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 MnPST4lv[XOnIFHzd4F6 NUnZWGFoOS93L{GwJO69VQ>? MWiwMlUhcA>? M2HUZWROW09? M2\1S5Jm\HWlZYOgR2szKGurbnHz[UBi[3Srdnn0fUBidmRicHzheIVt\XRiYXfndoVo[XSrb36= NFXlOpMzPjN6MUSzOy=>
HDMEC NVfNWpc{U2mwYYPlJGF{e2G7 MViwMlI2NzBwNT:xJO69VQ>? MlG0NlQhcA>? Mm\BSG1UVw>? MkHmdoVlfWOnczDDT|Ihc2mwYYPlJIFkfGm4aYT5MEB3X0ZiZYjwdoV{e2mxbjDhcoQhe2WlcnX0bY9v NXS4RmxSOjZ|OEG0N|c>
HDMEC NUf3R|I3TnWwY4Tpc44hSXO|YYm= M3XKVFAvOjVxMD61M|Eh|ryP M4DJO|I1KGh? M1qwS2ROW09? NFvrO4dz\WS3Y3XzJIV5eHKnc4Ppc44hd2ZiVlPBUU0yKGK3dDDuc5QhUUODTT2x NVjiU4FxOjZ|OEG0N|c>
HDMEC NYftdHhZTnWwY4Tpc44hSXO|YYm= NVezVoxkOSEQvF2= M{HzSVI1KGh? M1vzemROW09? MWDh[oZm[3S|IIP1ZoNmdGy3bHHyJIxw[2GuaYrheIlwdiCxZjDOSmFV[zFiYX7kJJBpd3OyaH:tdFY2 M{P4OFI3OzhzNEO3
A549  Mm\QSpVv[3Srb36gRZN{[Xl? MX[zM|ExyqEQvF2= MXO0PEBp NVfoWnlXe3WycILld5NmeyC2aHWgcYlkem:yaXzsZZIucW6mdXPl[EBmgHC{ZYPzbY9vKG:oIICtSmFM MWCyOlMyQDhyMB?=
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HDMEC M1LvS2Z2dmO2aX;uJGF{e2G7 MWS1NEDPxE1? MUSxM|UhcA>? M2C1cWROW09? NHn0Z5hl\WO{ZXHz[ZMhfGinIH71Z4xm[XJic3nncoFtKG:oIIDoc5NxcG:{eXzheIVlKHB4NTDpckBVVkZvzsGtd5RqdXWuYYTl[EBJTE2HQ9Mg NVnvb5lmOjZzOEm1PFY>
HEK293 MWfLbY5ie2ViQYPzZZk> MVmwMlXDqM7:TR?= NHLaUVAyPSCvaX6= NITJSlNFVVOR M4\uOJJm\HWlZYOgR2szKGurbnHz[UBi[3Srdnn0fS=> MorQNlU5QDd4Mk[=
Hela MlztT4lv[XOnIFHzd4F6 Mn;XNE42yqEQvF2= NHPNSVUyPSCvaX6= NYfufJliTE2VTx?= NWXBeXNjemWmdXPld{BEUzJia3nuZZNmKGGldHn2bZR6 NWjiUIRqOjV6OEe2NlY>
LAMA84 NXvBTFhvU2mwYYPlJGF{e2G7 M4HEOVAvPcLizszN NYC3T3M1OTVibXnu NE[z[2hFVVOR MmPJdoVlfWOnczDDT|Ihc2mwYYPlJIFkfGm4aYT5 NXLHb4s6OjV6OEe2NlY>
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NU-DUL MmDBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHXGTJc2NTJ3IN88US=> MmnvOFghcA>? MknSbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> MmKxNlU4QDh{Nkm=
Oci Ly 3 M2P1TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3:4OFUuOjVizszN M{TGR|Q5KGh? NGP3OoxqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NFz4S|kzPTd6OEK2PS=>
Oci Ly 10 NF7wUG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXj6dGl2PS1{NTFOwG0> M2npNlQ5KGh? Ml65bY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> MW[yOVc5QDJ4OR?=
Oci Ly 1 NUDsWpBYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHKVFA2NTJ3IN88US=> NIrmVVA1QCCq M4[5VolvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> NVH2enl3OjV5OEiyOlk>
Oci Ly 18 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\KSGg2NTJ3IN88US=> NIDvb441QCCq MYrpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 NIXDVoUzPTd6OEK2PS=>
Oci Ly 19  M3[0Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYD6fW1TPS1{NTFOwG0> NHyxUG81QCCq Mn62bY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> NFHBTIIzPTd6OEK2PS=>
