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 NETwU2NMcW6jc3WgRZN{[Xl? MUKxM|UwOTBizszN NYfYS|BvOC53IHi= NHTMNnZFVVOR M3;WO5Jm\HWlZYOgR2szKGurbnHz[UBi[3Srdnn0fUBidmRicHzheIVt\XRiYXfndoVo[XSrb36= M2HPbFI3OzhzNEO3
HDMEC NGSwW2pMcW6jc3WgRZN{[Xl? NWfBUGxCOC5{NT:wMlUwOSEQvF2= Mk\lNlQhcA>? MorHSG1UVw>? NYPRfJVkemWmdXPld{BEUzJia3nuZZNmKGGldHn2bZR6NCC4V1[g[ZhxemW|c3nvckBidmRic3XjdoV1cW:w NEXwcZAzPjN6MUSzOy=>
HDMEC M1y3UWZ2dmO2aX;uJGF{e2G7 M2GwZlAvOjVxMD61M|Eh|ryP NH7DO|UzPCCq MWnEUXNQ M3jOXJJm\HWlZYOg[ZhxemW|c3nvckBw\iCYQ1HNMVEh[nW2IH7veEBKS0GPLUG= M2LRXVI3OzhzNEO3
HDMEC NUDqcnhoTnWwY4Tpc44hSXO|YYm= NVLPXYI3OSEQvF2= NVf0VHJTOjRiaB?= M3nVdGROW09? NHHnWoli\m[nY4TzJJN2[mOnbHz1cIFzKGyxY3HsbZpifGmxbjDv[kBPTkGWY{GgZY5lKHCqb4PwbI8ueDZ3 M4m4cVI3OzhzNEO3
A549  M1S3PGZ2dmO2aX;uJGF{e2G7 NIWzcHg{NzFywrFOwG0> NGnNZVY1QCCq NYXyeJpQe3WycILld5NmeyC2aHWgcYlkem:yaXzsZZIucW6mdXPl[EBmgHC{ZYPzbY9vKG:oIICtSmFM M4HyXVI3OzF6OECw
HDMEC NYPsTGpjU2mwYYPlJGF{e2G7 MYGxMVUxKM7:TR?= MWW1JIg> NIjQdFNFVVOR MWfk[YNz\WG|ZYOgR2szKGurbnHz[UBi[3Srdnn0fUB4cXSqb4X0JIFn\mWldHnu[{Bk\WyuII\pZYJqdGm2eR?= NWPyfFJlOjZzOEm1PFY>
HDMEC NGq0OFJHfW6ldHnvckBCe3OjeR?= Mn;YOVAh|ryP NYPnOoluOS93IHi= M4XUcmROW09? MUXk[YNz\WG|ZYOgeIhmKG63Y3zlZZIhe2mpbnHsJI9nKHCqb4PwbI9zgWyjdHXkJJA3PSCrbjDUUmYu|rFvc4TpcZVt[XSnZDDISG1GS8Li MYKyOlE5QTV6Nh?=
HEK293 NVrXeXY6U2mwYYPlJGF{e2G7 NH:zdYQxNjYEoN88US=> MVWxOUBucW5? M2rKb2ROW09? MYry[YR2[2W|IFPLNkBscW6jc3WgZYN1cX[rdIm= NIXYUoMzPTh6N{[yOi=>
Hela MXLLbY5ie2ViQYPzZZk> M4PMTVAvPcLizszN NYeyZW8xOTVibXnu NXq4b4h1TE2VTx?= MVPy[YR2[2W|IFPLNkBscW6jc3WgZYN1cX[rdIm= NI\LcIczPTh6N{[yOi=>
LAMA84 MWrLbY5ie2ViQYPzZZk> MXewMlXDqM7:TR?= NGjTT2IyPSCvaX6= M3fqR2ROW09? NY\5bpJ7emWmdXPld{BEUzJia3nuZZNmKGGldHn2bZR6 MWKyOVg5PzZ{Nh?=
HEK293 NFzzW|JHfW6ldHnvckBCe3OjeR?= M4LjUFMh|ryP NXXFfVNmPSCq M4r5cWROW09? MlLGR2szKHCqb4PwbI9zgWyjdHXzJIVKTjOsIHH0JHNmejF{Nx?= NUP3e2d{OjV6OEe2NlY>
UM-SCC1 NV3NbHZZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHONE4yNTNyIN88US=> MkfMNU02KGR? M{e4[2lEPTB;ND6xJO69VQ>? NYq3W3JqOjV5OUiwOlE>
UM-SCC46 MkT3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrlWI1KOC5zLUOwJO69VQ>? NUDyXIZ3OS13IHS= NIP1bWJKSzVyPUOuOEDPxE1? MWKyOVc6QDB4MR?=
