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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USD 320 In stock
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6 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.

    (B and C) Jurkat cells were pretreated for 2 h with DES (3 μM) and CX-4945 (10 μM) individually or in combination, and were then treated with PMA (50 ng/mL) plus PHA (1 μg/mL) for 6 and 24 h. IL-2 mRNA expression was detected by qRT-PCR analysis (B) and the amounts of secreted IL-2 in the culture medium were measured by ELISA (C). #p < .01 (vs. the PMA/PHA, DES, and CX-4945 untreated cell population); *p < .01; **p < .001 (vs. the cell population treated with only PMA/PHA).

    Biomed Pharmacother, 2018, 98:357-363. 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 NV;IdlJTU2mwYYPlJGF{e2G7 NV3p[Fd2OS93L{GwJO69VQ>? MkjFNE42KGh? M{TGWWROW09? MVjy[YR2[2W|IFPLNkBscW6jc3WgZYN1cX[rdImgZY5lKHCuYYTlcIV1KGGpZ4Ll[4F1cW:w Mk\aNlY{QDF2M{e=
HDMEC MW\LbY5ie2ViQYPzZZk> MlLvNE4zPS9yLkWvNUDPxE1? NWT4O4JLOjRiaB?= MmTxSG1UVw>? M3[y[ZJm\HWlZYOgR2szKGurbnHz[UBi[3Srdnn0fUwhfleIIHX4dJJme3Orb36gZY5lKHOnY4LleIlwdg>? NIXkNFczPjN6MUSzOy=>
HDMEC NF74THNHfW6ldHnvckBCe3OjeR?= M3jJUVAvOjVxMD61M|Eh|ryP NVzGOZM2OjRiaB?= NIjUSotFVVOR MmOwdoVlfWOnczDlfJBz\XO|aX;uJI9nKF[FQV2tNUBjfXRibn;0JGlESU1vMR?= NF;6WJozPjN6MUSzOy=>
HDMEC Mnn0SpVv[3Srb36gRZN{[Xl? NHnrT5UyKM7:TR?= NEflVGozPCCq NX\sN4VGTE2VTx?= M3nTWoFn\mWldIOgd5Vj[2WubIXsZZIhdG:lYXzpfoF1cW:wIH;mJG5HSVSlMTDhcoQheGixc4Doc{1xPjV? MoX6NlY{QDF2M{e=
A549  NYHHN5lOTnWwY4Tpc44hSXO|YYm= MV:zM|ExyqEQvF2= NUfu[3VOPDhiaB?= Mon2d5VxeHKnc4Pld{B1cGVibXnjdo9xcWyuYYKtbY5lfWOnZDDlfJBz\XO|aX;uJI9nKHBvRlHL NGLzc20zPjNzOEiwNC=>
HDMEC NWHRW5NvU2mwYYPlJGF{e2G7 NFizS4syNTVyIN88US=> NV3JUo5TPSCq NFjSbplFVVOR MWfk[YNz\WG|ZYOgR2szKGurbnHz[UBi[3Srdnn0fUB4cXSqb4X0JIFn\mWldHnu[{Bk\WyuII\pZYJqdGm2eR?= M1fjZVI3OTh7NUi2
HDMEC MmDTSpVv[3Srb36gRZN{[Xl? MWG1NEDPxE1? NWq4OWdGOS93IHi= NUGyc5ROTE2VTx?= Mn;B[IVkemWjc3XzJJRp\SCwdXPs[YFzKHOrZ37hcEBw\iCyaH;zdIhwenmuYYTl[EBxPjViaX6gWG5HNc7zLYP0bY12dGG2ZXSgTGROTUQEoB?= MnTKNlYyQDl3OE[=
HEK293 MVnLbY5ie2ViQYPzZZk> MkXUNE42yqEQvF2= M1zhXVE2KG2rbh?= MoezSG1UVw>? NEXye2Zz\WS3Y3XzJGNMOiCtaX7hd4Uh[WO2aY\peJk> NUn2SmJrOjV6OEe2NlY>
Hela MVzLbY5ie2ViQYPzZZk> Ml7xNE42yqEQvF2= MXexOUBucW5? M2TSTGROW09? NYPnfW97emWmdXPld{BEUzJia3nuZZNmKGGldHn2bZR6 MV[yOVg5PzZ{Nh?=
