Silmitasertib (CX-4945)

Catalog No.S2248

Silmitasertib (CX-4945) Chemical Structure

Molecular Weight(MW): 349.77

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

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In DMSO USD 291 In stock
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5 Customer Reviews

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

    (E) Pretreatment with CX4945 blocks TNF-induced phosphorylation of BRMS1. H157 cells were pretreated with CX4945 (30 µM) for 2 h, followed by stimulation with TNF (20 ng/mL) for an additional 1 h. Immunofluorescence assays were performed using antibodies against BRMS1 (pS30) (red)/CK2α' (green)/DAPI (blue).

    Cancer Res, 2016, 76(9):2675-86. Silmitasertib (CX-4945) purchased from Selleck.

  • Immunofluorescence analysis for Ser536 p-NF-κB cellular localization of RS4;11cells treated with CX-4945 (5 μM) and bortezomib (2.5 nM) either alone or in combination. Cells were treated, collected at 22 h and reacted with an antibody to Ser536 p-NF-κB which was revealed by a Cy3-conjugated secondary antibody. DAPI was used to label nuclei.

    Oncotarget, 2015, 51: S659-S660. Silmitasertib (CX-4945) purchased from Selleck.

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

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

Purity & Quality Control

Choose Selective Casein Kinase Inhibitors

Biological Activity

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

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

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
platelets M{TudWtqdmG|ZTDBd5NigQ>? NGDUfJcyNzVxMUCg{txO NFXCe4sxNjViaB?= MmTFSG1UVw>? MVLy[YR2[2W|IFPLNkBscW6jc3WgZYN1cX[rdImgZY5lKHCuYYTlcIV1KGGpZ4Ll[4F1cW:w M4Lpc|I3OzhzNEO3
HDMEC NGC0VYtMcW6jc3WgRZN{[Xl? MXOwMlI2NzBwNT:xJO69VQ>? MXOyOEBp M{PET2ROW09? NEKyRpRz\WS3Y3XzJGNMOiCtaX7hd4Uh[WO2aY\peJktKH[ZRjDlfJBz\XO|aX;uJIFv\CC|ZXPy[ZRqd25? M1rkVlI3OzhzNEO3
HDMEC MoPtSpVv[3Srb36gRZN{[Xl? MmfQNE4zPS9yLkWvNUDPxE1? MX[yOEBp M4Xz[GROW09? MX\y[YR2[2W|IHX4dJJme3Orb36gc4YhXkODTT2xJIJ2fCCwb4SgTWNCVS1z M4DWcVI3OzhzNEO3
HDMEC NVzscJlXTnWwY4Tpc44hSXO|YYm= MnXBNUDPxE1? MWCyOEBp NXroRlBnTE2VTx?= MmfrZYZn\WO2czDzeYJk\WyudXzhdkBtd2OjbHn6ZZRqd25ib3[gUmZCXGNzIHHu[EBxcG:|cHjvMZA3PQ>? Mn[zNlY{QDF2M{e=
A549  NXjPfYE{TnWwY4Tpc44hSXO|YYm= MUSzM|ExyqEQvF2= MXO0PEBp MU\zeZBxemW|c3XzJJRp\SCvaXPyc5BqdGyjcj3pcoR2[2WmIHX4dJJme3Orb36gc4YheC2IQVu= Ml7zNlY{OTh6MEC=
HDMEC NXzRPGJoU2mwYYPlJGF{e2G7 NFXN[HMyNTVyIN88US=> NFLvTHI2KGh? Mni3SG1UVw>? MXvk[YNz\WG|ZYOgR2szKGurbnHz[UBi[3Srdnn0fUB4cXSqb4X0JIFn\mWldHnu[{Bk\WyuII\pZYJqdGm2eR?= NFHlXpQzPjF6OUW4Oi=>
HDMEC NGjoc3BHfW6ldHnvckBCe3OjeR?= M2HTelUxKM7:TR?= M37odFEwPSCq NXLvT4NVTE2VTx?= M37TNYRm[3KnYYPld{B1cGViboXjcIVieiC|aXfuZYwhd2ZicHjvd5Bpd3K7bHH0[YQheDZ3IHnuJHRPTi4QsT3zeIlufWyjdHXkJGhFVUWFwrC= M1foUVI3OTh7NUi2
