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 NVXjV5lzU2mwYYPlJGF{e2G7 NIDuUlUyNzVxMUCg{txO MknpNE42KGh? MmnlSG1UVw>? NE\kbGdz\WS3Y3XzJGNMOiCtaX7hd4Uh[WO2aY\peJkh[W6mIIDsZZRmdGW2IHHn[5Jm\2G2aX;u MnKxNlY{QDF2M{e=
HDMEC MVvLbY5ie2ViQYPzZZk> NIfTUGIxNjJ3L{CuOU8yKM7:TR?= MWGyOEBp NX\6PYtuTE2VTx?= MmXYdoVlfWOnczDDT|Ihc2mwYYPlJIFkfGm4aYT5MEB3X0ZiZYjwdoV{e2mxbjDhcoQhe2WlcnX0bY9v MWSyOlM5OTR|Nx?=
HDMEC MYTGeY5kfGmxbjDBd5NigQ>? MWCwMlI2NzBwNT:xJO69VQ>? M4e4UFI1KGh? M3nhXmROW09? NXHYfVFvemWmdXPld{BmgHC{ZYPzbY9vKG:oIG\DRW0uOSCkdYSgco91KEmFQV2tNS=> Mme0NlY{QDF2M{e=
HDMEC MmrXSpVv[3Srb36gRZN{[Xl? Mmm3NUDPxE1? MYKyOEBp M4DMVGROW09? MY\h[oZm[3S|IIP1ZoNmdGy3bHHyJIxw[2GuaYrheIlwdiCxZjDOSmFV[zFiYX7kJJBpd3OyaH:tdFY2 NFHVS2YzPjN6MUSzOy=>
A549  NXntPIJ{TnWwY4Tpc44hSXO|YYm= MlLSN{8yOMLizszN NVLQVY9mPDhiaB?= NUnH[FZbe3WycILld5NmeyC2aHWgcYlkem:yaXzsZZIucW6mdXPl[EBmgHC{ZYPzbY9vKG:oIICtSmFM MX2yOlMyQDhyMB?=
HDMEC NUm1NHdUU2mwYYPlJGF{e2G7 MYmxMVUxKM7:TR?= NInIZXU2KGh? NXvX[5pJTE2VTx?= M3GzbYRm[3KnYYPld{BEUzJia3nuZZNmKGGldHn2bZR6KHerdHjveZQh[W[oZXP0bY5oKGOnbHygeoli[mmuaYT5 MVuyOlE5QTV6Nh?=
HDMEC NGPqWYxHfW6ldHnvckBCe3OjeR?= NHS1TWc2OCEQvF2= NX\3PXB2OS93IHi= MXfEUXNQ NVXrfo1z\GWlcnXhd4V{KHSqZTDueYNt\WG{IIPp[45idCCxZjDwbI9{eGixconsZZRm\CCyNkWgbY4hXE6ILd8xMZN1cW23bHH0[YQhUESPRVRCpC=> NEHTOIgzPjF6OUW4Oi=>
HEK293 Ml2yT4lv[XOnIFHzd4F6 NUDqfHVoOC53wrFOwG0> M2S4S|E2KG2rbh?= MnPiSG1UVw>? Mn3SdoVlfWOnczDDT|Ihc2mwYYPlJIFkfGm4aYT5 M1X5c|I2QDh5NkK2
Hela NUjEcoU1U2mwYYPlJGF{e2G7 M37OV|AvPcLizszN MVWxOUBucW5? NUnS[2NCTE2VTx?= MXfy[YR2[2W|IFPLNkBscW6jc3WgZYN1cX[rdIm= MoTTNlU5QDd4Mk[=
LAMA84 MkC4T4lv[XOnIFHzd4F6 MorHNE42yqEQvF2= MYexOUBucW5? MmC3SG1UVw>? MojWdoVlfWOnczDDT|Ihc2mwYYPlJIFkfGm4aYT5 M1nvXlI2QDh5NkK2
HEK293 M1nFSmZ2dmO2aX;uJGF{e2G7 NIrhTVE{KM7:TR?= MV21JIg> MXrEUXNQ NYLvSnFYS0t{IIDoc5NxcG:{eXzheIV{KGWLRkPqJIF1KFOnckGyOy=> MV[yOVg5PzZ{Nh?=
UM-SCC1 MmXMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7uNE4yNTNyIN88US=> MWKxMVUh\A>? MlfmTWM2OD12LkGg{txO MYqyOVc6QDB4MR?=
UM-SCC46 M2HTUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrlNE4yNTNyIN88US=> NGLyW|MyNTViZB?= MlT1TWM2OD1|LkSg{txO NEnxboIzPTd7OEC2NS=>