LAMA84 NV70cWlkU2mwYYPlJGF{e2G7 MX[wMlXDqM7:TR?= NEnrSI0yPSCvaX6= NUfjVWpsTE2VTx?= NIDiU4Nz\WS3Y3XzJGNMOiCtaX7hd4Uh[WO2aY\peJk> MXGyOVg5PzZ{Nh?=
HEK293 M2ezPWZ2dmO2aX;uJGF{e2G7 NUjV[npKOyEQvF2= Mn;oOUBp MljESG1UVw>? NI\DNnZEUzJicHjvd5Bpd3K7bHH0[ZMh\UmIM3qgZZQhW2W{MUK3 NYe4O|ZUOjV6OEe2NlY>
UM-SCC1 NF2wVZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXewMlEuOzBizszN M1Hre|EuPSCm NVnTUGdLUUN3ME20MlEh|ryP MWGyOVc6QDB4MR?=
UM-SCC46 NFrINZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPt[JcxNjFvM{Cg{txO M3zaWVEuPSCm M3HLU2lEPTB;Mz60JO69VQ>? NGX4V4wzPTd7OEC2NS=>
UM-SCC1 NWLYfXJsTnWwY4Tpc44hSXO|YYm= MlX2NE42NzRxMUCg{txO MmjkO|IhcA>? NIm2[Xlld3ewLYLl[5Vt[XSnczD0bIUh\XiycnXzd4lwdiCxZjDOSk3FwEJuIFLjcE1ZVCCjbnSgeZAuemWpdXzheIV{KHSqZTDlfJBz\XO|aX;uJI9nKHB3MzygdFIyNCCDUD2xJIFv\CCLTD24JINwdmOnboTyZZRqd25iZHXw[Y5l\W62bIm= M130UVI2Pzl6ME[x
UM-SCC46 M2DycWZ2dmO2aX;uJGF{e2G7 MkfZNE42NzRxMUCg{txO MYC3NkBp M2nQOYRwf25vcnXneYxifGW|IITo[UBmgHC{ZYPzbY9vKG:oIF7GMeS5SixiQnPsMXhNNCCyNUOsJJAzOSxiQWCtNUBidmRidYCtdoVofWyjdHXzJJRp\SCneIDy[ZN{cW:wIFnMMVgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> MlrqNlU4QThyNkG=
NU-DUL MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\3d4RJPS1{NTFOwG0> NHP6[Yc1QCCq NF\YR49qdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NFnxRpMzPTd6OEK2PS=>
Oci Ly 3 M1j3cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTrOU0zPSEQvF2= NY\CNJhRPDhiaB?= Mn:xbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> MmP5NlU4QDh{Nkm=
Oci Ly 10 NXL3TppZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrvOU0zPSEQvF2= MXu0PEBp NHP1bmlqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 Mn;yNlU4QDh{Nkm=
Oci Ly 1 NGjzSIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWm1MVI2KM7:TR?= M1vSXFQ5KGh? NIOyR25qdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NUXQ[5Z4OjV5OEiyOlk>
Oci Ly 18 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUm1MVI2KM7:TR?= NH;sOmU1QCCq MXTpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 NY\LTXZQOjV5OEiyOlk>
Oci Ly 19  MljTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4O3XFUuOjVizszN M3nUTFQ5KGh? MVvpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 MofrNlU4QDh{Nkm=
Raji MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DKdlUuOjVizszN NXPFSoVjPDhiaB?= M4jYPIlvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> MnHKNlU4QDh{Nkm=