Raji NYqx[4MxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmSzOU0zPSEQvF2= M3raU|Q5KGh? NXGwfIJbcW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? MnjuNlU4QDh{Nkm=
H1299 NUH6fG1XT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\1WJk4OS93L{GwJO69VQ>? NVTQZVR{PzJiaB?= MkCxbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> MoC3NlU4PTB|MEi=
Calu-1  M3;F[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHTSFMyNzVxMUCg{txO MXu3NkBp NVnYN2tMcW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? MWqyOVc2ODNyOB?=
H358 M3SwWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPtR5VIOS93L{GwJO69VQ>? MlvHO|IhcA>? MmTYbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> NEm3bIczPTd3MEOwPC=>
H1299 MorBRZBweHSxc3nzJGF{e2G7 NIriW4wyOCEQvF2= NWrudZdDPzJiaB?= Ml[zbY5lfWOnczDhdI9xfG:|aYO= MUiyOVc2ODNyOB?=
Calu-1  M2fNW2Fxd3C2b4Ppd{BCe3OjeR?= MkDqNVAh|ryP MkCxO|IhcA>? MnLpbY5lfWOnczDhdI9xfG:|aYO= MlT0NlU4PTB|MEi=
H358 MVTBdI9xfG:|aYOgRZN{[Xl? NYDLfmdSOTBizszN MVi3NkBp MnjLbY5lfWOnczDhdI9xfG:|aYO= NEXCfZQzPTd3MEOwPC=>
PC9/GR NHrC[VVHfW6ldHnvckBCe3OjeR?= MXW1JOK2VQ>? MnrsOFghcA>? Mn7PbY5lfWOnczDheZRweGijZ4m= MX6yOVQ5PjRyOR?=
PC9/ER NV;idIptTnWwY4Tpc44hSXO|YYm= NGrRXGY2KML3TR?= M1nleFQ5KGh? MlKwbY5lfWOnczDheZRweGijZ4m= M2XxOVI2PDh4NEC5
H28 NV3UXop7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NETPdGcxNjBzLUOwJO69VQ>? NX;DNm84PzJiaB?= Mm\xSG1UVw>? NHnXPXdKSzVyPUeuNkDPxE1? MVOyOVQzOjB6MR?=
H2052 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXYSIlCOC5yMT2zNEDPxE1? MmLtO|IhcA>? NFTTTXRFVVOR NWPZd3BpUUN3ME2yMlAh|ryP NUnx[ZcxOjV2MkKwPFE>
UM-SCC-1 MX;DcI9vd2enbnnjJGF{e2G7 MkjxNE42NTVizszN NXLk[lNlOTRiZB?= M1fUPWROW09? M3;jVeKhcW6qaXLpeJMh[2yxbn;n[Y5q[yC|dYL2bZZidCCjbnSgd5Bp\XKnIH\vdo1ifGmxbh?= MoLoNlU{PzlyMU[=
UM-SCC-46 M4W5[2Ntd26xZ3XubYMhSXO|YYm= NWXYVVc4OC53LUWg{txO MlfUNVQh\A>? MXPEUXNQ M4jqPeKhcW6qaXLpeJMh[2yxbn;n[Y5q[yC|dYL2bZZidCCjbnSgd5Bp\XKnIH\vdo1ifGmxbh?= NHnuNIIzPTN5OUCxOi=>
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MDA-MB-231 NGL5OYNHfW6ldHnvckBCe3OjeR?= NGHybXIzNzVxMUCg{txO NHLUTpI1KGh? MX;k[YNz\WG|ZYOgeIhmKGOxboP0bZR2fGm4ZTDwbI9{eGixconsZZRqd25ib3[gZo91cCBicD3TOVI6NXB4NTDhcoQheC2VMUK5MWFsfA>? M2rtdFI2OTV|N{K1
MDA-MB-231 NY\BRnh3TnWwY4Tpc44hSXO|YYm= NXHYUGRjOi93L{GwJO69VQ>? M4PS[FQhcA>? NYDN[|J{cW6qaXLpeJMhe2W{aX7lJFUzQSCyaH;zdIhwenmuYYTpc44h[W6mIITo[UBmgHC{ZYPzbY9vKG:oIFnMMVYtKEmOLUi= MVuyOVE2Ozd{NR?=
ARPE-19 MlXtT4lv[XOnIFHzd4F6 MkXaOU8yOC9{MDFOwG0> MYqyOE81QCCq Ml7ubY5pcWKrdIOgR2szKGurbnHz[UBi[3Srdnn0fUBifCCjIHPvcoNmdnS{YYTpc44hd2ZiNdMg{txO MVSyOFY5PjB6MB?=
