CX-4945 (Silmitasertib)

Catalog No.S2248

CX-4945 (Silmitasertib) Chemical Structure

Molecular Weight(MW): 349.77

CX-4945 (Silmitasertib) 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.

Size Price Stock Quantity  
In DMSO USD 291 In stock
USD 170 In stock
USD 320 In stock

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4 Customer Reviews

  • Nat Commun 2014 5, 3393. CX-4945 (Silmitasertib) 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. CX-4945 (Silmitasertib) purchased from Selleck.

  • Cell Signal 2014 26(7), 1567-75. CX-4945 (Silmitasertib) purchased from Selleck.

    Cell Signal 2014 26(7), 1567-75. CX-4945 (Silmitasertib) purchased from Selleck.

Purity & Quality Control

Choose Selective Casein Kinase Inhibitors

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description CX-4945 (Silmitasertib) 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 NHOzeodMcW6jc3WgRZN{[Xl? NWjmZmxkOS93L{GwJO69VQ>? NEXSZWExNjViaB?= NF[xNW5FVVOR NIjMcmFz\WS3Y3XzJGNMOiCtaX7hd4Uh[WO2aY\peJkh[W6mIIDsZZRmdGW2IHHn[5Jm\2G2aX;u NGjSWpgzPjN6MUSzOy=>
HDMEC NIfreHlMcW6jc3WgRZN{[Xl? MYewMlI2NzBwNT:xJO69VQ>? NVfaZ5pvOjRiaB?= NWrMZnJKTE2VTx?= NGjBTpVz\WS3Y3XzJGNMOiCtaX7hd4Uh[WO2aY\peJktKH[ZRjDlfJBz\XO|aX;uJIFv\CC|ZXPy[ZRqd25? MX[yOlM5OTR|Nx?=
HDMEC NXnRVGdQTnWwY4Tpc44hSXO|YYm= M4n2[VAvOjVxMD61M|Eh|ryP NH35PGkzPCCq MX\EUXNQ MlSwdoVlfWOnczDlfJBz\XO|aX;uJI9nKF[FQV2tNUBjfXRibn;0JGlESU1vMR?= MVqyOlM5OTR|Nx?=
HDMEC M3v4UWZ2dmO2aX;uJGF{e2G7 M162bVEh|ryP M{TKRlI1KGh? NWDVPYFOTE2VTx?= M3fZ[YFn\mWldIOgd5Vj[2WubIXsZZIhdG:lYXzpfoF1cW:wIH;mJG5HSVSlMTDhcoQheGixc4Doc{1xPjV? MV[yOlM5OTR|Nx?=
A549  NIn4T5JHfW6ldHnvckBCe3OjeR?= NITkTW4{NzFywrFOwG0> MUi0PEBp NXfMNFkxe3WycILld5NmeyC2aHWgcYlkem:yaXzsZZIucW6mdXPl[EBmgHC{ZYPzbY9vKG:oIICtSmFM MYOyOlMyQDhyMB?=
HDMEC NWLQ[m5yU2mwYYPlJGF{e2G7 M2P4NVEuPTBizszN NUX5TodJPSCq NY\tXmdzTE2VTx?= NFrGd4hl\WO{ZXHz[ZMhS0t{IHvpcoF{\SCjY4Tpeol1gSC5aYToc5V1KGGoZnXjeIlv\yClZXzsJJZq[WKrbHn0fS=> NUC4UmRyOjZzOEm1PFY>
HDMEC Mn\YSpVv[3Srb36gRZN{[Xl? M2OxN|UxKM7:TR?= NF;Gc5EyNzViaB?= NEH1[mhFVVOR Mmfy[IVkemWjc3XzJJRp\SCwdXPs[YFzKHOrZ37hcEBw\iCyaH;zdIhwenmuYYTl[EBxPjViaX6gWG5HNc7zLYP0bY12dGG2ZXSgTGROTUQEoB?= NWHsWYY6OjZzOEm1PFY>
HEK293 NVfYSms1U2mwYYPlJGF{e2G7 NFrGeI0xNjYEoN88US=> M3O5bVE2KG2rbh?= Ml;1SG1UVw>? MYTy[YR2[2W|IFPLNkBscW6jc3WgZYN1cX[rdIm= M4\JNFI2QDh5NkK2
