5XJJJOi93L{GwJO69VQ>? NVjJZ4hSPCCq MX7k[YNz\WG|ZYOgeIhmKGOxboP0bZR2fGm4ZTDwbI9{eGixconsZZRqd25ib3[gZo91cCBicD3TOVI6NXB4NTDhcoQheC2VMUK5MWFsfA>? MlzZNlUyPTN5MkW=
MDA-MB-231 Ml;LSpVv[3Srb36gRZN{[Xl? NFvN[3IzNzVxMUCg{txO M1nIPVQhcA>? MYfpcohq[mm2czDz[ZJqdmViNUK5JJBpd3OyaH;yfYxifGmxbjDhcoQhfGinIHX4dJJme3Orb36gc4YhUUxvNjygTWwuQA>? NV3IO21ROjVzNUO3NlU>
ARPE-19 NXfo[5dsU2mwYYPlJGF{e2G7 NFzCNZM2NzFyL{KwJO69VQ>? NF3sd|czPC92ODDo MoP4bY5pcWKrdIOgR2szKGurbnHz[UBi[3Srdnn0fUBifCCjIHPvcoNmdnS{YYTpc44hd2ZiNdMg{txO MnT2NlQ3QDZyOEC=
ARPE-19 MkHPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2ixPVExKM7:TR?= M3fCb|I1NTl4IHi= NUHHNVZUTE2VTx?= M2\uO4lvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk> MlLvNlQ3QDZyOEC=
HCT116  M13Zbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnzpNVAh|ryP MlHrNlQuQTZiaB?= MWXEUXNQ MXzpcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 MXKyOFY5PjB6MB?=
ARPE-19 M1jBVWZ2dmO2aX;uJGF{e2G7 MmHhNVAh|ryP M2LROlQhcA>? M2qzNWROW09? NXTvNXVQ[2G3c3XzJGVTNXO2cnXzd{Bz\XOyb37z[UBwfmW{IITo[UBxNWWLRkNOtUBjemGwY3isJIJ2fCCmb3XzJI5wfCCrbnT1Z4UhS0iRUNMg NXnvXYpIOjR4OE[wPFA>
HCT116  Mn;oSpVv[3Srb36gRZN{[Xl? MnjPNVAh|ryP M3T1XFQhcA>? M3r5ZmROW09? MXLjZZV{\XNiRWKtd5Rz\XO|IILld5BwdnOnIH;2[ZIhfGinIICt[WlHOs7zIHLyZY5kcCxiYoX0JIRw\XNibn;0JIlv\HWlZTDDTG9RyqB? MWOyOFY5PjB6MB?=
HCT116  NU\0VVAxSXCxcITvd4l{KEG|c3H5 NXLGRVNGOTBizszN MVSyOE81QCCq NH[1WWRFVVOR MoLZbY5lfWOnczDhdI9xfG:|aYO= MXeyOFY5PjB6MB?=
Nalm6  NYDKcnpPTnWwY4Tpc44hSXO|YYm= MXyxNE8zOCEQvF2= M2jLT|I1KGh? MYPy[ZN2dHS|IHnuJIRm[3KnYYPl[EBRXEWQIIDoc5NxcG:{eXzheIlwdiCjdDD0bIUhS0t{IIThdodmfCC{ZYPp[JVmKFN|OECgZY5lKGOxbnPvcYl1[W62IHTve45z\We3bHH0bY9vKG:oIGDUSW4heHKxdHXpckBmgHC{ZYPzbY9v MVeyOFU3OTd7Mh?=
SUP-B15 MmrVSpVv[3Srb36gRZN{[Xl? NVX5eHhtOTBxMkCg{txO MYKyOEBp MVTy[ZN2dHS|IHnuJIRm[3KnYYPl[EBRXEWQIIDoc5NxcG:{eXzheIlwdiCjdDD0bIUhS0t{IIThdodmfCC{ZYPp[JVmKFN|OECgZY5lKGOxbnPvcYl1[W62IHTve45z\We3bHH0bY9vKG:oIGDUSW4heHKxdHXpckBmgHC{ZYPzbY9v Mo\UNlQ2PjF5OUK=
Nalm6  Mkn5RZBweHSxc3nzJGF{e2G7 MlrmOk8yOCEQvF2= MVS0PEBp MoH2bY5lfWOnczDhdI9xfG:|aYO= NV7PR5c{OjR3NkG3PVI>
SUP-B15 NGniN3ZCeG:ydH;zbZMhSXO|YYm= M3GwTFYwOTBizszN MXK0PEBp NFPBXopqdmS3Y3XzJIFxd3C2b4Ppdy=> NWPveHdpOjR3NkG3PVI>
C2C12 MYHGeY5kfGmxbjDBd5NigQ>? NGjaSlM{KM7:TR?= M3zmTlEzNzJ2L{S4JIg> NILCTZNqdmirYnn0d{B1cGViZYjwdoV{e2mxbjDv[kBwe3Snb3PsZZN1KGSrZn\ldoVvfGmjdHnvckBu[XKtZYLzJIFv\CCDa4SgdIhwe3Cqb4L5cIF1cW:w NIjQdIUzPDJ7M{CxNS=>
Jurkat M2rzRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHsO3VwOS1zMDFOwG0> Mlv5OFghcA>? MXrJR|UxRTRwOTFOwG0> NVvn[FZUOjR{NUOwNlQ>