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HCT116  NXLmdXhVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;pVVExKM7:TR?= MoDaNlQuQTZiaB?= M{G5OGROW09? MWjpcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 M1fh[VI1Pjh4MEiw
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HCT116  NXzSSWJRTnWwY4Tpc44hSXO|YYm= MoHFNVAh|ryP MVy0JIg> MWXEUXNQ M3zLTINifXOnczDFVk1{fHKnc4OgdoV{eG:wc3Wgc5ZmeiC2aHWgdE1mUUZ{zsGgZpJidmOqLDDieZQh\G:nczDuc5QhcW6mdXPlJGNJV1EEoB?= NHr1NoMzPDZ6NkC4NC=>
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Nalm6  MmL5RZBweHSxc3nzJGF{e2G7 NHvCWJc3NzFyIN88US=> M3zPdVQ5KGh? NUTFOlJicW6mdXPld{BieG:ydH;zbZM> M1jkTlI1PTZzN{my
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C2C12 MVPGeY5kfGmxbjDBd5NigQ>? NHz4[Xg{KM7:TR?= M3XHVFEzNzJ2L{S4JIg> M33pNolvcGmkaYTzJJRp\SCneIDy[ZN{cW:wIH;mJI9{fGWxY3zhd5Qh\GmoZnXy[Y51cWG2aX;uJI1iemuncoOgZY5lKEGtdDDwbI9{eGixconsZZRqd25? M17qRlI1Ojl|MEGx
Jurkat MljZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYKxMVExKM7:TR?= MY[0PEBp M4X1V2lEPTB;ND65JO69VQ>? M3j5ZlI1OjV|MEK0
CEM-R M3PLUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTvNU0yOCEQvF2= MVq0PEBp M{fTbmlEPTB;NDFOwG0> MWOyOFI2OzB{NB?=
CEM-S M4\nWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HYfVEuOTBizszN MVW0PEBp M2XTcWlEPTB;ND62JO69VQ>? MkXmNlQzPTNyMkS=
MOLT-4 M3TGWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXq1ToRTOS1zMDFOwG0> NWjGU4JnPDhiaB?= NEW1[4JKSzVyPUWuO{DPxE1? MoPkNlQzPTNyMkS=
PF-382 NW\yUZp5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV35RZdIOS1zMDFOwG0> NH;YOok1QCCq MV;JR|UxRTRwNTFOwG0> Mkf2NlQzPTNyMkS=
ALL-SIL M{[5WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M32xRlEuOTBizszN NYnielNDPDhiaB?= NGr2O29KSzVyPUWuO{DPxE1? MnrTNlQzPTNyMkS=
HPB-ALL MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\2PWgyNTFyIN88US=> MYm0PEBp NU\Ze4o6UUN3ME22MlEh|ryP NFvYeFIzPDJ3M{CyOC=>
DND-41 MlvlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPrZ|gyNTFyIN88US=> M2TDNFQ5KGh? NVTmPFdUUUN3ME25JO69VQ>? NVPZNHdIOjR{NUOwNlQ>
ALL-SIL NXi1WZEzSXCxcITvd4l{KEG|c3H5 M1\Td|Uh|ryP Mn30NlQwPDhiaB?= M2PYcolv\HWlZYOgZZBweHSxc3nz NWLuUFl4OjR{NUOwNlQ>
DND-41 NYezXIlKSXCxcITvd4l{KEG|c3H5 MXy1JO69VQ>? M{T5NFI1NzR6IHi= MYrpcoR2[2W|IHHwc5B1d3Orcx?= NEfJe2szPDJ3M{CyOC=>
MOLT-4 NU\KXZRqSXCxcITvd4l{KEG|c3H5 M1\kd|Uh|ryP MkLCNlQwPDhiaB?= NVLQc2l6cW6mdXPld{BieG:ydH;zbZM> NETMOGYzPDJ3M{CyOC=>
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INA-6 M4Tl[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTtdZF6OC12MDFOwG0> NEflTJg1QCCq NGfPendKSzVyPUKuOFIhyrWP M17CXVI1ODh4NEm0
Jeko-1 NWLBVIZ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrvNE01OCEQvF2= NIXvV2g1QCCq NYrrU4FEUUN3ME2yMlQhyrWPwrC= MojoNlQxQDZ2OUS=