H1299 NWXKSY92T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13ubVEwPS9zMDFOwG0> M3nadVczKGh? NGrmVppqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NWnk[mhvOjV5NUCzNFg>
Calu-1  MkiwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE[y[|EyNzVxMUCg{txO MUe3NkBp M4DCRolvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> MX:yOVc2ODNyOB?=
H358 MmXGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHGNU82NzFyIN88US=> NHHUO4k4OiCq MUXpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 Mn3TNlU4PTB|MEi=
H1299 MV\BdI9xfG:|aYOgRZN{[Xl? NHnLVY8yOCEQvF2= NEnCVlk4OiCq M4\ONYlv\HWlZYOgZZBweHSxc3nz MnPaNlU4PTB|MEi=
Calu-1  M2XsSGFxd3C2b4Ppd{BCe3OjeR?= M4jSeVExKM7:TR?= NXWwUlFNPzJiaB?= M4KwXIlv\HWlZYOgZZBweHSxc3nz MljKNlU4PTB|MEi=
H358 Mn\KRZBweHSxc3nzJGF{e2G7 MWKxNEDPxE1? MkD3O|IhcA>? NGLQeG1qdmS3Y3XzJIFxd3C2b4Ppdy=> NV\heJRXOjV5NUCzNFg>
PC9/GR M4X2UWZ2dmO2aX;uJGF{e2G7 MXS1JOK2VQ>? MoDPOFghcA>? M3XndYlv\HWlZYOgZZV1d3CqYXf5 MljrNlU1QDZ2MEm=
PC9/ER MV;GeY5kfGmxbjDBd5NigQ>? MU[1JOK2VQ>? NGmzUoY1QCCq MlP0bY5lfWOnczDheZRweGijZ4m= MXOyOVQ5PjRyOR?=
H28 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\oU3dwOC5yMT2zNEDPxE1? MVe3NkBp MWrEUXNQ M3mzS2lEPTB;Nz6yJO69VQ>? Mkn4NlU1OjJyOEG=
H2052 NXHhTW1bT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUmwMlAyNTNyIN88US=> NFO0dWs4OiCq NXzqZ4lTTE2VTx?= NX7sXnR7UUN3ME2yMlAh|ryP NXTVeZljOjV2MkKwPFE>
UM-SCC-1 NFfSVoNEdG:wb3flcolkKEG|c3H5 NHPCcnIxNjVvNTFOwG0> MoXJNVQh\A>? M1nGW2ROW09? NULEWnB3yqCrbnjpZol1eyClbH;uc4dmdmmlIIP1dpZqfmGuIHHu[EB{eGincnWg[o9zdWG2aX;u NHfpZ5kzPTN5OUCxOi=>
UM-SCC-46 M3\QSmNtd26xZ3XubYMhSXO|YYm= M{HZR|AvPS13IN88US=> M2rGcFE1KGR? M3HyRmROW09? MVxCpIlvcGmkaYTzJINtd26xZ3XubYMhe3W{dnn2ZYwh[W6mIIPwbIVz\SCob4LtZZRqd25? M{PxVlI2Ozd7MEG2
U87-MG MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW[xM|UwOTBizszN MUmyOE81QC95MjDo MXHEUXNQ MX3pcohq[mm2czDj[YxtKGe{b4f0bEBjd3SqIHPvcoNmdnS{YYTpc44h[W6mIITpcYUh\GWyZX7k[Y51dHl? MYWyOVI1OTh7Nx?=
MDA-MB-231 MVnGeY5kfGmxbjDBd5NigQ>? M2LBWFIwPS9zMDFOwG0> MmjkOEBp NVrhNIdI\GWlcnXhd4V{KHSqZTDjc45{fGm2dYTpeoUheGixc4Doc5J6dGG2aX;uJI9nKGKxdHigJJAuWzV{OT3wOlUh[W6mIICtV|EzQS2Da4S= NVnCd5BJOjVzNUO3NlU>