UM-SCC1 M2TTTmZ2dmO2aX;uJGF{e2G7 NGLQVWgxNjVxND:xNEDPxE1? NXHzXZFTPzJiaB?= MmfM[I94di2{ZXf1cIF1\XNidHjlJIV5eHKnc4Ppc44hd2ZiTl[tyNhDNCCEY3ytXGwh[W6mIIXwMZJm\3WuYYTld{B1cGViZYjwdoV{e2mxbjDv[kBxPTNuIICyNUwhSVBvMTDhcoQhUUxvODDjc45k\W62cnH0bY9vKGSncHXu[IVvfGy7 NYO1fVB3OjV5OUiwOlE>
UM-SCC46 NEP3NHBHfW6ldHnvckBCe3OjeR?= MYiwMlUwPC9zMDFOwG0> MlLiO|IhcA>? NEfDfWlld3ewLYLl[5Vt[XSnczD0bIUh\XiycnXzd4lwdiCxZjDOSk3FwEJuIFLjcE1ZVCxicEWzMEBxOjFuIFHQMVEh[W6mIIXwMZJm\3WuYYTld{B1cGViZYjwdoV{e2mxbjDJUE05KGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> MkKwNlU4QThyNkG=
NU-DUL NETzSmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojCOU0zPSEQvF2= NIH6Voo1QCCq NYLjeFFScW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? MWGyOVc5QDJ4OR?=
Oci Ly 3 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nyNVUuOjVizszN M4K3VlQ5KGh? M4XHcIlvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> NXLGXGU2OjV5OEiyOlk>
Oci Ly 10 M1LYTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUG1MVI2KM7:TR?= NX\GV5RHPDhiaB?= M33MTIlvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> MmLsNlU4QDh{Nkm=
Oci Ly 1 NUTGWXJ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfmSWh5PS1{NTFOwG0> NX35b3NzPDhiaB?= MWrpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 NWW3VGJrOjV5OEiyOlk>
Oci Ly 18 Ml3NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjCVVNuPS1{NTFOwG0> NIHhPVM1QCCq MYrpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 NWLTWoFyOjV5OEiyOlk>
Oci Ly 19  NULSSnhJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkPMOU0zPSEQvF2= Ml3OOFghcA>? Mkf5bY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> Mne3NlU4QDh{Nkm=
Raji NEj5XlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3[5U|UuOjVizszN MYi0PEBp M4T3[olvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> MmW0NlU4QDh{Nkm=
H1299 NInTUHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXEUIoyNzVxMUCg{txO NWH5OGF3PzJiaB?= M4rNRYlvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> NIXjUHMzPTd3MEOwPC=>
Calu-1  NWrLWVV[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2Pre|EwPS9zMDFOwG0> MWK3NkBp MUXpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 NXzaTlF4OjV5NUCzNFg>