HEK293 NY\HUGh5U2mwYYPlJGF{e2G7 MUmwMlXDqM7:TR?= Ml\zNVUhdWmw M3z6emROW09? MVry[YR2[2W|IFPLNkBscW6jc3WgZYN1cX[rdIm= NYjRZlk6OjV6OEe2NlY>
Hela M4j6T2tqdmG|ZTDBd5NigQ>? NXnGR4VYOC53wrFOwG0> NYXBOWJxOTVibXnu NHzQXoVFVVOR M1nidZJm\HWlZYOgR2szKGurbnHz[UBi[3Srdnn0fS=> NF7wd|kzPTh6N{[yOi=>
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UM-SCC1 M4PP[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYPBN4F7OC5zLUOwJO69VQ>? NVKw[|Y2OS13IHS= M3jJd2lEPTB;ND6xJO69VQ>? MXuyOVc6QDB4MR?=
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Oci Ly 3 NIDSUmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWe1MVI2KM7:TR?= M{H2TlQ5KGh? M{ezRolvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> NVvubJlvOjV5OEiyOlk>
Oci Ly 10 NEfTfphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUH5OFdoPS1{NTFOwG0> NW\uZ49IPDhiaB?= MUHpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 NFHCfnczPTd6OEK2PS=>
Oci Ly 1 NEPacFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33ubVUuOjVizszN NWjOeIMzPDhiaB?= MnLBbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> NUXNZYRsOjV5OEiyOlk>
Oci Ly 18 NFvGOpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPxXJNKPS1{NTFOwG0> NX;JR5JKPDhiaB?= M1LK[YlvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> M3zDdlI2Pzh6Mk[5
Oci Ly 19  NEXpOmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3fENFUuOjVizszN M{[3PFQ5KGh? NFTLNGhqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 Mnm2NlU4QDh{Nkm=
Raji MoTRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2exdlUuOjVizszN MnfvOFghcA>? M13QOolvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> MnqzNlU4QDh{Nkm=
H1299 Mo\XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV6xM|UwOTBizszN M4jtdlczKGh? MX3pcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 M4\IZ|I2PzVyM{C4
Calu-1  M3:3bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnhNU82NzFyIN88US=> NV\UOYREPzJiaB?= M1z5T4lvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> MVmyOVc2ODNyOB?=
H358 NGnGempIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TMeFEwPS9zMDFOwG0> M3e5R|czKGh? M3Sxd4lvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> M1\CPFI2PzVyM{C4
H1299 NXrlVIF5SXCxcITvd4l{KEG|c3H5 MlHENVAh|ryP MYW3NkBp MkKzbY5lfWOnczDhdI9xfG:|aYO= M1rPZVI2PzVyM{C4
Calu-1  NEi5NmtCeG:ydH;zbZMhSXO|YYm= NV7tTmo6OTBizszN M{DHclczKGh? MUHpcoR2[2W|IHHwc5B1d3Orcx?= NXjEcnR2OjV5NUCzNFg>
H358 MX3BdI9xfG:|aYOgRZN{[Xl? NUPFS|Y1OTBizszN NF3Ke5A4OiCq MVHpcoR2[2W|IHHwc5B1d3Orcx?= MUGyOVc2ODNyOB?=
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PC9/ER MVHGeY5kfGmxbjDBd5NigQ>? M3HtfFUhyrWP MXy0PEBp NXXnZnd6cW6mdXPld{BifXSxcHjh[5k> MU[yOVQ5PjRyOR?=