MDA-MB-231 NEDMbnJHfW6ldHnvckBCe3OjeR?= M3Oyb|IwPS9zMDFOwG0> M1vhdVQhcA>? NGnOZ5NqdmirYnn0d{B{\XKrbnWgOVI6KHCqb4PwbI9zgWyjdHnvckBidmRidHjlJIV5eHKnc4Ppc44hd2ZiSVytOkwhUUxvOB?= NGDyeIQzPTF3M{eyOS=>
ARPE-19 NI\HdINMcW6jc3WgRZN{[Xl? M133PFUwOTBxMkCg{txO MkXwNlQwPDhiaB?= M{fmdIlvcGmkaYTzJGNMOiCtaX7hd4Uh[WO2aY\peJkh[XRiYTDjc45k\W62cnH0bY9vKG:oIEZCpO69VQ>? NUHkSZRxOjR4OE[wPFA>
ARPE-19 MkPhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrMR2dKOTBizszN MUGyOE06PiCq NIrhbmtFVVOR M1HT[YlvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk> MknXNlQ3QDZyOEC=
HCT116  MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fMRVExKM7:TR?= NXnxfGhtOjRvOU[gbC=> MUTEUXNQ Mk\YbY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> MUWyOFY5PjB6MB?=
ARPE-19 M3rsTmZ2dmO2aX;uJGF{e2G7 M{PYUlExKM7:TR?= M4rKUlQhcA>? NX\l[HlpTE2VTx?= MVjjZZV{\XNiRWKtd5Rz\XO|IILld5BwdnOnIH;2[ZIhfGinIICt[WlHOs7zIHLyZY5kcCxiYoX0JIRw\XNibn;0JIlv\HWlZTDDTG9RyqB? NXXWd21OOjR4OE[wPFA>
HCT116  MXXGeY5kfGmxbjDBd5NigQ>? M1X6bFExKM7:TR?= M4XIPFQhcA>? M1[1T2ROW09? M4n3UYNifXOnczDFVk1{fHKnc4OgdoV{eG:wc3Wgc5ZmeiC2aHWgdE1mUUZ{zsGgZpJidmOqLDDieZQh\G:nczDuc5QhcW6mdXPlJGNJV1EEoB?= M2\JRlI1Pjh4MEiw
HCT116  M17GVWFxd3C2b4Ppd{BCe3OjeR?= MUexNEDPxE1? NYTGN2drOjRxNEigbC=> M{LoS2ROW09? Ml;YbY5lfWOnczDhdI9xfG:|aYO= M3ez[lI1Pjh4MEiw
Nalm6  M1TQRmZ2dmO2aX;uJGF{e2G7 M2XjNlExNzJyIN88US=> NE[wVmYzPCCq M1jsZZJme3WudIOgbY4h\GWlcnXhd4VlKFCWRV6gdIhwe3Cqb4L5cIF1cW:wIHH0JJRp\SCFS{KgeIFz\2W2IILld4llfWViU{O4NEBidmRiY3;uZ49ucXSjboSg[I94dnKnZ4XsZZRqd25ib3[gVHRGViCycn;0[YlvKGW6cILld5Nqd25? NVnITm9POjR3NkG3PVI>
SUP-B15 MXfGeY5kfGmxbjDBd5NigQ>? MnXaNVAwOjBizszN NWjNUpJXOjRiaB?= MWPy[ZN2dHS|IHnuJIRm[3KnYYPl[EBRXEWQIIDoc5NxcG:{eXzheIlwdiCjdDD0bIUhS0t{IIThdodmfCC{ZYPp[JVmKFN|OECgZY5lKGOxbnPvcYl1[W62IHTve45z\We3bHH0bY9vKG:oIGDUSW4heHKxdHXpckBmgHC{ZYPzbY9v NY\iN28yOjR3NkG3PVI>
Nalm6  NFPnO29CeG:ydH;zbZMhSXO|YYm= MnXiOk8yOCEQvF2= MmP2OFghcA>? NWHFeWpycW6mdXPld{BieG:ydH;zbZM> MkH6NlQ2PjF5OUK=
SUP-B15 MVrBdI9xfG:|aYOgRZN{[Xl? MlTsOk8yOCEQvF2= NF3H[Ik1QCCq MVzpcoR2[2W|IHHwc5B1d3Orcx?= NHe2RZYzPDV4MUe5Ni=>
C2C12 NXy5VYFVTnWwY4Tpc44hSXO|YYm= NYfMUotZOyEQvF2= MWOxNk8zPC92ODDo MULpcohq[mm2czD0bIUh\XiycnXzd4lwdiCxZjDvd5Rmd2OuYYP0JIRq\m[ncnXueIlifGmxbjDtZZJs\XK|IHHu[EBCc3RicHjvd5Bpd3K7bHH0bY9v Ml7WNlQzQTNyMUG=
Jurkat M{PP[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7jUHYyNTFyIN88US=> NHv2fVA1QCCq NX32SWs3UUN3ME20Mlkh|ryP NUDCNHo5OjR{NUOwNlQ>