H358 M3LjZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjjXXFwOS93L{GwJO69VQ>? M{fTeVczKGh? MmLTbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> MVGyOVc2ODNyOB?=
H1299 NGGycWNCeG:ydH;zbZMhSXO|YYm= NX;aO5ZmOTBizszN M2ryeVczKGh? NInoVWRqdmS3Y3XzJIFxd3C2b4Ppdy=> M1LSZVI2PzVyM{C4
Calu-1  NV:wc2N[SXCxcITvd4l{KEG|c3H5 M4nqZ|ExKM7:TR?= M4L2blczKGh? MULpcoR2[2W|IHHwc5B1d3Orcx?= M{HxNFI2PzVyM{C4
H358 MmPrRZBweHSxc3nzJGF{e2G7 Mo\XNVAh|ryP MnK0O|IhcA>? MknXbY5lfWOnczDhdI9xfG:|aYO= M1jHN|I2PzVyM{C4
PC9/GR MVLGeY5kfGmxbjDBd5NigQ>? M4PTOFUhyrWP MUm0PEBp M4rpdolv\HWlZYOgZZV1d3CqYXf5 NFi4bWkzPTR6NkSwPS=>
PC9/ER MVnGeY5kfGmxbjDBd5NigQ>? MoTPOUDDvU1? M1HyNVQ5KGh? NVrEbGZOcW6mdXPld{BifXSxcHjh[5k> MX[yOVQ5PjRyOR?=
H28 M4D6U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfle5VTOC5yMT2zNEDPxE1? MWe3NkBp NYnZZ2k5TE2VTx?= MoTJTWM2OD15LkKg{txO NVTlUlQzOjV2MkKwPFE>
H2052 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXrTV2V{OC5yMT2zNEDPxE1? MXG3NkBp NV7uVmtRTE2VTx?= MW\JR|UxRTJwMDFOwG0> MlrrNlU1OjJyOEG=
UM-SCC-1 M1HOeWNtd26xZ3XubYMhSXO|YYm= NUTl[ZhyOC53LUWg{txO MWmxOEBl MkTJSG1UVw>? M3ToXeKhcW6qaXLpeJMh[2yxbn;n[Y5q[yC|dYL2bZZidCCjbnSgd5Bp\XKnIH\vdo1ifGmxbh?= Mk\yNlU{PzlyMU[=
UM-SCC-46 Mk\6R4xwdm:pZX7pZ{BCe3OjeR?= NH;seoYxNjVvNTFOwG0> M{TJb|E1KGR? Mo\VSG1UVw>? Ml;PxsBqdmirYnn0d{BkdG:wb3flcolkKHO3co\peoFtKGGwZDDzdIhmemViZn;ycYF1cW:w NULwW2tDOjV|N{mwNVY>
U87-MG MnzRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37FZVEwPS9zMDFOwG0> MV[yOE81QC95MjDo NInk[olFVVOR NF3HOJRqdmirYnn0d{Bk\WyuIHfyc5d1cCCkb4ToJINwdmOnboTyZZRqd25iYX7kJJRqdWViZHXw[Y5l\W62bIm= NVvnNGpSOjV{NEG4PVc>
MDA-MB-231 MlLSSpVv[3Srb36gRZN{[Xl? MmrsNk82NzFyIN88US=> NH;DTlQ1KGh? NHLvU2pl\WO{ZXHz[ZMhfGinIHPvcpN1cXS3dHn2[UBxcG:|cHjvdplt[XSrb36gc4Yh[m:2aDCgdE1UPTJ7LYC2OUBidmRicD3TNVI6NUGtdB?= NWPnbXh1OjVzNUO3NlU>
MDA-MB-231 NIm2RYtHfW6ldHnvckBCe3OjeR?= MYGyM|UwOTBizszN MmnMOEBp NIXTbGxqdmirYnn0d{B{\XKrbnWgOVI6KHCqb4PwbI9zgWyjdHnvckBidmRidHjlJIV5eHKnc4Ppc44hd2ZiSVytOkwhUUxvOB?= NEHkWXEzPTF3M{eyOS=>
ARPE-19 M3LIRmtqdmG|ZTDBd5NigQ>? NWjJfJlYPS9zMD:yNEDPxE1? NWq3NJlyOjRxNEigbC=> MoO1bY5pcWKrdIOgR2szKGurbnHz[UBi[3Srdnn0fUBifCCjIHPvcoNmdnS{YYTpc44hd2ZiNdMg{txO MmniNlQ3QDZyOEC=
ARPE-19 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYWxNEDPxE1? MVuyOE06PiCq NIfOeXpFVVOR M4XjOolvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk> NFPlXFQzPDZ6NkC4NC=>