UM-SCC1 MYTGeY5kfGmxbjDBd5NigQ>? M3PmelAvPS92L{GwJO69VQ>? NUPxUlE{PzJiaB?= Ml[z[I94di2{ZXf1cIF1\XNidHjlJIV5eHKnc4Ppc44hd2ZiTl[tyNhDNCCEY3ytXGwh[W6mIIXwMZJm\3WuYYTld{B1cGViZYjwdoV{e2mxbjDv[kBxPTNuIICyNUwhSVBvMTDhcoQhUUxvODDjc45k\W62cnH0bY9vKGSncHXu[IVvfGy7 NF3DVWozPTd7OEC2NS=>
UM-SCC46 M{\HZWZ2dmO2aX;uJGF{e2G7 NYO1NYJsOC53L{SvNVAh|ryP M{P6blczKGh? NWHFd3h{\G:5bj3y[Yd2dGG2ZYOgeIhmKGW6cILld5Nqd25ib3[gUmYuzLiELDDCZ4wuYExuIIC1N{wheDJzLDDBVE0yKGGwZDD1dE1z\We3bHH0[ZMhfGinIHX4dJJme3Orb36gTWwuQCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NVjMSXZIOjV5OUiwOlE>
NU-DUL NYjZ[GxxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlriOU0zPSEQvF2= NXXyUFJKPDhiaB?= MlrNbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> NHH2WHQzPTd6OEK2PS=>
Oci Ly 3 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYS0NYlJPS1{NTFOwG0> NUX4dJV1PDhiaB?= MmL1bY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> MmLwNlU4QDh{Nkm=
Oci Ly 10 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\GVlg2NTJ3IN88US=> NV\B[GJnPDhiaB?= NV3neXpscW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? M3nFUFI2Pzh6Mk[5
Oci Ly 1 NWjnXFZnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1PxfFUuOjVizszN MoD2OFghcA>? NVXlT4s6cW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? NWjtSWUyOjV5OEiyOlk>
Oci Ly 18 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjrOU0zPSEQvF2= MnHYOFghcA>? M17sfIlvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> NHTl[YkzPTd6OEK2PS=>
Oci Ly 19  NIeyWllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DxOFUuOjVizszN NWGyc|B[PDhiaB?= NGLLd2RqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 MV:yOVc5QDJ4OR?=
Raji MljmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rSSVUuOjVizszN MV60PEBp M2XIc4lvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> M{PkV|I2Pzh6Mk[5
H1299 M3zHeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDnNU82NzFyIN88US=> NEjhNGg4OiCq MWjpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 MYWyOVc2ODNyOB?=
Calu-1  MljvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\YSpYyNzVxMUCg{txO MYm3NkBp MYHpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 M1fZOlI2PzVyM{C4