CEM-R NUPlNWNZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWP6VGtnOS1zMDFOwG0> NGi3VXE1QCCq MULJR|UxRTRizszN M2rVVVI1OjV|MEK0
CEM-S MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;GOFEuOTBizszN NHnhWGk1QCCq MX;JR|UxRTRwNjFOwG0> NEjKVY4zPDJ3M{CyOC=>
MOLT-4 M1fGWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHQS|gyNTFyIN88US=> MWe0PEBp NFvHR|dKSzVyPUWuO{DPxE1? NVjUS|dqOjR{NUOwNlQ>
PF-382 MoC4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUOxMVExKM7:TR?= M3K0UlQ5KGh? MoLOTWM2OD12LkWg{txO NITMSmQzPDJ3M{CyOC=>
ALL-SIL NFW4N4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2S5SlEuOTBizszN Mly2OFghcA>? M{O3NGlEPTB;NT63JO69VQ>? M4H5RVI1OjV|MEK0
HPB-ALL NEnSeWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jPUlEuOTBizszN NF3Ubo41QCCq M3fP[mlEPTB;Nj6xJO69VQ>? NUXo[JRkOjR{NUOwNlQ>
DND-41 NXPUTIpGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1PXUlEuOTBizszN M{PwU|Q5KGh? MXjJR|UxRTlizszN MVKyOFI2OzB{NB?=
ALL-SIL MlXrRZBweHSxc3nzJGF{e2G7 MmnYOUDPxE1? NYD1fo9UOjRxNEigbC=> NXvRUoRjcW6mdXPld{BieG:ydH;zbZM> MUGyOFI2OzB{NB?=
DND-41 MY\BdI9xfG:|aYOgRZN{[Xl? M3L4dlUh|ryP MmDONlQwPDhiaB?= MY\pcoR2[2W|IHHwc5B1d3Orcx?= NUX1XG9FOjR{NUOwNlQ>
MOLT-4 NYrqUVI2SXCxcITvd4l{KEG|c3H5 NXi5V2gxPSEQvF2= NXLEbHRJOjRxNEigbC=> M3G5Xolv\HWlZYOgZZBweHSxc3nz MYKyOFI2OzB{NB?=
U-266 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFPseYMxNTRyIN88US=> M3LkOlQ5KGh? MWLJR|UxRTF7LkigxtVOyqB? MUiyOFA5PjR7NB?=
INA-6 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvTeGExOC12MDFOwG0> MU[0PEBp M{Xj[GlEPTB;Mj60NkDDvU1? NIK4N5gzPDB6NkS5OC=>
Jeko-1 M3uwemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHyNE01OCEQvF2= NVGyb5RNPDhiaB?= NXW3W3pxUUN3ME2yMlQhyrWPwrC= NVzrcnNrOjRyOE[0PVQ>
Rec-1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHCNE01OCEQvF2= NYDaU3FSPDhiaB?= MkK4TWM2OD1zLkS2JOK2VcLi M2L6dFI1ODh4NEm0
A549 NVnUXZRwTnWwY4Tpc44hSXO|YYm= MkW2NVAh|ryP M3r1ZVEzNzJ2L{S4JIg> M1i0eolvcGmkaYTzJHRITi4QskGtbY5lfWOnZDDtbYdz[XSrb36gZY5lKGmwdnHzbY9v NWrzPHpHOjRyMkO5N|g>
A549 NVzh[|BMTnWwY4Tpc44hSXO|YYm= M3jGVVMh|ryP NH7OdYE1QCCq NGXKVmlqdmirYnn0d{BVT0ZvzsKxMYlv\HWlZXSgZYN1cX[jdHnvckBw\iCVbXHkJIFv\CCneIDy[ZN{cW:wIH;mJHNv[WmuIHHu[EBVf2m|dB?= M{PLN|I1ODJ|OUO4
S-LAMA84 MULGeY5kfGmxbjDBd5NigQ>? M2DRTlPDqM7:TR?= M1\qfVI1KGh? NUnYSIJGTE2VTx?= MXfy[YR2[2W|IFPLNkBi[3Srdnn0fS=> MoTtNlQxOTJzMEm=