CEM-R MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTiWGR4OS1zMDFOwG0> NVXuSnI{PDhiaB?= MYDJR|UxRTRizszN NIXlbZQzPDJ3M{CyOC=>
CEM-S NHnrWnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYGxMVExKM7:TR?= NVPMVmpYPDhiaB?= NW[zRZV[UUN3ME20MlYh|ryP NIjuPFgzPDJ3M{CyOC=>
MOLT-4 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXONU0yOCEQvF2= MWi0PEBp Mn\ITWM2OD13Lkeg{txO Mm\aNlQzPTNyMkS=
PF-382 NFPW[GNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnWZ4xHOS1zMDFOwG0> NGTKbmg1QCCq NGnBPYFKSzVyPUSuOUDPxE1? NX7kT5YzOjR{NUOwNlQ>
ALL-SIL NXHQTHZjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWWxMVExKM7:TR?= NXjNb3BOPDhiaB?= NXP4eVc6UUN3ME21Mlch|ryP NEjFNYgzPDJ3M{CyOC=>
HPB-ALL NUjp[mVoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF;pVJIyNTFyIN88US=> M2S3SVQ5KGh? MX;JR|UxRTZwMTFOwG0> Mk[4NlQzPTNyMkS=
DND-41 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4PjR|EuOTBizszN NXXUU2U3PDhiaB?= MnPrTWM2OD17IN88US=> M13reFI1OjV|MEK0
ALL-SIL MUTBdI9xfG:|aYOgRZN{[Xl? NYr1WoxoPSEQvF2= NIi3UJczPC92ODDo M3ra[4lv\HWlZYOgZZBweHSxc3nz MnXmNlQzPTNyMkS=
DND-41 MnjDRZBweHSxc3nzJGF{e2G7 NXWyTm5mPSEQvF2= MlnQNlQwPDhiaB?= MnK5bY5lfWOnczDhdI9xfG:|aYO= NEWyT|AzPDJ3M{CyOC=>
MOLT-4 M3nJVGFxd3C2b4Ppd{BCe3OjeR?= MV61JO69VQ>? MUCyOE81QCCq NYr6SmMycW6mdXPld{BieG:ydH;zbZM> M4DVNFI1OjV|MEK0
U-266 NV3CeYF7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MonBNE01OCEQvF2= MUK0PEBp MlnZTWM2OD1zOT64JOK2VcLi MnXjNlQxQDZ2OUS=
INA-6 NVnpSFFKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYOwMVQxKM7:TR?= NVHFbVhUPDhiaB?= MV7JR|UxRTJwNEKgxtVO MkHaNlQxQDZ2OUS=
Jeko-1 NV7GXYUyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEj0PFcxNTRyIN88US=> NYK1S5ZOPDhiaB?= NVfXNnZ5UUN3ME2yMlQhyrWPwrC= M2nXWVI1ODh4NEm0
Rec-1 NHTVT|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfGUFAxNTRyIN88US=> M2DvS|Q5KGh? NIHsb2FKSzVyPUGuOFYhyrWPwrC= NUG4[Yl2OjRyOE[0PVQ>
A549 NXSwWWppTnWwY4Tpc44hSXO|YYm= NF;Lc3QyOCEQvF2= NWP5VYVTOTJxMkSvOFghcA>? NHjiZlFqdmirYnn0d{BVT0ZvzsKxMYlv\HWlZXSgcYloemG2aX;uJIFv\CCrbo\hd4lwdg>? NHztclgzPDB{M{mzPC=>
A549 MlSySpVv[3Srb36gRZN{[Xl? MWKzJO69VQ>? MXW0PEBp MWjpcohq[mm2czDUS2Yu|rJzLXnu[JVk\WRiYXP0bZZifGmxbjDv[kBUdWGmIHHu[EBmgHC{ZYPzbY9vKG:oIGPuZYltKGGwZDDUe4l{fA>? M3:0e|I1ODJ|OUO4
S-LAMA84 MnTBSpVv[3Srb36gRZN{[Xl? NWPkdFNqO8LizszN MWeyOEBp MYPEUXNQ MmfndoVlfWOnczDDT|Ih[WO2aY\peJk> NGrPfHEzPDBzMkGwPS=>
R-LAMA84 MXHGeY5kfGmxbjDBd5NigQ>? MWezxsDPxE1? NXL6W5lGOjRiaB?= NX[4XnZMTE2VTx?= NYLpU4J5emWmdXPld{BEUzJiYXP0bZZqfHl? NGLGPIYzPDBzMkGwPS=>
S-LAMA84 Mle4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEmwOIozNjVvMUCg{txO MnjCOFghcA>? MoLWSG1UVw>? MnnmbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> NUXwZ4hlOjRyMUKxNFk>