H358 MlzNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2O4eFEwPS9zMDFOwG0> NXu3Wo81PzJiaB?= M2jYe4lvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> MoHVNlU4PTB|MEi=
H1299 MkjxRZBweHSxc3nzJGF{e2G7 NFqy[ZEyOCEQvF2= NX\5SWJzPzJiaB?= MlSxbY5lfWOnczDhdI9xfG:|aYO= NHzJR4QzPTd3MEOwPC=>
Calu-1  MVTBdI9xfG:|aYOgRZN{[Xl? Mn\UNVAh|ryP M3zrXlczKGh? MlrmbY5lfWOnczDhdI9xfG:|aYO= Ml7QNlU4PTB|MEi=
H358 NYrvUnR7SXCxcITvd4l{KEG|c3H5 M1vxU|ExKM7:TR?= MW[3NkBp Mn\tbY5lfWOnczDhdI9xfG:|aYO= NIrYV5kzPTd3MEOwPC=>
PC9/GR MXvGeY5kfGmxbjDBd5NigQ>? NXOzdpdLPSEEtV2= MUC0PEBp M3PWfYlv\HWlZYOgZZV1d3CqYXf5 MUGyOVQ5PjRyOR?=
PC9/ER NXLXUGNJTnWwY4Tpc44hSXO|YYm= MYS1JOK2VQ>? NGC1SII1QCCq NVroTXo6cW6mdXPld{BifXSxcHjh[5k> M3fhcFI2PDh4NEC5
H28 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUWwMlAyNTNyIN88US=> NUX6O|dGPzJiaB?= M3f4cGROW09? NGH4UHRKSzVyPUeuNkDPxE1? MkjPNlU1OjJyOEG=
H2052 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYewMlAyNTNyIN88US=> MWm3NkBp MnruSG1UVw>? M3vrNmlEPTB;Mj6wJO69VQ>? MoDENlU1OjJyOEG=
UM-SCC-1 NEnuOFREdG:wb3flcolkKEG|c3H5 NILJepoxNjVvNTFOwG0> NIDwTYUyPCCm Mnu2SG1UVw>? NVryOFg2yqCrbnjpZol1eyClbH;uc4dmdmmlIIP1dpZqfmGuIHHu[EB{eGincnWg[o9zdWG2aX;u MlHGNlU{PzlyMU[=
UM-SCC-46 M3ryPWNtd26xZ3XubYMhSXO|YYm= NXzxbVJpOC53LUWg{txO NEDoZVQyPCCm MWfEUXNQ NIPDc4bDqGmwaHnibZR{KGOub37v[4VvcWNic4Xyeol3[WxiYX7kJJNxcGW{ZTDmc5Ju[XSrb36= NIiyUXYzPTN5OUCxOi=>
U87-MG MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVSxM|UwOTBizszN M3G1VFI1NzR6L{eyJIg> NHXXb|RFVVOR NGiwdGJqdmirYnn0d{Bk\WyuIHfyc5d1cCCkb4ToJINwdmOnboTyZZRqd25iYX7kJJRqdWViZHXw[Y5l\W62bIm= M3K3NlI2OjRzOEm3
MDA-MB-231 MY\GeY5kfGmxbjDBd5NigQ>? MoPKNk82NzFyIN88US=> NYjxN5lHPCCq MX7k[YNz\WG|ZYOgeIhmKGOxboP0bZR2fGm4ZTDwbI9{eGixconsZZRqd25ib3[gZo91cCBicD3TOVI6NXB4NTDhcoQheC2VMUK5MWFsfA>? NYDWTIxTOjVzNUO3NlU>
MDA-MB-231 NF\BdIRHfW6ldHnvckBCe3OjeR?= MknzNk82NzFyIN88US=> NWDH[2FDPCCq M{nH[IlvcGmkaYTzJJNmemmwZTC1NlkheGixc4Doc5J6dGG2aX;uJIFv\CC2aHWg[ZhxemW|c3nvckBw\iCLTD22MEBKVC16 MV2yOVE2Ozd{NR?=
ARPE-19 NWLQcHVZU2mwYYPlJGF{e2G7 M13BWVUwOTBxMkCg{txO MoLRNlQwPDhiaB?= NI\OdWlqdmirYnn0d{BEUzJia3nuZZNmKGGldHn2bZR6KGG2IHGgZ49v[2WwdILheIlwdiCxZjC1xsDPxE1? NHK2[WkzPDZ6NkC4NC=>