HCT116  NUDT[pFkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1TiOFExKM7:TR?= MmmyNlQuQTZiaB?= NUm4coVlTE2VTx?= MnrGbY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> NGD3VXUzPDZ6NkC4NC=>
ARPE-19 NFK3OIlHfW6ldHnvckBCe3OjeR?= MmfpNVAh|ryP NHjMc5Y1KGh? MVPEUXNQ MWPjZZV{\XNiRWKtd5Rz\XO|IILld5BwdnOnIH;2[ZIhfGinIICt[WlHOs7zIHLyZY5kcCxiYoX0JIRw\XNibn;0JIlv\HWlZTDDTG9RyqB? M2m1PFI1Pjh4MEiw
HCT116  MlPXSpVv[3Srb36gRZN{[Xl? MkfDNVAh|ryP M4jBO|QhcA>? M37jemROW09? M3PJV4NifXOnczDFVk1{fHKnc4OgdoV{eG:wc3Wgc5ZmeiC2aHWgdE1mUUZ{zsGgZpJidmOqLDDieZQh\G:nczDuc5QhcW6mdXPlJGNJV1EEoB?= NFzVe2IzPDZ6NkC4NC=>
HCT116  M1LsXGFxd3C2b4Ppd{BCe3OjeR?= MV2xNEDPxE1? MVGyOE81QCCq MVzEUXNQ MXLpcoR2[2W|IHHwc5B1d3Orcx?= NEfaW4IzPDZ6NkC4NC=>
Nalm6  NYfpT3RSTnWwY4Tpc44hSXO|YYm= NGH5bXYyOC9{MDFOwG0> M13MeFI1KGh? MmPLdoV{fWy2czDpckBl\WO{ZXHz[YQhWFSHTjDwbI9{eGixconsZZRqd25iYYSgeIhmKEONMjD0ZZJo\XRicnXzbYR2\SCVM{iwJIFv\CClb37jc41qfGGwdDDkc5dvemWpdXzheIlwdiCxZjDQWGVPKHC{b4TlbY4h\XiycnXzd4lwdg>? MmPhNlQ2PjF5OUK=
SUP-B15 NYPQVFdMTnWwY4Tpc44hSXO|YYm= M{P1OlExNzJyIN88US=> M4\iPVI1KGh? NWrLXGpremW|dXz0d{BqdiCmZXPy[YF{\WRiUGTFUkBxcG:|cHjvdplt[XSrb36gZZQhfGinIFPLNkB1[XKpZYSgdoV{cWS3ZTDTN|gxKGGwZDDjc45kd22rdHHueEBld3ewcnXneYxifGmxbjDv[kBRXEWQIIDyc5RmcW5iZYjwdoV{e2mxbh?= NYm4fIM1OjR3NkG3PVI>
Nalm6  MYDBdI9xfG:|aYOgRZN{[Xl? MWS2M|ExKM7:TR?= MlvwOFghcA>? NG\oSoRqdmS3Y3XzJIFxd3C2b4Ppdy=> NVrkO5VMOjR3NkG3PVI>
SUP-B15 NEfG[VFCeG:ydH;zbZMhSXO|YYm= NXTP[5F4Pi9zMDFOwG0> MlPlOFghcA>? NInDdlRqdmS3Y3XzJIFxd3C2b4Ppdy=> MVmyOFU3OTd7Mh?=
C2C12 NWnRc4NZTnWwY4Tpc44hSXO|YYm= NGPtVlU{KM7:TR?= NEjQVJEyOi9{ND:0PEBp MWLpcohq[mm2czD0bIUh\XiycnXzd4lwdiCxZjDvd5Rmd2OuYYP0JIRq\m[ncnXueIlifGmxbjDtZZJs\XK|IHHu[EBCc3RicHjvd5Bpd3K7bHH0bY9v NXnjOlhmOjR{OUOwNVE>
Jurkat MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPkNU0yOCEQvF2= NHrUbnI1QCCq MVjJR|UxRTRwOTFOwG0> NF\GSGUzPDJ3M{CyOC=>
CEM-R NIj1VFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1ToV|EuOTBizszN NXLIdItIPDhiaB?= M1vwbWlEPTB;NDFOwG0> MXeyOFI2OzB{NB?=
CEM-S MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DOZVEuOTBizszN NIXJWVk1QCCq NHWwSo5KSzVyPUSuOkDPxE1? NFHpcHMzPDJ3M{CyOC=>