R-LAMA84 NGnWNXdHfW6ldHnvckBCe3OjeR?= NHfEU44{yqEQvF2= NVTpSVBmOjRiaB?= M2izOmROW09? NV7OW|A3emWmdXPld{BEUzJiYXP0bZZqfHl? M4HJVVI1ODF{MUC5
S-LAMA84 MlG3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWOyMlUuOTBizszN Ml7kOFghcA>? NHzPR4NFVVOR MojxbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> M{PTNVI1ODF{MUC5
R-LAMA84 M3zWdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPzNk42NTFyIN88US=> Mlm5OFghcA>? MlHzSG1UVw>? NVrwXodPcW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? MmjENlQxOTJzMEm=
A549 NFTaO5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYWxTI9FOC1|MDFOwG0> M3OwSVczKGh? NGm4NYpFVVOR NUjnT4VYUUN3ME20MlE2KM7:TTygbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> NIXEeoozOzZ3MUS0Ny=>
H1299 M{\qUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnSZW0xNTNyIN88US=> MYO3NkBp NXS1eWl4TE2VTx?= M{TaXWlEPTB;MT64NEDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJINwdmOnboTyZZRqd25iZHXw[Y5l\W62bIm= MknwNlM3PTF2NEO=
A549 MlL1SpVv[3Srb36gRZN{[Xl? M2nQTlEwOTBizszN MUO0PEBp MXLEUXNQ M{fONYxm[WS|IITvJIEh\G:|ZT3k[ZBmdmSnboSg[IVkemWjc3WgbY4hVm:2Y3igdoVxd3K2ZYKgZYN1cX[rdIm= MVmyN|Y2OTR2Mx?=
LNCap NF7pSYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoS5NE0{OCEQvF2= M17aelQh\A>? NX\oc5E4UUN3ME20MlU6yqEQvF2= MnXGNlI5OzJ|MU[=
A431  NWi2cYVyTnWwY4Tpc44hSXO|YYm= M1nzflExKM7:TR?= M1judVMxKG2rbh?= NEXzTXFifHSnboXheIV{KFCLM1utRYt1NW2WT2Kgd4lodmGuaX7n NXntcGVvOjJ|OEe5PFg>
H2170  M1;MXmZ2dmO2aX;uJGF{e2G7 M2rIblExKM7:TR?= MkLFN|AhdWmw M17JboF1fGWwdXH0[ZMhWEl|Sz3Bb5QudVSRUjDzbYdv[Wyrbne= MV2yNlM5Pzl6OB?=
A431  NHnS[4NHfW6ldHnvckBCe3OjeR?= Ml7CNVAh|ryP M3nKWlQuOjRiaB?= MkG2[Y5p[W6lZYOgZZBweHSxc3nzJJdqfGhiZYLsc5Rqdmmk Mk\5NlI{QDd7OEi=
H2170  MmqxSpVv[3Srb36gRZN{[Xl? MkiyNVAh|ryP NFLwN4E1NTJ2IHi= NV7VWJpp\W6qYX7j[ZMh[XCxcITvd4l{KHerdHig[ZJtd3Srbnni NVLsb|dtOjJ|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 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 )

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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).

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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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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

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