ARPE-19 NFPOfIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXTRXVYOTBizszN NYPySlBXOjRvOU[gbC=> NHfPd2JFVVOR MmrBbY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> NXPVPVdPOjR4OE[wPFA>
HCT116  NI\NV3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPRfmJ{OTBizszN NWDaTYYyOjRvOU[gbC=> NGfNXpFFVVOR M{\zT4lvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk> NEG5c5gzPDZ6NkC4NC=>
ARPE-19 NVfhe3RqTnWwY4Tpc44hSXO|YYm= NF7TOmIyOCEQvF2= NGPuVIg1KGh? NWTJ[JdETE2VTx?= NWLqTHRJ[2G3c3XzJGVTNXO2cnXzd{Bz\XOyb37z[UBwfmW{IITo[UBxNWWLRkNOtUBjemGwY3isJIJ2fCCmb3XzJI5wfCCrbnT1Z4UhS0iRUNMg MUeyOFY5PjB6MB?=
HCT116  M4Dnd2Z2dmO2aX;uJGF{e2G7 NXG1ZWp7OTBizszN Mly4OEBp NY\MVGRSTE2VTx?= NXnBOo5I[2G3c3XzJGVTNXO2cnXzd{Bz\XOyb37z[UBwfmW{IITo[UBxNWWLRkNOtUBjemGwY3isJIJ2fCCmb3XzJI5wfCCrbnT1Z4UhS0iRUNMg NUfDOlB6OjR4OE[wPFA>
HCT116  NVflcVJkSXCxcITvd4l{KEG|c3H5 NF7BOIoyOCEQvF2= NVO4OVVuOjRxNEigbC=> NHvyPXRFVVOR M{nrPIlv\HWlZYOgZZBweHSxc3nz MUOyOFY5PjB6MB?=
Nalm6  MkTpSpVv[3Srb36gRZN{[Xl? NFjHRZIyOC9{MDFOwG0> M1HrN|I1KGh? NYjUXm5{emW|dXz0d{BqdiCmZXPy[YF{\WRiUGTFUkBxcG:|cHjvdplt[XSrb36gZZQhfGinIFPLNkB1[XKpZYSgdoV{cWS3ZTDTN|gxKGGwZDDjc45kd22rdHHueEBld3ewcnXneYxifGmxbjDv[kBRXEWQIIDyc5RmcW5iZYjwdoV{e2mxbh?= NHG1dmkzPDV4MUe5Ni=>
SUP-B15 NGPqUo9HfW6ldHnvckBCe3OjeR?= NI[1boMyOC9{MDFOwG0> NEHHSYgzPCCq NXOyU|RKemW|dXz0d{BqdiCmZXPy[YF{\WRiUGTFUkBxcG:|cHjvdplt[XSrb36gZZQhfGinIFPLNkB1[XKpZYSgdoV{cWS3ZTDTN|gxKGGwZDDjc45kd22rdHHueEBld3ewcnXneYxifGmxbjDv[kBRXEWQIIDyc5RmcW5iZYjwdoV{e2mxbh?= MUiyOFU3OTd7Mh?=
Nalm6  M{Cwd2Fxd3C2b4Ppd{BCe3OjeR?= M1z1NFYwOTBizszN M3HubFQ5KGh? MXvpcoR2[2W|IHHwc5B1d3Orcx?= NFzCRpczPDV4MUe5Ni=>
SUP-B15 MnniRZBweHSxc3nzJGF{e2G7 MVm2M|ExKM7:TR?= NGf3d4w1QCCq NUjPfW5NcW6mdXPld{BieG:ydH;zbZM> NEX2R|kzPDV4MUe5Ni=>
C2C12 NVfqTG4{TnWwY4Tpc44hSXO|YYm= MX:zJO69VQ>? NY[1SFhIOTJxMkSvOFghcA>? MVzpcohq[mm2czD0bIUh\XiycnXzd4lwdiCxZjDvd5Rmd2OuYYP0JIRq\m[ncnXueIlifGmxbjDtZZJs\XK|IHHu[EBCc3RicHjvd5Bpd3K7bHH0bY9v MnvFNlQzQTNyMUG=
Jurkat NI\0VYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHT1O5EyNTFyIN88US=> NGnnN5o1QCCq MorvTWM2OD12Lkmg{txO M2jMflI1OjV|MEK0