MOLT-4 NIrVcmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVSyUldUOS1zMDFOwG0> M{\0XFQ5KGh? NY[2[4EyUUN3ME21Mlch|ryP NUTI[Y9pOjR{NUOwNlQ>
PF-382 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4PrXlEuOTBizszN M4Dkb|Q5KGh? NYD0e|VRUUN3ME20MlUh|ryP M2nvcFI1OjV|MEK0
ALL-SIL MoX5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXPSYkyNTFyIN88US=> NVTRbos2PDhiaB?= NFvS[IJKSzVyPUWuO{DPxE1? M4XQU|I1OjV|MEK0
HPB-ALL NW\wcllPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXWxMVExKM7:TR?= MU[0PEBp NHW1SlBKSzVyPU[uNUDPxE1? M{PLRVI1OjV|MEK0
DND-41 NILwd3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWC5O2ZSOS1zMDFOwG0> MmPPOFghcA>? NF7YRXVKSzVyPUmg{txO M3i3[FI1OjV|MEK0
ALL-SIL MonJRZBweHSxc3nzJGF{e2G7 MoXuOUDPxE1? NF7CRY8zPC92ODDo M3:3[olv\HWlZYOgZZBweHSxc3nz NE\vcnozPDJ3M{CyOC=>
DND-41 NIOzZWlCeG:ydH;zbZMhSXO|YYm= NUTGNGllPSEQvF2= NWfVSYRkOjRxNEigbC=> MljRbY5lfWOnczDhdI9xfG:|aYO= M{DKUlI1OjV|MEK0
MOLT-4 NX7zNpg1SXCxcITvd4l{KEG|c3H5 NXS5ZmRrPSEQvF2= NFP6[FMzPC92ODDo NFXib5JqdmS3Y3XzJIFxd3C2b4Ppdy=> M{PHR|I1OjV|MEK0
U-266 MlPIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmC0NE01OCEQvF2= NX\R[ldWPDhiaB?= M1rVUGlEPTB;MUmuPEDDvU4EoB?= M3LSZVI1ODh4NEm0
INA-6 MoX2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37QdVAuPDBizszN MnXaOFghcA>? NELwT2RKSzVyPUKuOFIhyrWP MXSyOFA5PjR7NB?=
Jeko-1 M3nS[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvuNE01OCEQvF2= MV[0PEBp NUj6doNqUUN3ME2yMlQhyrWPwrC= MYOyOFA5PjR7NB?=
Rec-1 Mk\NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\Jd|AuPDBizszN NEnuOnA1QCCq MmPETWM2OD1zLkS2JOK2VcLi NFvzbYkzPDB6NkS5OC=>
A549 MoXMSpVv[3Srb36gRZN{[Xl? M4HMW|ExKM7:TR?= MUWxNk8zPC92ODDo MoXSbY5pcWKrdIOgWGdHNc7{MT3pcoR2[2WmIH3p[5JifGmxbjDhcoQhcW64YYPpc44> M3q4PFI1ODJ|OUO4
A549 M1rJSWZ2dmO2aX;uJGF{e2G7 MV6zJO69VQ>? NUO0XHh7PDhiaB?= NGD0NIFqdmirYnn0d{BVT0ZvzsKxMYlv\HWlZXSgZYN1cX[jdHnvckBw\iCVbXHkJIFv\CCneIDy[ZN{cW:wIH;mJHNv[WmuIHHu[EBVf2m|dB?= NXP1b5UxOjRyMkO5N|g>
S-LAMA84 MkDuSpVv[3Srb36gRZN{[Xl? M1nwR|PDqM7:TR?= MW[yOEBp NVPtO3BJTE2VTx?= NX74SI5zemWmdXPld{BEUzJiYXP0bZZqfHl? NXviWYF[OjRyMUKxNFk>
R-LAMA84 NVLiVVZuTnWwY4Tpc44hSXO|YYm= M{iyZVPDqM7:TR?= MWOyOEBp M1X3eGROW09? NVX1TVJxemWmdXPld{BEUzJiYXP0bZZqfHl? NV[ydW46OjRyMUKxNFk>