Hela Mke3T4lv[XOnIFHzd4F6 NXTSNlg3OC53wrFOwG0> MnTJNVUhdWmw NVj5OY86TE2VTx?= NGDENopz\WS3Y3XzJGNMOiCtaX7hd4Uh[WO2aY\peJk> NYHHVpVzOjV6OEe2NlY>
LAMA84 MWTLbY5ie2ViQYPzZZk> NFrldHIxNjYEoN88US=> MXuxOUBucW5? NF7KWoZFVVOR MnTOdoVlfWOnczDDT|Ihc2mwYYPlJIFkfGm4aYT5 NGT5bHkzPTh6N{[yOi=>
HEK293 NIjOS3dHfW6ldHnvckBCe3OjeR?= NV20O|hpOyEQvF2= MmTiOUBp NYjib3d[TE2VTx?= MoPPR2szKHCqb4PwbI9zgWyjdHXzJIVKTjOsIHH0JHNmejF{Nx?= MXmyOVg5PzZ{Nh?=
UM-SCC1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mkm4NE4yNTNyIN88US=> MWmxMVUh\A>? NHSxUHRKSzVyPUSuNUDPxE1? NVzlZXJlOjV5OUiwOlE>
UM-SCC46 M1LpXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWKwMlEuOzBizszN MljwNU02KGR? MofYTWM2OD1|LkSg{txO NY[1V3BVOjV5OUiwOlE>
UM-SCC1 Ml\vSpVv[3Srb36gRZN{[Xl? MlS4NE42NzRxMUCg{txO NFLXN244OiCq MUnkc5dvNXKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCQRj5EvGItKEKlbD3YUEBidmRidYCtdoVofWyjdHXzJJRp\SCneIDy[ZN{cW:wIH;mJJA2OyxicEKxMEBCWC1zIHHu[EBKVC16IHPvcoNmdnS{YYTpc44h\GWyZX7k[Y51dHl? NX\xcYtYOjV5OUiwOlE>
UM-SCC46 NHHkdJNHfW6ldHnvckBCe3OjeR?= MmLCNE42NzRxMUCg{txO NXPLcWs2PzJiaB?= NXvBOpEy\G:5bj3y[Yd2dGG2ZYOgeIhmKGW6cILld5Nqd25ib3[gUmYuzLiELDDCZ4wuYExuIIC1N{wheDJzLDDBVE0yKGGwZDD1dE1z\We3bHH0[ZMhfGinIHX4dJJme3Orb36gTWwuQCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NHTrblgzPTd7OEC2NS=>
NU-DUL MnHqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXe2PFhZPS1{NTFOwG0> NYrybpQyPDhiaB?= MV3pcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 MljxNlU4QDh{Nkm=
Oci Ly 3 MkH3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXS1MVI2KM7:TR?= MlOyOFghcA>? MorzbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> NFvSPFYzPTd6OEK2PS=>
Oci Ly 10 NFv1T5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTzVoVGPS1{NTFOwG0> MUe0PEBp M4DKe4lvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> MYSyOVc5QDJ4OR?=
Oci Ly 1 MluyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX[1MVI2KM7:TR?= NX\DbotmPDhiaB?= NHH3VY5qdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 M3f2R|I2Pzh6Mk[5
Oci Ly 18 NXTsVWkxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1j1Z|UuOjVizszN MnKxOFghcA>? MnT6bY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> MlX1NlU4QDh{Nkm=
Oci Ly 19  NEXVXIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3rT4J3PS1{NTFOwG0> NH7yT4Q1QCCq NGLFZYlqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 MkTtNlU4QDh{Nkm=