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UM-SCC-1 MV3DcI9vd2enbnnjJGF{e2G7 NUD3WHR[OC53LUWg{txO NFv0XZEyPCCm MmXYSG1UVw>? NHLhR3rDqGmwaHnibZR{KGOub37v[4VvcWNic4Xyeol3[WxiYX7kJJNxcGW{ZTDmc5Ju[XSrb36= MlTrNlU{PzlyMU[=
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MDA-MB-231 M1viSmZ2dmO2aX;uJGF{e2G7 NW[5T|VnOi93L{GwJO69VQ>? NYPnUWNDPCCq M1HIeIRm[3KnYYPld{B1cGViY3;ud5RqfHW2aY\lJJBpd3OyaH;yfYxifGmxbjDv[kBjd3SqIDDwMXM2OjlvcE[1JIFv\CCyLWOxNlkuSWu2 Mn;1NlUyPTN5MkW=
MDA-MB-231 MYXGeY5kfGmxbjDBd5NigQ>? MljLNk82NzFyIN88US=> MmO5OEBp NIXKbGNqdmirYnn0d{B{\XKrbnWgOVI6KHCqb4PwbI9zgWyjdHnvckBidmRidHjlJIV5eHKnc4Ppc44hd2ZiSVytOkwhUUxvOB?= MWmyOVE2Ozd{NR?=
ARPE-19 NH;veVVMcW6jc3WgRZN{[Xl? NHfBOXc2NzFyL{KwJO69VQ>? MYOyOE81QCCq MV\pcohq[mm2czDDT|Ihc2mwYYPlJIFkfGm4aYT5JIF1KGFiY3;uZ4VvfHKjdHnvckBw\iB3wrFOwG0> NVPvPJNEOjR4OE[wPFA>
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HCT116  NFXI[|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYrY[ldHOTBizszN MV6yOE06PiCq Mo\uSG1UVw>? NILIWmhqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 M3Kw[FI1Pjh4MEiw
ARPE-19 MXjGeY5kfGmxbjDBd5NigQ>? M4j2NFExKM7:TR?= NXK2Zo44PCCq NIrCU41FVVOR MWDjZZV{\XNiRWKtd5Rz\XO|IILld5BwdnOnIH;2[ZIhfGinIICt[WlHOs7zIHLyZY5kcCxiYoX0JIRw\XNibn;0JIlv\HWlZTDDTG9RyqB? NEm2c3UzPDZ6NkC4NC=>
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Nalm6  NXPTbGR{SXCxcITvd4l{KEG|c3H5 M1ryUFYwOTBizszN NGWzcmI1QCCq NGDTOG5qdmS3Y3XzJIFxd3C2b4Ppdy=> NH7hVlYzPDV4MUe5Ni=>
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CEM-R M4XDWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk[1NU0yOCEQvF2= MXe0PEBp M{\Lc2lEPTB;NDFOwG0> M1S4TVI1OjV|MEK0
CEM-S MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVyxMVExKM7:TR?= NF[wZ5I1QCCq M{C2[WlEPTB;ND62JO69VQ>? MVKyOFI2OzB{NB?=
MOLT-4 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLiWoVDOS1zMDFOwG0> MV[0PEBp M4\ub2lEPTB;NT63JO69VQ>? M1i0NVI1OjV|MEK0
PF-382 NYLOeFlqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVO4UJRyOS1zMDFOwG0> MVm0PEBp MVnJR|UxRTRwNTFOwG0> NVPSO|ViOjR{NUOwNlQ>
ALL-SIL M{\2Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjkNU0yOCEQvF2= NWHGUHRvPDhiaB?= NWTRRnVGUUN3ME21Mlch|ryP NWW1bXBjOjR{NUOwNlQ>
HPB-ALL MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLYd3MyNTFyIN88US=> M4PwOFQ5KGh? NFHDSoxKSzVyPU[uNUDPxE1? NXuzV2NxOjR{NUOwNlQ>
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ALL-SIL NW\VbGtvSXCxcITvd4l{KEG|c3H5 NHPkVFI2KM7:TR?= NFLCfoMzPC92ODDo MnqzbY5lfWOnczDhdI9xfG:|aYO= NGrlbI8zPDJ3M{CyOC=>
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MOLT-4 MkLyRZBweHSxc3nzJGF{e2G7 NUXOfGZ[PSEQvF2= MYqyOE81QCCq M{\0WYlv\HWlZYOgZZBweHSxc3nz NXzR[XpjOjR{NUOwNlQ>
U-266 NIrIOllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPKb40xNTRyIN88US=> NH;OWG01QCCq MYLJR|UxRTF7LkigxtVOyqB? NUTSb3o5OjRyOE[0PVQ>