CEM-R NU\u[XZwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrCNU0yOCEQvF2= M2jXcVQ5KGh? NFS3N5ZKSzVyPUSg{txO M3[4OVI1OjV|MEK0
CEM-S Mn;QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWCxMVExKM7:TR?= NV;GNotJPDhiaB?= M1e3WGlEPTB;ND62JO69VQ>? NEDENoczPDJ3M{CyOC=>
MOLT-4 NGLJ[2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4XpW|EuOTBizszN MlL5OFghcA>? NGTHWYFKSzVyPUWuO{DPxE1? M2\IVlI1OjV|MEK0
PF-382 Ml35S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEm2TZAyNTFyIN88US=> NUDTV5FKPDhiaB?= NF:0O|lKSzVyPUSuOUDPxE1? MVeyOFI2OzB{NB?=
ALL-SIL M1i0XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLpenNMOS1zMDFOwG0> MoW5OFghcA>? MXzJR|UxRTVwNzFOwG0> NE[wT3gzPDJ3M{CyOC=>
HPB-ALL NFHUVI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnacIUzOS1zMDFOwG0> NUPnW2pSPDhiaB?= MnXWTWM2OD14LkGg{txO NGfMZYUzPDJ3M{CyOC=>
DND-41 NF\odpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjoRXhXOS1zMDFOwG0> M1TDSFQ5KGh? NHuwWYNKSzVyPUmg{txO M{DGNlI1OjV|MEK0
ALL-SIL M1n6fWFxd3C2b4Ppd{BCe3OjeR?= NEHmZos2KM7:TR?= MnmzNlQwPDhiaB?= NXPw[ZNscW6mdXPld{BieG:ydH;zbZM> NWLoeXRVOjR{NUOwNlQ>
DND-41 NX;ocXpnSXCxcITvd4l{KEG|c3H5 NYTNU49zPSEQvF2= MXyyOE81QCCq NHLU[3VqdmS3Y3XzJIFxd3C2b4Ppdy=> MWqyOFI2OzB{NB?=
MOLT-4 M3HFNWFxd3C2b4Ppd{BCe3OjeR?= MXu1JO69VQ>? MmH1NlQwPDhiaB?= M2juTolv\HWlZYOgZZBweHSxc3nz MWqyOFI2OzB{NB?=
U-266 NYfVNnFjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TE[lAuPDBizszN NInEe5o1QCCq NGLXXmRKSzVyPUG5MlghyrWPwrC= NHrmUIEzPDB6NkS5OC=>
INA-6 Ml\HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWWwMVQxKM7:TR?= Moi2OFghcA>? NIjPS|dKSzVyPUKuOFIhyrWP MlG1NlQxQDZ2OUS=
Jeko-1 NFLIe2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{e3bVAuPDBizszN MlvUOFghcA>? M1PQNWlEPTB;Mj60JOK2VcLi NHfn[JgzPDB6NkS5OC=>
Rec-1 NGe2S|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWOwMVQxKM7:TR?= NUjy[VJmPDhiaB?= M17RUmlEPTB;MT60OkDDvU4EoB?= NFHj[mczPDB6NkS5OC=>
A549 M3juRWZ2dmO2aX;uJGF{e2G7 MmLxNVAh|ryP NGPiR5oyOi9{ND:0PEBp NY[3XZNJcW6qaXLpeJMhXEeILd8yNU1qdmS3Y3XkJI1q\3KjdHnvckBidmRiaX72ZZNqd25? M1y4eFI1ODJ|OUO4
A549 MUXGeY5kfGmxbjDBd5NigQ>? NHLudpY{KM7:TR?= MUW0PEBp MYjpcohq[mm2czDUS2Yu|rJzLXnu[JVk\WRiYXP0bZZifGmxbjDv[kBUdWGmIHHu[EBmgHC{ZYPzbY9vKG:oIGPuZYltKGGwZDDUe4l{fA>? M1LMPFI1ODJ|OUO4