Raji MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHsSnRiPS1{NTFOwG0> M2jze|Q5KGh? Ml32bY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> NIr4TWQzPTd6OEK2PS=>
H1299 NWjPbZN6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjRNU82NzFyIN88US=> M2D0c|czKGh? NVfZVFN4cW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? NYn6WJY6OjV5NUCzNFg>
Calu-1  M3HqXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\iTFRFOS93L{GwJO69VQ>? M2izUFczKGh? NGmyRoNqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NU\ZbJY{OjV5NUCzNFg>
H358 NEjEcWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWKxM|UwOTBizszN Ml7VO|IhcA>? NYHydHRkcW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? NFL4NlYzPTd3MEOwPC=>
H1299 NF7kS2lCeG:ydH;zbZMhSXO|YYm= M2[3eVExKM7:TR?= M4ezUlczKGh? MmTmbY5lfWOnczDhdI9xfG:|aYO= NXrNeG1FOjV5NUCzNFg>
Calu-1  NHK3N4RCeG:ydH;zbZMhSXO|YYm= NVLiNnN1OTBizszN NYruc3c1PzJiaB?= NU\WfJh1cW6mdXPld{BieG:ydH;zbZM> MVKyOVc2ODNyOB?=
H358 NYDv[W9WSXCxcITvd4l{KEG|c3H5 NEP1NW0yOCEQvF2= M2Dqc|czKGh? MUPpcoR2[2W|IHHwc5B1d3Orcx?= MVKyOVc2ODNyOB?=
PC9/GR M4WySWZ2dmO2aX;uJGF{e2G7 MkW5OUDDvU1? NYrwW3QyPDhiaB?= MkXPbY5lfWOnczDheZRweGijZ4m= MkmxNlU1QDZ2MEm=
PC9/ER NEjFTVBHfW6ldHnvckBCe3OjeR?= M4Ow[FUhyrWP MlrhOFghcA>? NETET3pqdmS3Y3XzJIF2fG:yaHHnfS=> NILWWVczPTR6NkSwPS=>
H28 MofDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfiNE4xOS1|MDFOwG0> NV;pSmgxPzJiaB?= M3jueWROW09? MoPxTWM2OD15LkKg{txO NHfUT5IzPTR{MkC4NS=>
H2052 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TtWlAvODFvM{Cg{txO NFXrclU4OiCq MlOwSG1UVw>? MVjJR|UxRTJwMDFOwG0> MV6yOVQzOjB6MR?=
UM-SCC-1 MXvDcI9vd2enbnnjJGF{e2G7 M1rZNVAvPS13IN88US=> MV:xOEBl NV\nWW9OTE2VTx?= M{D0NeKhcW6qaXLpeJMh[2yxbn;n[Y5q[yC|dYL2bZZidCCjbnSgd5Bp\XKnIH\vdo1ifGmxbh?= NFvnO2kzPTN5OUCxOi=>
UM-SCC-46 NUfsTVRjS2yxbn;n[Y5q[yCDc4PhfS=> NIXY[5MxNjVvNTFOwG0> NX3VVJZoOTRiZB?= MnvPSG1UVw>? MUZCpIlvcGmkaYTzJINtd26xZ3XubYMhe3W{dnn2ZYwh[W6mIIPwbIVz\SCob4LtZZRqd25? M2W1dlI2Ozd7MEG2
U87-MG MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVGxM|UwOTBizszN M2jXVFI1NzR6L{eyJIg> M3i5b2ROW09? MnfsbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[m:2aDDjc45k\W62cnH0bY9vKGGwZDD0bY1mKGSncHXu[IVvfGy7 NV25[I5HOjV{NEG4PVc>
MDA-MB-231 MnTYSpVv[3Srb36gRZN{[Xl? MkTyNk82NzFyIN88US=> M3zFVlQhcA>? NH7EOYdl\WO{ZXHz[ZMhfGinIHPvcpN1cXS3dHn2[UBxcG:|cHjvdplt[XSrb36gc4Yh[m:2aDCgdE1UPTJ7LYC2OUBidmRicD3TNVI6NUGtdB?= MWCyOVE2Ozd{NR?=