INA-6 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfPNE01OCEQvF2= NEK4Tlc1QCCq M1i5O2lEPTB;Mj60NkDDvU1? MlO4NlQxQDZ2OUS=
Jeko-1 NXS0XnlsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1zTUFAuPDBizszN NFi4PWU1QCCq M3PJbmlEPTB;Mj60JOK2VcLi M17CNFI1ODh4NEm0
Rec-1 MkTkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYPNc|FjOC12MDFOwG0> M2m0N|Q5KGh? NUfmT3oyUUN3ME2xMlQ3KML3TdMg NY\XZoVQOjRyOE[0PVQ>
A549 MYjGeY5kfGmxbjDBd5NigQ>? MUWxNEDPxE1? NEjqVJoyOi9{ND:0PEBp NELmRmZqdmirYnn0d{BVT0ZvzsKxMYlv\HWlZXSgcYloemG2aX;uJIFv\CCrbo\hd4lwdg>? NVyxO3pxOjRyMkO5N|g>
A549 NHHxdGtHfW6ldHnvckBCe3OjeR?= MmrmN{DPxE1? NVm5cWYzPDhiaB?= M3jlfolvcGmkaYTzJHRITi4QskGtbY5lfWOnZDDhZ5RqfmG2aX;uJI9nKFOvYXSgZY5lKGW6cILld5Nqd25ib3[gV45icWxiYX7kJHR4cXO2 NVXndHZuOjRyMkO5N|g>
S-LAMA84 MkTRSpVv[3Srb36gRZN{[Xl? NE\zbo4{yqEQvF2= NFvYdIozPCCq M37NXWROW09? NEDt[YRz\WS3Y3XzJGNMOiCjY4Tpeol1gQ>? NGXzbVMzPDBzMkGwPS=>
R-LAMA84 MVLGeY5kfGmxbjDBd5NigQ>? M{[5O|PDqM7:TR?= NF7pSpQzPCCq MXPEUXNQ NGnMbmNz\WS3Y3XzJGNMOiCjY4Tpeol1gQ>? NFXnU2UzPDBzMkGwPS=>
S-LAMA84 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonMNk42NTFyIN88US=> MUi0PEBp MkTjSG1UVw>? MWrpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 NG[3cZczPDBzMkGwPS=>
R-LAMA84 NVH0dGVoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVO1XWxoOi53LUGwJO69VQ>? NXLkVYhIPDhiaB?= M2\lUWROW09? NV;lZXFKcW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? MnnHNlQxOTJzMEm=
A549 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX[wMVMxKM7:TR?= NEi0d4E4OiCq NWTaNYViTE2VTx?= NIPmeo9KSzVyPUSuNVUh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 NF7HfokzOzZ3MUS0Ny=>
H1299 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\xNE0{OCEQvF2= NESxdWI4OiCq MWrEUXNQ M2\t[WlEPTB;MT64NEDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJINwdmOnboTyZZRqd25iZHXw[Y5l\W62bIm= MXOyN|Y2OTR2Mx?=
A549 Mn7PSpVv[3Srb36gRZN{[Xl? M3[yRlEwOTBizszN MmewOFghcA>? NYXIeGt7TE2VTx?= MY\s[YFleyC2bzDhJIRwe2VvZHXw[Y5l\W62IHTlZ5Jm[XOnIHnuJG5wfGOqIILldI9zfGW{IHHjeIl3cXS7 NXn3XXpkOjN4NUG0OFM>
LNCap NVvKO4U5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjDTJUxNTNyIN88US=> M{DyTVQh\A>? MkWyTWM2OD12LkW5xsDPxE1? NGrsW2szOjh|MkOxOi=>
A431  MVXGeY5kfGmxbjDBd5NigQ>? M{PxXFExKM7:TR?= MXqzNEBucW5? NHThT4FifHSnboXheIV{KFCLM1utRYt1NW2WT2Kgd4lodmGuaX7n NGK2NHAzOjN6N{m4PC=>
H2170  NVftOo5VTnWwY4Tpc44hSXO|YYm= M3;BclExKM7:TR?= NXfYUWlIOzBibXnu MVvheJRmdnWjdHXzJHBKO0tvQXv0MY1VV1Jic3nncoFtcW6p M3XKWVIzOzh5OUi4
A431  Mk\zSpVv[3Srb36gRZN{[Xl? NXPtPWNpOTBizszN MXy0MVI1KGh? MYHlcohidmOnczDhdI9xfG:|aYOge4l1cCCncnzveIlvcWJ? M3fHZVIzOzh5OUi4
H2170  MVHGeY5kfGmxbjDBd5NigQ>? M4W0S|ExKM7:TR?= Mn:4OE0zPCCq NYK5eo9G\W6qYX7j[ZMh[XCxcITvd4l{KHerdHig[ZJtd3Srbnni NEPIXVkzOjN6N{m4PC=>