S-LAMA84 Mn7IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1:zXFIvPS1zMDFOwG0> M1zE[FQ5KGh? MoDaSG1UVw>? M4DWZ4lvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> NHvqR5gzPDBzMkGwPS=>
R-LAMA84 M1LZ[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPWNk42NTFyIN88US=> NIP4WWg1QCCq NXzpXGF1TE2VTx?= MmXObY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> M4TU[FI1ODF{MUC5
A549 NYDBfXZ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXmNE0{OCEQvF2= MmnYO|IhcA>? MmrCSG1UVw>? NFXBdZRKSzVyPUSuNVUh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 M3K4UFI{PjVzNESz
H1299 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXtXHhTOC1|MDFOwG0> M{HkZVczKGh? M{fMTmROW09? MlzmTWM2OD1zLkiwJO69VSxiaX7obYJqfHNiY3XscEBoem:5dHigZ49v[2WwdILheIlwdiCmZYDlcoRmdnSueR?= MmD1NlM3PTF2NEO=
A549 MWnGeY5kfGmxbjDBd5NigQ>? NEmyOWgyNzFyIN88US=> NYPFWXozPDhiaB?= NHnkTpFFVVOR NXjrVVdqdGWjZIOgeI8h[SCmb4PlMYRmeGWwZHXueEBl\WO{ZXHz[UBqdiCQb4TjbEBz\XCxcoTldkBi[3Srdnn0fS=> Ml\CNlM3PTF2NEO=
LNCap Mn3sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTKNYZkOC1|MDFOwG0> NVvRUmk6PCCm NXPRSosxUUN3ME20MlU6yqEQvF2= NVvxcJNpOjJ6M{KzNVY>
A431  NGDkV2hHfW6ldHnvckBCe3OjeR?= MmPBNVAh|ryP NXjIXGdNOzBibXnu MmPlZZR1\W63YYTld{BRUTONLVHreE1uXE:UIIPp[45idGmwZx?= MUiyNlM5Pzl6OB?=
H2170  M2jETGZ2dmO2aX;uJGF{e2G7 MXSxNEDPxE1? NYfYdYJtOzBibXnu NHvnU3VifHSnboXheIV{KFCLM1utRYt1NW2WT2Kgd4lodmGuaX7n MXeyNlM5Pzl6OB?=
A431  NHPB[GZHfW6ldHnvckBCe3OjeR?= NYjsUZJ[OTBizszN M3S5NVQuOjRiaB?= Mni0[Y5p[W6lZYOgZZBweHSxc3nzJJdqfGhiZYLsc5Rqdmmk M3L6[FIzOzh5OUi4
H2170  NVXIc2lHTnWwY4Tpc44hSXO|YYm= NEDHTFcyOCEQvF2= NVvTWHVDPC1{NDDo NIj4VmFmdmijbnPld{BieG:ydH;zbZMhf2m2aDDldoxwfGmwaXK= NUfJTYM2OjJ|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]
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  • 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 individually and in order:
1% CMC Na
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
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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*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

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