Rec-1 MljkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mki0NE01OCEQvF2= MXe0PEBp M3\3e2lEPTB;MT60OkDDvU4EoB?= NGTqUGIzPDB6NkS5OC=>
A549 NYfiNZozTnWwY4Tpc44hSXO|YYm= M2jScFExKM7:TR?= NX;yRm1lOTJxMkSvOFghcA>? M1jld4lvcGmkaYTzJHRITi4QskGtbY5lfWOnZDDtbYdz[XSrb36gZY5lKGmwdnHzbY9v NYXrXpNxOjRyMkO5N|g>
A549 M2O0Z2Z2dmO2aX;uJGF{e2G7 NY\NUnRQOyEQvF2= NUTDclM4PDhiaB?= MlLUbY5pcWKrdIOgWGdHNc7{MT3pcoR2[2WmIHHjeIl3[XSrb36gc4YhW22jZDDhcoQh\XiycnXzd4lwdiCxZjDTcoFqdCCjbnSgWJdqe3R? NFe1dYYzPDB{M{mzPC=>
S-LAMA84 NUCyW2htTnWwY4Tpc44hSXO|YYm= MVGzxsDPxE1? MmS3NlQhcA>? NXfJSlVOTE2VTx?= NX\QSohOemWmdXPld{BEUzJiYXP0bZZqfHl? NW\tN5ZVOjRyMUKxNFk>
R-LAMA84 NWPr[W1ETnWwY4Tpc44hSXO|YYm= NGCyc|c{yqEQvF2= NX\OZWU2OjRiaB?= NY\MZWU{TE2VTx?= M3rJepJm\HWlZYOgR2szKGGldHn2bZR6 NUnNdZQxOjRyMUKxNFk>
S-LAMA84 M{LFSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkC0Nk42NTFyIN88US=> M4HWSVQ5KGh? M4rnV2ROW09? NV\MVXJpcW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? NUTtVlloOjRyMUKxNFk>
R-LAMA84 NUjQd4RiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjmR5YzNjVvMUCg{txO M{\5V|Q5KGh? MV\EUXNQ MXPpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 NHnwdIwzPDBzMkGwPS=>
A549 NV\NcHdPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4XSV|AuOzBizszN NX;NUHZ4PzJiaB?= M4HQS2ROW09? NInxdoJKSzVyPUSuNVUh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 NIjZcFQzOzZ3MUS0Ny=>
H1299 MonmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TlflAuOzBizszN NXO1XZNPPzJiaB?= NWXLSXdKTE2VTx?= NHTLbo9KSzVyPUGuPFAh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 NH3vbpAzOzZ3MUS0Ny=>
A549 NEX0TmtHfW6ldHnvckBCe3OjeR?= MnLQNU8yOCEQvF2= MmLmOFghcA>? NYHtV2pPTE2VTx?= MWLs[YFleyC2bzDhJIRwe2VvZHXw[Y5l\W62IHTlZ5Jm[XOnIHnuJG5wfGOqIILldI9zfGW{IHHjeIl3cXS7 MV2yN|Y2OTR2Mx?=
LNCap MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUKwMVMxKM7:TR?= MXi0JIQ> MYLJR|UxRTRwNUpCpO69VQ>? Mkf0NlI5OzJ|MU[=
A431  M17oW2Z2dmO2aX;uJGF{e2G7 NIrSW2wyOCEQvF2= MkDUN|AhdWmw NIfGZ2lifHSnboXheIV{KFCLM1utRYt1NW2WT2Kgd4lodmGuaX7n M2HmW|IzOzh5OUi4
H2170  Mmf0SpVv[3Srb36gRZN{[Xl? Mn\RNVAh|ryP MXizNEBucW5? NH3kd4VifHSnboXheIV{KFCLM1utRYt1NW2WT2Kgd4lodmGuaX7n NF7JVnEzOjN6N{m4PC=>
A431  NUD3UIFRTnWwY4Tpc44hSXO|YYm= Mm\tNVAh|ryP M{W0fVQuOjRiaB?= NESyc5dmdmijbnPld{BieG:ydH;zbZMhf2m2aDDldoxwfGmwaXK= MUmyNlM5Pzl6OB?=
H2170  NYjzVZcyTnWwY4Tpc44hSXO|YYm= NVvxXHhJOTBizszN M2XuSVQuOjRiaB?= NFji[phmdmijbnPld{BieG:ydH;zbZMhf2m2aDDldoxwfGmwaXK= NV\HSVZCOjJ|OEe5PFg>

... 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 slightly soluble or insoluble
Ethanol slightly soluble or insoluble
In vivo Add solvents individually and in order:

* 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
    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