... Click to View More Cell Line Experimental Data

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

Protocol

Kinase Assay:[2]
+ Expand

CK2 Kinase Assay:

CX-4945 is added at a volume of 10 μL to a reaction mixture comprising 10 μL of assay dilution buffer (ADB; 20 mM MOPS, pH 7.2, 25 mM β-glycerolphosphate, 5 mM EGTA, 1 mM sodium orthovanadate, and 1 mM dithiothreitol), 10 μL of substrate peptide (RRRDDDSDDD, dissolved in ADB at a concentration of 1 mM), 10 μL of recombinant human CK2 (ααββ-holoenzyme, 25 ng dissolved in ADB). Reactions are initiated by the addition of 10 μL of ATP solution (90% 75 mM MgCl2, 75 μM ATP (final ATP concentration=15 μM) dissolved in ADB; 10% [γ-33P]ATP (stock 1 mCi/100 μL; 3000 Ci/mM and maintained for 10 minutes at 30 °C. The reactions are quenched with 100 μL of 0.75% phosphoric acid and then transferred to and filtered through a phosphocellulose filter plate. After washing each well five times with 0.75% phosphoric acid, the plate is dried under vacuum for 5 minutes and, following the addition of 15 μL of scintillation fluid to each well, the residual radioactivity is measured using a Wallac luminescence counter. The IC50 values are derived from eight concentrations of CX-4945 over a range of 0.0001 μM to 1 μM.
Cell Research:[1]
+ Expand
  • Cell lines: SKBr3, MDA-MB-453, BT-474, ZR-75-1, MDA-MB-231, MDA-MB-468, T47D, MCF 7, Hs578T, MDA-MB-361, UACC-812, et al.
  • Concentrations: Dissolved in DMSO, final concentrations ~100 μM
  • Incubation Time: 4 days
  • Method: Cells are seeded at a density of 3,000 cells per well 24 hours prior to treatment, in appropriate media, and then treated with various concentrations of CX-4945. Suspensions cells are seeded and treated on the same day. Following 4 days of incubation, Alamar Blue (20 μL, 10% of volume per well) is added and the cells are further incubated at 37 °C for 4-5 hours. Fluorescence with excitation wavelength at 530-560 nm and emission wavelength at 590 nm is measured.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: Female immunocompromised mice CrTac:Ncr-Foxn1nu injected with BxPC-3 or BT-474 cells
  • Formulation: Dissolved in DMSO, and diluted in PBS
  • Dosages: 25 or 75 mg/kg
  • Administration: Oral gavage twice daily
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 16 mg/mL (45.74 mM)
Water Insoluble
Ethanol Insoluble

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

Chemical Information

Molecular Weight 349.77
Formula

C19H12ClN3O2

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

Bio Calculators

Molarity Calculator

Molarity Calculator

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

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

  • Mass
    Concentration
    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
    V1
    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