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 26 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 NYXLc4RsU2mwYYPlJGF{e2G7 M4HW[VEwPS9zMDFOwG0> NF\5RWMxNjViaB?= MVTEUXNQ MljpdoVlfWOnczDDT|Ihc2mwYYPlJIFkfGm4aYT5JIFv\CCybHH0[YxmfCCjZ3fy[YdifGmxbh?= M2n6UFI3OzhzNEO3
HDMEC M2W2WWtqdmG|ZTDBd5NigQ>? NHmwWpkxNjJ3L{CuOU8yKM7:TR?= MX[yOEBp Mor1SG1UVw>? MVLy[YR2[2W|IFPLNkBscW6jc3WgZYN1cX[rdImsJJZYTiCneIDy[ZN{cW:wIHHu[EB{\WO{ZYTpc44> M2m3b|I3OzhzNEO3
HDMEC Ml3ISpVv[3Srb36gRZN{[Xl? Mle3NE4zPS9yLkWvNUDPxE1? NUTXV4dJOjRiaB?= NG\IZZVFVVOR NYrONmNyemWmdXPld{BmgHC{ZYPzbY9vKG:oIG\DRW0uOSCkdYSgco91KEmFQV2tNS=> MXSyOlM5OTR|Nx?=
HDMEC M{HCOWZ2dmO2aX;uJGF{e2G7 Mni2NUDPxE1? NFTrNmszPCCq NGroeo9FVVOR NUnPU4RM[W[oZXP0d{B{fWKlZXzseYxieiCub3PhcIl7[XSrb36gc4YhVk[DVHOxJIFv\CCyaH;zdIhwNXB4NR?= NXe1UHJUOjZ|OEG0N|c>
A549  MkOzSpVv[3Srb36gRZN{[Xl? MojGN{8yOMLizszN NVfFZWdvPDhiaB?= M3;Pd5N2eHC{ZYPz[ZMhfGinIH3pZ5JweGmubHHyMYlv\HWlZXSg[ZhxemW|c3nvckBw\iCyLV\BTy=> NVva[Zp4OjZ|MUi4NFA>
HDMEC MkD2T4lv[XOnIFHzd4F6 MV6xMVUxKM7:TR?= Ml25OUBp M2jBZmROW09? Mmj4[IVkemWjc3XzJGNMOiCtaX7hd4Uh[WO2aY\peJkhf2m2aH;1eEBi\m[nY4Tpcoch[2WubDD2bYFjcWyrdIm= NVrT[4VMOjZzOEm1PFY>
HDMEC MYLGeY5kfGmxbjDBd5NigQ>? NVXhNWRUPTBizszN NXPHSogyOS93IHi= MkS5SG1UVw>? MYjk[YNz\WG|ZYOgeIhmKG63Y3zlZZIhe2mpbnHsJI9nKHCqb4PwbI9zgWyjdHXkJJA3PSCrbjDUUmYu|rFvc4TpcZVt[XSnZDDISG1GS8Li MW[yOlE5QTV6Nh?=
HEK293 NUSwW2JEU2mwYYPlJGF{e2G7 M1[wPVAvPcLizszN M3;k[FE2KG2rbh?= NXPUO5ZOTE2VTx?= MV\y[YR2[2W|IFPLNkBscW6jc3WgZYN1cX[rdIm= NHHGe5AzPTh6N{[yOi=>
Hela M{ToZWtqdmG|ZTDBd5NigQ>? MmnQNE42yqEQvF2= NIf4bnkyPSCvaX6= M{fRNGROW09? MVHy[YR2[2W|IFPLNkBscW6jc3WgZYN1cX[rdIm= MlqxNlU5QDd4Mk[=
LAMA84 MmfnT4lv[XOnIFHzd4F6 MYGwMlXDqM7:TR?= NVHhU3drOTVibXnu M1qzXmROW09? MXPy[YR2[2W|IFPLNkBscW6jc3WgZYN1cX[rdIm= NUnwfHBlOjV6OEe2NlY>
HEK293 NXrRfWVQTnWwY4Tpc44hSXO|YYm= NI\PbZA{KM7:TR?= NGPXd3U2KGh? MWTEUXNQ M4XpbGNMOiCyaH;zdIhwenmuYYTld{BmUUZ|ajDheEBU\XJzMke= MmTINlU5QDd4Mk[=
UM-SCC1 NHjSfpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFnMZ5kxNjFvM{Cg{txO NGTjWHUyNTViZB?= MonzTWM2OD12LkGg{txO NUjXeGJ7OjV5OUiwOlE>
UM-SCC46 Mn\LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3mybVAvOS1|MDFOwG0> MXKxMVUh\A>? MV\JR|UxRTNwNDFOwG0> MojqNlU4QThyNkG=
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NU-DUL MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;OOU0zPSEQvF2= MV60PEBp MWDpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 M1:weVI2Pzh6Mk[5
Oci Ly 3 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXG1MVI2KM7:TR?= MUC0PEBp MYjpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 MUOyOVc5QDJ4OR?=
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Oci Ly 1 M1\kRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXi1MVI2KM7:TR?= NIXZU5E1QCCq MULpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 M{jEWlI2Pzh6Mk[5
Oci Ly 18 MmLlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1v0dFUuOjVizszN Mk\EOFghcA>? MV\pcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 NEfUNIczPTd6OEK2PS=>
Oci Ly 19  MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH:4d5Q2NTJ3IN88US=> NYroXYlEPDhiaB?= MXvpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 NFfmW4wzPTd6OEK2PS=>
Raji NYrCV4hIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXj1NGRFPS1{NTFOwG0> MXK0PEBp MXfpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 NFTEOpEzPTd6OEK2PS=>
H1299 MkfoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmD1NU82NzFyIN88US=> NWrtSYVpPzJiaB?= MYrpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 NEPBeIIzPTd3MEOwPC=>
Calu-1  MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlS2NU82NzFyIN88US=> M3;Ve|czKGh? M{[wTolvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> NUXWeXJPOjV5NUCzNFg>
H358 NHnPSphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTJRXkyNzVxMUCg{txO M4j5WlczKGh? NEXLb4FqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 M1P3flI2PzVyM{C4
H1299 MmS5RZBweHSxc3nzJGF{e2G7 M4C1OVExKM7:TR?= MmfmO|IhcA>? MoezbY5lfWOnczDhdI9xfG:|aYO= NX24eZlIOjV5NUCzNFg>
Calu-1  MkjDRZBweHSxc3nzJGF{e2G7 M{C1UVExKM7:TR?= Mn3NO|IhcA>? NUTTd5BDcW6mdXPld{BieG:ydH;zbZM> NYLIOFVKOjV5NUCzNFg>
H358 NWPNNHR6SXCxcITvd4l{KEG|c3H5 NHTGc4UyOCEQvF2= Mk\hO|IhcA>? MVTpcoR2[2W|IHHwc5B1d3Orcx?= Mn3pNlU4PTB|MEi=
PC9/GR MXLGeY5kfGmxbjDBd5NigQ>? NXTEfYVpPSEEtV2= MXG0PEBp M13kPIlv\HWlZYOgZZV1d3CqYXf5 NV;5ZZpzOjV2OE[0NFk>
PC9/ER MUnGeY5kfGmxbjDBd5NigQ>? NIjOTI82KML3TR?= NXfETJV6PDhiaB?= NX;HN41mcW6mdXPld{BifXSxcHjh[5k> Ml;WNlU1QDZ2MEm=
H28 NVXyTWl2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLLNE4xOS1|MDFOwG0> M2LGVFczKGh? Mn20SG1UVw>? NGDmXnNKSzVyPUeuNkDPxE1? NVrPVIgyOjV2MkKwPFE>
H2052 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnicHBxOC5yMT2zNEDPxE1? M2PNe|czKGh? NFLNdZRFVVOR MVPJR|UxRTJwMDFOwG0> NEPEbo8zPTR{MkC4NS=>
UM-SCC-1 MoHjR4xwdm:pZX7pZ{BCe3OjeR?= Mn3VNE42NTVizszN Mnv6NVQh\A>? MYLEUXNQ MYtCpIlvcGmkaYTzJINtd26xZ3XubYMhe3W{dnn2ZYwh[W6mIIPwbIVz\SCob4LtZZRqd25? M3SwO|I2Ozd7MEG2
UM-SCC-46 NXHPbnl[S2yxbn;n[Y5q[yCDc4PhfS=> NGPyS4UxNjVvNTFOwG0> NYSzVINXOTRiZB?= NWnleXBMTE2VTx?= NHX1fIrDqGmwaHnibZR{KGOub37v[4VvcWNic4Xyeol3[WxiYX7kJJNxcGW{ZTDmc5Ju[XSrb36= Mnq4NlU{PzlyMU[=
U87-MG M4TCNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYOxM|UwOTBizszN NHi2O4gzPC92OD:3NkBp MXHEUXNQ M4LaNolvcGmkaYTzJINmdGxiZ4Lve5RpKGKxdHigZ49v[2WwdILheIlwdiCjbnSgeIlu\SCmZYDlcoRmdnSueR?= MXGyOVI1OTh7Nx?=
MDA-MB-231 NIXl[VBHfW6ldHnvckBCe3OjeR?= NHjtWHkzNzVxMUCg{txO MUG0JIg> M3LpUIRm[3KnYYPld{B1cGViY3;ud5RqfHW2aY\lJJBpd3OyaH;yfYxifGmxbjDv[kBjd3SqIDDwMXM2OjlvcE[1JIFv\CCyLWOxNlkuSWu2 M2\peFI2OTV|N{K1
MDA-MB-231 MoXrSpVv[3Srb36gRZN{[Xl? NUHxdXRROi93L{GwJO69VQ>? M4mxNlQhcA>? MlPUbY5pcWKrdIOgd4VzcW6nIEWyPUBxcG:|cHjvdplt[XSrb36gZY5lKHSqZTDlfJBz\XO|aX;uJI9nKEmOLU[sJGlNNTh? NEizPVYzPTF3M{eyOS=>
ARPE-19 MoP3T4lv[XOnIFHzd4F6 NVTUeVVYPS9zMD:yNEDPxE1? NGO2N44zPC92ODDo NHuyOpFqdmirYnn0d{BEUzJia3nuZZNmKGGldHn2bZR6KGG2IHGgZ49v[2WwdILheIlwdiCxZjC1xsDPxE1? MYCyOFY5PjB6MB?=
ARPE-19 NEPxcmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDZOVIyOCEQvF2= M4fCbFI1NTl4IHi= NYLrVZJyTE2VTx?= MUXpcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 NEHqbWszPDZ6NkC4NC=>
HCT116  NWrUSIxwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUmxNEDPxE1? MVmyOE06PiCq M4fPNWROW09? M3HHWYlvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk> M4HFblI1Pjh4MEiw
ARPE-19 M4O3UWZ2dmO2aX;uJGF{e2G7 MXGxNEDPxE1? MlvvOEBp NYL5fFFvTE2VTx?= NVXXcYM1[2G3c3XzJGVTNXO2cnXzd{Bz\XOyb37z[UBwfmW{IITo[UBxNWWLRkNOtUBjemGwY3isJIJ2fCCmb3XzJI5wfCCrbnT1Z4UhS0iRUNMg M3Lv[|I1Pjh4MEiw
HCT116  MoD0SpVv[3Srb36gRZN{[Xl? MYixNEDPxE1? MYe0JIg> MUfEUXNQ MVPjZZV{\XNiRWKtd5Rz\XO|IILld5BwdnOnIH;2[ZIhfGinIICt[WlHOs7zIHLyZY5kcCxiYoX0JIRw\XNibn;0JIlv\HWlZTDDTG9RyqB? M{HzXVI1Pjh4MEiw
HCT116  MoqzRZBweHSxc3nzJGF{e2G7 MmLNNVAh|ryP M1nzbFI1NzR6IHi= NGr0OJlFVVOR NIP4NYpqdmS3Y3XzJIFxd3C2b4Ppdy=> MV[yOFY5PjB6MB?=
Nalm6  M2[4ZWZ2dmO2aX;uJGF{e2G7 M4D4bFExNzJyIN88US=> M1zabFI1KGh? MVTy[ZN2dHS|IHnuJIRm[3KnYYPl[EBRXEWQIIDoc5NxcG:{eXzheIlwdiCjdDD0bIUhS0t{IIThdodmfCC{ZYPp[JVmKFN|OECgZY5lKGOxbnPvcYl1[W62IHTve45z\We3bHH0bY9vKG:oIGDUSW4heHKxdHXpckBmgHC{ZYPzbY9v NV\G[FVEOjR3NkG3PVI>
SUP-B15 NXvPVmtxTnWwY4Tpc44hSXO|YYm= NUTMXo9wOTBxMkCg{txO MX:yOEBp NUfXbYZbemW|dXz0d{BqdiCmZXPy[YF{\WRiUGTFUkBxcG:|cHjvdplt[XSrb36gZZQhfGinIFPLNkB1[XKpZYSgdoV{cWS3ZTDTN|gxKGGwZDDjc45kd22rdHHueEBld3ewcnXneYxifGmxbjDv[kBRXEWQIIDyc5RmcW5iZYjwdoV{e2mxbh?= MnnLNlQ2PjF5OUK=
Nalm6  MmHBRZBweHSxc3nzJGF{e2G7 NXT6ZXRCPi9zMDFOwG0> NIXkV4Y1QCCq NUHVVFBVcW6mdXPld{BieG:ydH;zbZM> NXfqOmluOjR3NkG3PVI>
SUP-B15 NXrNU|BUSXCxcITvd4l{KEG|c3H5 MYq2M|ExKM7:TR?= NWTHXItJPDhiaB?= M33Sdolv\HWlZYOgZZBweHSxc3nz NF7HT4UzPDV4MUe5Ni=>
C2C12 NHftWJdHfW6ldHnvckBCe3OjeR?= NEfvSpc{KM7:TR?= MV2xNk8zPC92ODDo M4m1[YlvcGmkaYTzJJRp\SCneIDy[ZN{cW:wIH;mJI9{fGWxY3zhd5Qh\GmoZnXy[Y51cWG2aX;uJI1iemuncoOgZY5lKEGtdDDwbI9{eGixconsZZRqd25? M17jdFI1Ojl|MEGx
Jurkat MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWCxNIs4OS1zMDFOwG0> MUO0PEBp Mnz1TWM2OD12Lkmg{txO MVyyOFI2OzB{NB?=
CEM-R MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXWxMVExKM7:TR?= M1;MZlQ5KGh? NEj3SXdKSzVyPUSg{txO MViyOFI2OzB{NB?=
CEM-S NGnqVWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjiN2t4OS1zMDFOwG0> NUW4UppQPDhiaB?= NWTNWINKUUN3ME20MlYh|ryP M3\HWlI1OjV|MEK0
MOLT-4 M4r3cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLENU0yOCEQvF2= NYnGZ3dmPDhiaB?= MoLMTWM2OD13Lkeg{txO MmriNlQzPTNyMkS=
PF-382 NWjpbIZCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fQNlEuOTBizszN MVS0PEBp NETpWYZKSzVyPUSuOUDPxE1? M2K0TVI1OjV|MEK0
ALL-SIL NIDUeIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVGxMVExKM7:TR?= M2Ty[|Q5KGh? MoDWTWM2OD13Lkeg{txO MYSyOFI2OzB{NB?=
HPB-ALL MlnES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV[2eXdZOS1zMDFOwG0> NGq1XIg1QCCq NGLCRVZKSzVyPU[uNUDPxE1? MWKyOFI2OzB{NB?=
DND-41 NUfVO|ZxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HUXVEuOTBizszN MoHEOFghcA>? MXfJR|UxRTlizszN M1TKSVI1OjV|MEK0
ALL-SIL NYPMcm43SXCxcITvd4l{KEG|c3H5 MlLKOUDPxE1? MWmyOE81QCCq MkPvbY5lfWOnczDhdI9xfG:|aYO= NXLl[npuOjR{NUOwNlQ>
DND-41 MUDBdI9xfG:|aYOgRZN{[Xl? MoPIOUDPxE1? MlHoNlQwPDhiaB?= NFfPW4RqdmS3Y3XzJIFxd3C2b4Ppdy=> M{OySFI1OjV|MEK0
MOLT-4 M325fGFxd3C2b4Ppd{BCe3OjeR?= M3T1S|Uh|ryP NUn0dmk6OjRxNEigbC=> MXzpcoR2[2W|IHHwc5B1d3Orcx?= MXqyOFI2OzB{NB?=
U-266 NHzZeZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvvW3NQOC12MDFOwG0> M{LNRVQ5KGh? Mn7yTWM2OD1zOT64JOK2VcLi MYiyOFA5PjR7NB?=
INA-6 MkDaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{[3dFAuPDBizszN NHTFW3A1QCCq M1vuOWlEPTB;Mj60NkDDvU1? Mlu3NlQxQDZ2OUS=
Jeko-1 NWTac2NWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHnfXkxNTRyIN88US=> NHnOR|Y1QCCq M1;aZmlEPTB;Mj60JOK2VcLi M3TPUlI1ODh4NEm0
Rec-1 M{X4ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHIWGZEOC12MDFOwG0> MXq0PEBp MWjJR|UxRTFwNE[gxtVOyqB? NX3lTFBoOjRyOE[0PVQ>
A549 MXLGeY5kfGmxbjDBd5NigQ>? MVuxNEDPxE1? NFzKeHIyOi9{ND:0PEBp MoPJbY5pcWKrdIOgWGdHNc7{MT3pcoR2[2WmIH3p[5JifGmxbjDhcoQhcW64YYPpc44> NFn2U2kzPDB{M{mzPC=>
A549 MmfPSpVv[3Srb36gRZN{[Xl? Ml61N{DPxE1? M4DoXlQ5KGh? MnnPbY5pcWKrdIOgWGdHNc7{MT3pcoR2[2WmIHHjeIl3[XSrb36gc4YhW22jZDDhcoQh\XiycnXzd4lwdiCxZjDTcoFqdCCjbnSgWJdqe3R? MnPXNlQxOjN7M{i=
S-LAMA84 M1;GOGZ2dmO2aX;uJGF{e2G7 NGDjcYk{yqEQvF2= M4nPV|I1KGh? NXPwR2lvTE2VTx?= NYrrdWxOemWmdXPld{BEUzJiYXP0bZZqfHl? NVXqWphFOjRyMUKxNFk>
R-LAMA84 MXzGeY5kfGmxbjDBd5NigQ>? MmTsN:Kh|ryP MkL2NlQhcA>? NYXuUIl4TE2VTx?= M{fwOpJm\HWlZYOgR2szKGGldHn2bZR6 NUjZbpFbOjRyMUKxNFk>
S-LAMA84 NH:xTGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV[yT3MzOi53LUGwJO69VQ>? M{C2V|Q5KGh? M3frS2ROW09? Mn7TbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> MmrYNlQxOTJzMEm=
R-LAMA84 Ml\MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7lNk42NTFyIN88US=> NF[x[YE1QCCq MWjEUXNQ NHjBV|hqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NFXoT2kzPDBzMkGwPS=>
A549 NEHvUIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofBNE0{OCEQvF2= M2jqUVczKGh? MYnEUXNQ MUHJR|UxRTRwMUWg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDjc45k\W62cnH0bY9vKGSncHXu[IVvfGy7 MViyN|Y2OTR2Mx?=
H1299 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLESHIyOC1|MDFOwG0> NFTjdVU4OiCq MX3EUXNQ NGrFU2ZKSzVyPUGuPFAh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 NVTyeWpqOjN4NUG0OFM>
A549 MoLpSpVv[3Srb36gRZN{[Xl? M3GxPVEwOTBizszN MkDGOFghcA>? MXLEUXNQ M2rQXIxm[WS|IITvJIEh\G:|ZT3k[ZBmdmSnboSg[IVkemWjc3WgbY4hVm:2Y3igdoVxd3K2ZYKgZYN1cX[rdIm= M3vVWVI{PjVzNESz
LNCap M2HiNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7INE0{OCEQvF2= NVTkXIhDPCCm NGLWcYVKSzVyPUSuOVnDqM7:TR?= MX[yNlg{OjNzNh?=
A431  MkPySpVv[3Srb36gRZN{[Xl? NY\uZZJOOTBizszN M4DYR|MxKG2rbh?= MUHheJRmdnWjdHXzJHBKO0tvQXv0MY1VV1Jic3nncoFtcW6p MmfHNlI{QDd7OEi=
H2170  NE\ERYRHfW6ldHnvckBCe3OjeR?= NVTy[VAyOTBizszN NX\obFVkOzBibXnu M{\E[YF1fGWwdXH0[ZMhWEl|Sz3Bb5QudVSRUjDzbYdv[Wyrbne= MoPDNlI{QDd7OEi=
A431  M2DjV2Z2dmO2aX;uJGF{e2G7 MXuxNEDPxE1? NGHWWWU1NTJ2IHi= NGX4eVVmdmijbnPld{BieG:ydH;zbZMhf2m2aDDldoxwfGmwaXK= NV;RSWNwOjJ|OEe5PFg>
H2170  Ml:zSpVv[3Srb36gRZN{[Xl? NV3POXl6OTBizszN MYK0MVI1KGh? MnTM[Y5p[W6lZYOgZZBweHSxc3nzJJdqfGhiZYLsc5Rqdmmk MXiyNlM5Pzl6OB?=

... 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

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 )

  • C1
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    C2
    V2

* 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
NCT02128282 Recruiting Cholangiocarcinoma Senhwa Biosciences Inc. June 2014 Phase 1|Phase 2
NCT01199718 Unknown status Multiple Myeloma Cylene Pharmaceuticals September 2010 Phase 1
NCT01199718 Unknown status Multiple Myeloma Cylene Pharmaceuticals September 2010 Phase 1
NCT00891280 Unknown status Advanced Solid Tumors|Breast Cancer|Inflammatory Breast Cancer|Castleman''s Disease|Multiple Myeloma Cylene Pharmaceuticals February 2009 Phase 1
NCT00891280 Unknown status Advanced Solid Tumors|Breast Cancer|Inflammatory Breast Cancer|Castleman''s 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