MDA-MB-231 NX;WNWgzTnWwY4Tpc44hSXO|YYm= MYCyM|UwOTBizszN NUjsZXh{PCCq NFS2Z4lqdmirYnn0d{B{\XKrbnWgOVI6KHCqb4PwbI9zgWyjdHnvckBidmRidHjlJIV5eHKnc4Ppc44hd2ZiSVytOkwhUUxvOB?= MmO2NlUyPTN5MkW=
ARPE-19 NV\FcnN3U2mwYYPlJGF{e2G7 MVS1M|ExNzJyIN88US=> M1jrPVI1NzR6IHi= NIX1OlJqdmirYnn0d{BEUzJia3nuZZNmKGGldHn2bZR6KGG2IHGgZ49v[2WwdILheIlwdiCxZjC1xsDPxE1? NFu3XmczPDZ6NkC4NC=>
ARPE-19 MoHSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVWxNEDPxE1? NYrneFU4OjRvOU[gbC=> NYfkXXZpTE2VTx?= MUfpcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 MlvRNlQ3QDZyOEC=
HCT116  Mlu1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFPEZpEyOCEQvF2= MUOyOE06PiCq M3vVNWROW09? NWTDWJlPcW6qaXLpeJMh[2WubDDndo94fGhidHnt[UBl\XCnbnTlcpRtgQ>? NWfCSYs4OjR4OE[wPFA>
ARPE-19 MYnGeY5kfGmxbjDBd5NigQ>? NX7zeYZwOTBizszN M3vOW|QhcA>? MXfEUXNQ MXvjZZV{\XNiRWKtd5Rz\XO|IILld5BwdnOnIH;2[ZIhfGinIICt[WlHOs7zIHLyZY5kcCxiYoX0JIRw\XNibn;0JIlv\HWlZTDDTG9RyqB? M3n2TlI1Pjh4MEiw
HCT116  MVTGeY5kfGmxbjDBd5NigQ>? NXPTTIFqOTBizszN NGHFbY41KGh? NEnvbpZFVVOR NYfi[FE1[2G3c3XzJGVTNXO2cnXzd{Bz\XOyb37z[UBwfmW{IITo[UBxNWWLRkNOtUBjemGwY3isJIJ2fCCmb3XzJI5wfCCrbnT1Z4UhS0iRUNMg MYCyOFY5PjB6MB?=
HCT116  M2XqTGFxd3C2b4Ppd{BCe3OjeR?= Mn73NVAh|ryP NHzLcWYzPC92ODDo NWPBcVZxTE2VTx?= NV[1TJdJcW6mdXPld{BieG:ydH;zbZM> NGTPfFAzPDZ6NkC4NC=>
Nalm6  NHLYVY1HfW6ldHnvckBCe3OjeR?= M{S0S|ExNzJyIN88US=> MnfrNlQhcA>? MYLy[ZN2dHS|IHnuJIRm[3KnYYPl[EBRXEWQIIDoc5NxcG:{eXzheIlwdiCjdDD0bIUhS0t{IIThdodmfCC{ZYPp[JVmKFN|OECgZY5lKGOxbnPvcYl1[W62IHTve45z\We3bHH0bY9vKG:oIGDUSW4heHKxdHXpckBmgHC{ZYPzbY9v M3fsWlI1PTZzN{my
SUP-B15 MVzGeY5kfGmxbjDBd5NigQ>? MoHsNVAwOjBizszN MXSyOEBp M2nDR5Jme3WudIOgbY4h\GWlcnXhd4VlKFCWRV6gdIhwe3Cqb4L5cIF1cW:wIHH0JJRp\SCFS{KgeIFz\2W2IILld4llfWViU{O4NEBidmRiY3;uZ49ucXSjboSg[I94dnKnZ4XsZZRqd25ib3[gVHRGViCycn;0[YlvKGW6cILld5Nqd25? NXTsd3BLOjR3NkG3PVI>
Nalm6  NUewOYUzSXCxcITvd4l{KEG|c3H5 NVfyPXh[Pi9zMDFOwG0> NGrFOlk1QCCq NV3Hb5I{cW6mdXPld{BieG:ydH;zbZM> NWfvO3E4OjR3NkG3PVI>
SUP-B15 M3r6N2Fxd3C2b4Ppd{BCe3OjeR?= M{\BPVYwOTBizszN MlLpOFghcA>? MkLwbY5lfWOnczDhdI9xfG:|aYO= NIC0R48zPDV4MUe5Ni=>
C2C12 NUjFcFN3TnWwY4Tpc44hSXO|YYm= NYPNRVdLOyEQvF2= NGDVOJQyOi9{ND:0PEBp NH;UPZVqdmirYnn0d{B1cGViZYjwdoV{e2mxbjDv[kBwe3Snb3PsZZN1KGSrZn\ldoVvfGmjdHnvckBu[XKtZYLzJIFv\CCDa4SgdIhwe3Cqb4L5cIF1cW:w NIraWWozPDJ7M{CxNS=>