S-LAMA84 Mm\GSpVv[3Srb36gRZN{[Xl? NF7Xb5o{yqEQvF2= MknVNlQhcA>? MYnEUXNQ MYny[YR2[2W|IFPLNkBi[3Srdnn0fS=> NYGxPIt{OjRyMUKxNFk>
R-LAMA84 M3XDPWZ2dmO2aX;uJGF{e2G7 MUmzxsDPxE1? M1HnWlI1KGh? MW\EUXNQ MUHy[YR2[2W|IFPLNkBi[3Srdnn0fS=> MnTxNlQxOTJzMEm=
S-LAMA84 MlzLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV[yMlUuOTBizszN M{LGOlQ5KGh? MnS0SG1UVw>? NUToUnB6cW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? M1XhW|I1ODF{MUC5
R-LAMA84 MnHXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\ycIczNjVvMUCg{txO MXO0PEBp NH3XVYJFVVOR MnLwbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> MX:yOFAyOjFyOR?=
A549 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHtXYoxNTNyIN88US=> NI\ybm44OiCq M{fpdWROW09? NITlZYhKSzVyPUSuNVUh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 NGjQO3kzOzZ3MUS0Ny=>
H1299 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rKN|AuOzBizszN MU[3NkBp M1fSO2ROW09? MkjwTWM2OD1zLkiwJO69VSxiaX7obYJqfHNiY3XscEBoem:5dHigZ49v[2WwdILheIlwdiCmZYDlcoRmdnSueR?= M4XLOFI{PjVzNESz
A549 MVLGeY5kfGmxbjDBd5NigQ>? Ml3LNU8yOCEQvF2= NWjJZ4xmPDhiaB?= MWXEUXNQ M4XWboxm[WS|IITvJIEh\G:|ZT3k[ZBmdmSnboSg[IVkemWjc3WgbY4hVm:2Y3igdoVxd3K2ZYKgZYN1cX[rdIm= MYGyN|Y2OTR2Mx?=
LNCap MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfLNE0{OCEQvF2= MnLuOEBl M1e4NGlEPTB;ND61PeKh|ryP MkPtNlI5OzJ|MU[=
A431  NUfvTHNmTnWwY4Tpc44hSXO|YYm= MVixNEDPxE1? NHvheVc{OCCvaX6= NU[1S|hp[XS2ZX71ZZRmeyCSSUPLMWFsfC2vVF;SJJNq\26jbHnu[y=> NWHqeJh4OjJ|OEe5PFg>
H2170  NFqz[49HfW6ldHnvckBCe3OjeR?= M3e0[|ExKM7:TR?= M136WVMxKG2rbh?= MUPheJRmdnWjdHXzJHBKO0tvQXv0MY1VV1Jic3nncoFtcW6p NGDUcYYzOjN6N{m4PC=>
A431  NHq2OHBHfW6ldHnvckBCe3OjeR?= MlTZNVAh|ryP NE\FUnY1NTJ2IHi= M3e1TIVvcGGwY3XzJIFxd3C2b4Ppd{B4cXSqIHXycI91cW6rYh?= MnnSNlI{QDd7OEi=
H2170  NG\PV5BHfW6ldHnvckBCe3OjeR?= NFzBOYgyOCEQvF2= M2HoTlQuOjRiaB?= NGnteVVmdmijbnPld{BieG:ydH;zbZMhf2m2aDDldoxwfGmwaXK= M1;5flIzOzh5OUi4

... 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 )

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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