R-LAMA84 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXiTWczNjVvMUCg{txO M3\pZVQ5KGh? MlK2SG1UVw>? NXTBNGFPcW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? NGj4NYkzPDBzMkGwPS=>
A549 MlrnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTJd5IxNTNyIN88US=> MUK3NkBp NETFfoVFVVOR Mn\jTWM2OD12LkG1JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHigZ49v[2WwdILheIlwdiCmZYDlcoRmdnSueR?= NHP6cIozOzZ3MUS0Ny=>
H1299 NFnDSFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVq0SphOOC1|MDFOwG0> MUS3NkBp MmXxSG1UVw>? MWPJR|UxRTFwOECg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDjc45k\W62cnH0bY9vKGSncHXu[IVvfGy7 M{LnZlI{PjVzNESz
A549 MmTxSpVv[3Srb36gRZN{[Xl? MoDzNU8yOCEQvF2= MlXCOFghcA>? NVfvXlE6TE2VTx?= NVLibYhudGWjZIOgeI8h[SCmb4PlMYRmeGWwZHXueEBl\WO{ZXHz[UBqdiCQb4TjbEBz\XCxcoTldkBi[3Srdnn0fS=> M3\zV|I{PjVzNESz
LNCap NXrNb4F4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHweXlzOC1|MDFOwG0> NVuxSmliPCCm MXLJR|UxRTRwNUpCpO69VQ>? MkKzNlI5OzJ|MU[=
A431  NU\6e5I3TnWwY4Tpc44hSXO|YYm= MVixNEDPxE1? NHm2WIM{OCCvaX6= M3XXWYF1fGWwdXH0[ZMhWEl|Sz3Bb5QudVSRUjDzbYdv[Wyrbne= Ml7JNlI{QDd7OEi=
H2170  NV3MdG1YTnWwY4Tpc44hSXO|YYm= MnXxNVAh|ryP M{nteFMxKG2rbh?= MYHheJRmdnWjdHXzJHBKO0tvQXv0MY1VV1Jic3nncoFtcW6p M3fVO|IzOzh5OUi4
A431  MYrGeY5kfGmxbjDBd5NigQ>? MlHjNVAh|ryP MUG0MVI1KGh? NFfYflhmdmijbnPld{BieG:ydH;zbZMhf2m2aDDldoxwfGmwaXK= NHHTOVEzOjN6N{m4PC=>
H2170  MUXGeY5kfGmxbjDBd5NigQ>? M2ju[|ExKM7:TR?= NVj1RVBuPC1{NDDo Mnnr[Y5p[W6lZYOgZZBweHSxc3nzJJdqfGhiZYLsc5Rqdmmk M3XablIzOzh5OUi4

... 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]
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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]
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  • 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]
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  • 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

Molarity Calculator

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

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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* 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

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    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:

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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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.

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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