Jurkat MofzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvpNU0yOCEQvF2= NU[4TmJDPDhiaB?= NIrPTHVKSzVyPUSuPUDPxE1? NHrWeHczPDJ3M{CyOC=>
CEM-R NUj0[Fk6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\RdWhrOS1zMDFOwG0> NGS4VGs1QCCq NISyUJpKSzVyPUSg{txO NInKU3EzPDJ3M{CyOC=>
CEM-S M3uwXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXexMVExKM7:TR?= MWq0PEBp M{LSPGlEPTB;ND62JO69VQ>? NIG0XWozPDJ3M{CyOC=>
MOLT-4 NGWzVmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrjN3lMOS1zMDFOwG0> M2GwRVQ5KGh? MofSTWM2OD13Lkeg{txO NHvZepYzPDJ3M{CyOC=>
PF-382 MlX5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGi3RmcyNTFyIN88US=> MlX4OFghcA>? NV3kZndzUUN3ME20MlUh|ryP NHX4ZmczPDJ3M{CyOC=>
ALL-SIL MmrJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYixMVExKM7:TR?= NYfWeHFIPDhiaB?= NH76RZFKSzVyPUWuO{DPxE1? M3TXd|I1OjV|MEK0
HPB-ALL MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zESlEuOTBizszN NVTRS452PDhiaB?= NHrJN|hKSzVyPU[uNUDPxE1? MlL3NlQzPTNyMkS=
DND-41 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfpRlh[OS1zMDFOwG0> M2PQe|Q5KGh? M3exSGlEPTB;OTFOwG0> NF\mdmgzPDJ3M{CyOC=>
ALL-SIL MUjBdI9xfG:|aYOgRZN{[Xl? MlHTOUDPxE1? NEPPV2EzPC92ODDo NIrpRYJqdmS3Y3XzJIFxd3C2b4Ppdy=> NFHaS5gzPDJ3M{CyOC=>
DND-41 NF2wV4pCeG:ydH;zbZMhSXO|YYm= M4GzNFUh|ryP Moq1NlQwPDhiaB?= MVPpcoR2[2W|IHHwc5B1d3Orcx?= MV2yOFI2OzB{NB?=
MOLT-4 M1nyT2Fxd3C2b4Ppd{BCe3OjeR?= NFvpXWQ2KM7:TR?= NIjCWYIzPC92ODDo MWLpcoR2[2W|IHHwc5B1d3Orcx?= MY[yOFI2OzB{NB?=
U-266 NF\XRY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVewMVQxKM7:TR?= NXnQRWhrPDhiaB?= MnXCTWM2OD1zOT64JOK2VcLi MYSyOFA5PjR7NB?=
INA-6 NXu3d4xtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVmwMVQxKM7:TR?= MXO0PEBp MmjmTWM2OD1{LkSyJOK2VQ>? MXeyOFA5PjR7NB?=
Jeko-1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTIfoV2OC12MDFOwG0> NVrZU4lxPDhiaB?= M3LJOGlEPTB;Mj60JOK2VcLi NXvTNppmOjRyOE[0PVQ>
Rec-1 NInGNJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\uT2IxNTRyIN88US=> NWPPWVhYPDhiaB?= M3fDXmlEPTB;MT60OkDDvU4EoB?= NWC2T2s1OjRyOE[0PVQ>
A549 MnjnSpVv[3Srb36gRZN{[Xl? MX:xNEDPxE1? M37zd|EzNzJ2L{S4JIg> NE\uT5lqdmirYnn0d{BVT0ZvzsKxMYlv\HWlZXSgcYloemG2aX;uJIFv\CCrbo\hd4lwdg>? NFLrbY4zPDB{M{mzPC=>
A549 MlezSpVv[3Srb36gRZN{[Xl? MnHXN{DPxE1? NH7qcIY1QCCq NWO1UGUycW6qaXLpeJMhXEeILd8yNU1qdmS3Y3XkJIFkfGm4YYTpc44hd2ZiU33h[EBidmRiZYjwdoV{e2mxbjDv[kBUdmGrbDDhcoQhXHerc4S= NXzZe3d[OjRyMkO5N|g>
S-LAMA84 NIDZcJhHfW6ldHnvckBCe3OjeR?= NXz2[FlYO8LizszN MlL3NlQhcA>? NInFUJlFVVOR MXTy[YR2[2W|IFPLNkBi[3Srdnn0fS=> MX2yOFAyOjFyOR?=
R-LAMA84 MX;GeY5kfGmxbjDBd5NigQ>? M4\CVFPDqM7:TR?= MlzSNlQhcA>? M1jJbGROW09? MX;y[YR2[2W|IFPLNkBi[3Srdnn0fS=> NGTXcnAzPDBzMkGwPS=>
S-LAMA84 NVzEUmJ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1TWPFIvPS1zMDFOwG0> NUnNb4x6PDhiaB?= MoPKSG1UVw>? MnTDbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> MYSyOFAyOjFyOR?=
R-LAMA84 NUS3SHZkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYWyMlUuOTBizszN NILDbWY1QCCq NWXSXZU6TE2VTx?= M{Wy[4lvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> M363NVI1ODF{MUC5
A549 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVy3U5RoOC1|MDFOwG0> MV23NkBp M3rhWGROW09? NE\hSHpKSzVyPUSuNVUh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 MmjrNlM3PTF2NEO=
H1299 MnT5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jWW|AuOzBizszN NE\RfGc4OiCq M1rFU2ROW09? M{mzZmlEPTB;MT64NEDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJINwdmOnboTyZZRqd25iZHXw[Y5l\W62bIm= Mn3uNlM3PTF2NEO=
A549 NVfs[5p6TnWwY4Tpc44hSXO|YYm= NVzQVHhIOS9zMDFOwG0> M4HDZlQ5KGh? NYq4SlQ5TE2VTx?= NV\DRnBjdGWjZIOgeI8h[SCmb4PlMYRmeGWwZHXueEBl\WO{ZXHz[UBqdiCQb4TjbEBz\XCxcoTldkBi[3Srdnn0fS=> M2\rOFI{PjVzNESz
LNCap MmfVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlX2NE0{OCEQvF2= M4rDWlQh\A>? MnH2TWM2OD12LkW5xsDPxE1? NWfMV2RzOjJ6M{KzNVY>
A431  NG\mRZlHfW6ldHnvckBCe3OjeR?= M2jzPVExKM7:TR?= NXPpUFN{OzBibXnu NHroNmpifHSnboXheIV{KFCLM1utRYt1NW2WT2Kgd4lodmGuaX7n NF\xXIIzOjN6N{m4PC=>
H2170  M1XKeWZ2dmO2aX;uJGF{e2G7 MmPPNVAh|ryP NWjKRlQzOzBibXnu MY\heJRmdnWjdHXzJHBKO0tvQXv0MY1VV1Jic3nncoFtcW6p MUOyNlM5Pzl6OB?=
A431  NEnq[mVHfW6ldHnvckBCe3OjeR?= MknmNVAh|ryP MoD6OE0zPCCq MYXlcohidmOnczDhdI9xfG:|aYOge4l1cCCncnzveIlvcWJ? M{\MNVIzOzh5OUi4
H2170  NXjHdYZ4TnWwY4Tpc44hSXO|YYm= NYm0U40{OTBizszN MmLYOE0zPCCq NHzBUohmdmijbnPld{BieG:ydH;zbZMhf2m2aDDldoxwfGmwaXK= MXWyNlM5Pzl6OB?=

... 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 <1 mg/mL
Ethanol <1 mg/mL
In vivo

* 1 mg/ml means slightly soluble or insoluble.
* 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)

  • Mass
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    Volume
    Molecular Weight

*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
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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID