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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4 Customer Reviews

  • Nat Commun 2014 5, 3393. 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 MX\LbY5ie2ViQYPzZZk> NYXMVm1DOS93L{GwJO69VQ>? MXywMlUhcA>? NFexd|hFVVOR M33jNZJm\HWlZYOgR2szKGurbnHz[UBi[3Srdnn0fUBidmRicHzheIVt\XRiYXfndoVo[XSrb36= Mm\CNlY{QDF2M{e=
HDMEC M4eyRWtqdmG|ZTDBd5NigQ>? NE\IO|AxNjJ3L{CuOU8yKM7:TR?= M2W4S|I1KGh? MUfEUXNQ NXm4W3g{emWmdXPld{BEUzJia3nuZZNmKGGldHn2bZR6NCC4V1[g[ZhxemW|c3nvckBidmRic3XjdoV1cW:w NUTBRnB5OjZ|OEG0N|c>
HDMEC NH3WTllHfW6ldHnvckBCe3OjeR?= MXywMlI2NzBwNT:xJO69VQ>? NFHWOVQzPCCq M2SzPGROW09? Ml\FdoVlfWOnczDlfJBz\XO|aX;uJI9nKF[FQV2tNUBjfXRibn;0JGlESU1vMR?= M3\mOFI3OzhzNEO3
HDMEC NVf6WmlQTnWwY4Tpc44hSXO|YYm= NIDVTYgyKM7:TR?= M1fRPFI1KGh? MXPEUXNQ NWixTmxM[W[oZXP0d{B{fWKlZXzseYxieiCub3PhcIl7[XSrb36gc4YhVk[DVHOxJIFv\CCyaH;zdIhwNXB4NR?= MkjwNlY{QDF2M{e=
A549  NFrjSGZHfW6ldHnvckBCe3OjeR?= M1nZb|MwOTEEoN88US=> NE\TR3c1QCCq M3LQSpN2eHC{ZYPz[ZMhfGinIH3pZ5JweGmubHHyMYlv\HWlZXSg[ZhxemW|c3nvckBw\iCyLV\BTy=> NIHIWlAzPjNzOEiwNC=>
HDMEC NWi1OJBLU2mwYYPlJGF{e2G7 NIDKVXkyNTVyIN88US=> MoPNOUBp MYnEUXNQ MV\k[YNz\WG|ZYOgR2szKGurbnHz[UBi[3Srdnn0fUB4cXSqb4X0JIFn\mWldHnu[{Bk\WyuII\pZYJqdGm2eR?= M{\hb|I3OTh7NUi2
HDMEC M1;aeGZ2dmO2aX;uJGF{e2G7 M{iydFUxKM7:TR?= M{WwUlEwPSCq MYnEUXNQ NWXTTWpE\GWlcnXhd4V{KHSqZTDueYNt\WG{IIPp[45idCCxZjDwbI9{eGixconsZZRm\CCyNkWgbY4hXE6ILd8xMZN1cW23bHH0[YQhUESPRVRCpC=> MnXrNlYyQDl3OE[=
HEK293 MmTBT4lv[XOnIFHzd4F6 MYWwMlXDqM7:TR?= NGewPGIyPSCvaX6= NH7VOJFFVVOR M2j6UJJm\HWlZYOgR2szKGurbnHz[UBi[3Srdnn0fS=> M37IelI2QDh5NkK2
Hela M3zWNGtqdmG|ZTDBd5NigQ>? MXmwMlXDqM7:TR?= MXexOUBucW5? MVLEUXNQ MYDy[YR2[2W|IFPLNkBscW6jc3WgZYN1cX[rdIm= MVWyOVg5PzZ{Nh?=
LAMA84 MlLQT4lv[XOnIFHzd4F6 MnLvNE42yqEQvF2= NXn6T3RCOTVibXnu M1XrSmROW09? MnPVdoVlfWOnczDDT|Ihc2mwYYPlJIFkfGm4aYT5 MXKyOVg5PzZ{Nh?=
HEK293 Mny5SpVv[3Srb36gRZN{[Xl? MX:zJO69VQ>? MWq1JIg> NUXyTlZJTE2VTx?= NXHRPIFZS0t{IIDoc5NxcG:{eXzheIV{KGWLRkPqJIF1KFOnckGyOy=> MYCyOVg5PzZ{Nh?=
UM-SCC1 MlThS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1q2NFAvOS1|MDFOwG0> NXfESoVbOS13IHS= NYnZc4k6UUN3ME20MlEh|ryP NWDBWY5COjV5OUiwOlE>
UM-SCC46 MmPrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zjNFAvOS1|MDFOwG0> M2rSdlEuPSCm NV20WYhnUUN3ME2zMlQh|ryP Ml;yNlU4QThyNkG=
UM-SCC1 NFXVeZRHfW6ldHnvckBCe3OjeR?= MlHONE42NzRxMUCg{txO NYS2Zoc1PzJiaB?= M3nuZYRwf25vcnXneYxifGW|IITo[UBmgHC{ZYPzbY9vKG:oIF7GMeS5SixiQnPsMXhNKGGwZDD1dE1z\We3bHH0[ZMhfGinIHX4dJJme3Orb36gc4YheDV|LDDwNlEtKEGSLUGgZY5lKEmOLUigZ49v[2WwdILheIlwdiCmZYDlcoRmdnSueR?= NHfi[GwzPTd7OEC2NS=>
UM-SCC46 NHLhO3VHfW6ldHnvckBCe3OjeR?= NXGzPXg4OC53L{SvNVAh|ryP NV7yc3FZPzJiaB?= MkLa[I94di2{ZXf1cIF1\XNidHjlJIV5eHKnc4Ppc44hd2ZiTl[tyNhDNCCEY3ytXGwtKHB3MzygdFIyNCCDUD2xJIFv\CC3cD3y[Yd2dGG2ZYOgeIhmKGW6cILld5Nqd25iSVytPEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 M3\ENVI2Pzl6ME[x
NU-DUL MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIOySmE2NTJ3IN88US=> M1G1WFQ5KGh? MVPpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 NX7SS3dwOjV5OEiyOlk>
Oci Ly 3 M2Tzcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWm1MVI2KM7:TR?= NHPhXYM1QCCq NXnNTlV4cW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? MonTNlU4QDh{Nkm=
Oci Ly 10 NFvKOpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmLpOU0zPSEQvF2= M3rrc|Q5KGh? Mm\qbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> M1vHcVI2Pzh6Mk[5
Oci Ly 1 M17rW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmmzOU0zPSEQvF2= NHn1W5I1QCCq NH3oeldqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 MWOyOVc5QDJ4OR?=
Oci Ly 18 NV\Ib5oxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYO5dpFsPS1{NTFOwG0> NXvWNFN7PDhiaB?= M2HxeolvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> M{\6XlI2Pzh6Mk[5
Oci Ly 19  M3vLVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\yco0{PS1{NTFOwG0> NUHNVGhTPDhiaB?= MV7pcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 MkTBNlU4QDh{Nkm=
Raji MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUf4dXdkPS1{NTFOwG0> MoLqOFghcA>? NEjjS2RqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 MnnqNlU4QDh{Nkm=
H1299 NYO3d41wT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3wdG16OS93L{GwJO69VQ>? MUK3NkBp M2\EXIlvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> NUT4fWVUOjV5NUCzNFg>
Calu-1  NHruenhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY[xM|UwOTBizszN NU[yNJVsPzJiaB?= MWHpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 MmTFNlU4PTB|MEi=
H358 NILPc5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPYV28yNzVxMUCg{txO NEXWRng4OiCq M2HubIlvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> MornNlU4PTB|MEi=
H1299 NH\WUYlCeG:ydH;zbZMhSXO|YYm= M1vwVFExKM7:TR?= MYe3NkBp Mn;1bY5lfWOnczDhdI9xfG:|aYO= NFr3cZIzPTd3MEOwPC=>
Calu-1  NH;BSlVCeG:ydH;zbZMhSXO|YYm= MmrlNVAh|ryP M4m4[VczKGh? NXzmdolKcW6mdXPld{BieG:ydH;zbZM> M3HZelI2PzVyM{C4
H358 NH31c4NCeG:ydH;zbZMhSXO|YYm= NYHXNoxWOTBizszN NWTDWIVvPzJiaB?= MljMbY5lfWOnczDhdI9xfG:|aYO= NW\aTpBuOjV5NUCzNFg>
PC9/GR MlrJSpVv[3Srb36gRZN{[Xl? MXy1JOK2VQ>? NYfscJJyPDhiaB?= MWDpcoR2[2W|IHH1eI9xcGGpeR?= NYO5S|VPOjV2OE[0NFk>
PC9/ER NF\wZWVHfW6ldHnvckBCe3OjeR?= NF3ad3Q2KML3TR?= NGHKVHc1QCCq NU\ON2RVcW6mdXPld{BifXSxcHjh[5k> M3nzRVI2PDh4NEC5
H28 M1T6W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXmwMlAyNTNyIN88US=> NV;HdWFOPzJiaB?= MWjEUXNQ MWrJR|UxRTdwMjFOwG0> Ml;RNlU1OjJyOEG=
H2052 MnP5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDKNE4xOS1|MDFOwG0> NGHwXVc4OiCq NUTYeGo3TE2VTx?= NWDyWmRtUUN3ME2yMlAh|ryP M3XzbVI2PDJ{MEix
UM-SCC-1 MW\DcI9vd2enbnnjJGF{e2G7 NFrybZoxNjVvNTFOwG0> NIX4dJMyPCCm MkfBSG1UVw>? NGLm[3TDqGmwaHnibZR{KGOub37v[4VvcWNic4Xyeol3[WxiYX7kJJNxcGW{ZTDmc5Ju[XSrb36= NW\LXpVPOjV|N{mwNVY>
UM-SCC-46 MWLDcI9vd2enbnnjJGF{e2G7 M4e4U|AvPS13IN88US=> Ml3KNVQh\A>? NV\vNpFPTE2VTx?= M2fXcuKhcW6qaXLpeJMh[2yxbn;n[Y5q[yC|dYL2bZZidCCjbnSgd5Bp\XKnIH\vdo1ifGmxbh?= MkHWNlU{PzlyMU[=
U87-MG M{PPT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLqS|RqOS93L{GwJO69VQ>? NGDrTokzPC92OD:3NkBp NXe4THhGTE2VTx?= NXi1dHpvcW6qaXLpeJMh[2WubDDndo94fGhiYn;0bEBkd26lZX70doF1cW:wIHHu[EB1cW2nIHTldIVv\GWwdHz5 Mn3ONlUzPDF6OUe=
MDA-MB-231 M2XyfmZ2dmO2aX;uJGF{e2G7 NEPhdpgzNzVxMUCg{txO MnLsOEBp Ml;q[IVkemWjc3XzJJRp\SClb37zeIl1fXSrdnWgdIhwe3Cqb4L5cIF1cW:wIH;mJIJwfGhiIICtV|UzQS2yNkWgZY5lKHBvU{GyPU1Cc3R? M160NVI2OTV|N{K1
MDA-MB-231 MYHGeY5kfGmxbjDBd5NigQ>? MlewNk82NzFyIN88US=> M{K5[VQhcA>? MlXvbY5pcWKrdIOgd4VzcW6nIEWyPUBxcG:|cHjvdplt[XSrb36gZY5lKHSqZTDlfJBz\XO|aX;uJI9nKEmOLU[sJGlNNTh? MViyOVE2Ozd{NR?=
ARPE-19 M2rDbWtqdmG|ZTDBd5NigQ>? NYjnd5lIPS9zMD:yNEDPxE1? NGH6S3AzPC92ODDo NXK4bmVbcW6qaXLpeJMhS0t{IHvpcoF{\SCjY4Tpeol1gSCjdDDhJINwdmOnboTyZZRqd25ib3[gOeKh|ryP NXO2O|FWOjR4OE[wPFA>
ARPE-19 NXy4e3Y5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jn[VExKM7:TR?= MnTUNlQuQTZiaB?= M2XmOWROW09? NVHBdIFDcW6qaXLpeJMh[2WubDDndo94fGhidHnt[UBl\XCnbnTlcpRtgQ>? MXuyOFY5PjB6MB?=
HCT116  NUC0cXVTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPjOY0yOCEQvF2= MnftNlQuQTZiaB?= M{XiWGROW09? M2T5OIlvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk> NGjGT2EzPDZ6NkC4NC=>
ARPE-19 MUDGeY5kfGmxbjDBd5NigQ>? MWqxNEDPxE1? MVO0JIg> MXPEUXNQ MnzZZ4F2e2W|IFXSMZN1emW|czDy[ZNxd26|ZTDveoVzKHSqZTDwMYVKTjMQsTDidoFv[2huIHL1eEBld2W|IH7veEBqdmS3Y3WgR2hQWMLi MnTXNlQ3QDZyOEC=
HCT116  MkfqSpVv[3Srb36gRZN{[Xl? M{j3clExKM7:TR?= MknBOEBp NInjc5hFVVOR NHjXXnJk[XW|ZYOgSXIue3S{ZYPzJJJme3CxboPlJI93\XJidHjlJJAu\UmIMt8xJIJz[W6laDygZpV1KGSxZYOgco91KGmwZIXj[UBEUE:SwrC= NEHk[FkzPDZ6NkC4NC=>
HCT116  MV;BdI9xfG:|aYOgRZN{[Xl? NV7RNJQzOTBizszN M4DqO|I1NzR6IHi= MorrSG1UVw>? NEDoWFVqdmS3Y3XzJIFxd3C2b4Ppdy=> NFu1[VEzPDZ6NkC4NC=>
Nalm6  MUHGeY5kfGmxbjDBd5NigQ>? MVKxNE8zOCEQvF2= Mof2NlQhcA>? M{exVJJme3WudIOgbY4h\GWlcnXhd4VlKFCWRV6gdIhwe3Cqb4L5cIF1cW:wIHH0JJRp\SCFS{KgeIFz\2W2IILld4llfWViU{O4NEBidmRiY3;uZ49ucXSjboSg[I94dnKnZ4XsZZRqd25ib3[gVHRGViCycn;0[YlvKGW6cILld5Nqd25? MlTZNlQ2PjF5OUK=
SUP-B15 Mm\JSpVv[3Srb36gRZN{[Xl? MlLwNVAwOjBizszN M4D2UlI1KGh? M1\vPJJme3WudIOgbY4h\GWlcnXhd4VlKFCWRV6gdIhwe3Cqb4L5cIF1cW:wIHH0JJRp\SCFS{KgeIFz\2W2IILld4llfWViU{O4NEBidmRiY3;uZ49ucXSjboSg[I94dnKnZ4XsZZRqd25ib3[gVHRGViCycn;0[YlvKGW6cILld5Nqd25? MnTvNlQ2PjF5OUK=
Nalm6  MY\BdI9xfG:|aYOgRZN{[Xl? M1i4SFYwOTBizszN MUG0PEBp NYHwSXc3cW6mdXPld{BieG:ydH;zbZM> NHnnbYczPDV4MUe5Ni=>
SUP-B15 NXPEfpRMSXCxcITvd4l{KEG|c3H5 MnntOk8yOCEQvF2= MUS0PEBp NYK3NlhXcW6mdXPld{BieG:ydH;zbZM> NVjtc|V1OjR3NkG3PVI>
C2C12 Mn3LSpVv[3Srb36gRZN{[Xl? NHP2bnY{KM7:TR?= M16xdFEzNzJ2L{S4JIg> NGO4T5BqdmirYnn0d{B1cGViZYjwdoV{e2mxbjDv[kBwe3Snb3PsZZN1KGSrZn\ldoVvfGmjdHnvckBu[XKtZYLzJIFv\CCDa4SgdIhwe3Cqb4L5cIF1cW:w M3HDZVI1Ojl|MEGx
Jurkat M2\m[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfKT|IyNTFyIN88US=> NVjkV21vPDhiaB?= MWfJR|UxRTRwOTFOwG0> M4Czb|I1OjV|MEK0
CEM-R MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHqNU0yOCEQvF2= MmPGOFghcA>? NFjqNoRKSzVyPUSg{txO MnHwNlQzPTNyMkS=
CEM-S MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4S2UlEuOTBizszN MVK0PEBp NX\Pboc5UUN3ME20MlYh|ryP Mme2NlQzPTNyMkS=
MOLT-4 NYO3dIVuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3:zPFEuOTBizszN MofuOFghcA>? MlXhTWM2OD13Lkeg{txO MWCyOFI2OzB{NB?=
PF-382 NX3TN29VT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLRNU0yOCEQvF2= MmLHOFghcA>? M13VVWlEPTB;ND61JO69VQ>? M3zDcVI1OjV|MEK0
ALL-SIL MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTmWpY3OS1zMDFOwG0> Ml\HOFghcA>? M{HWNGlEPTB;NT63JO69VQ>? NXjtZYhuOjR{NUOwNlQ>
HPB-ALL MljxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jXbFEuOTBizszN M3LWcVQ5KGh? MYPJR|UxRTZwMTFOwG0> M2XYelI1OjV|MEK0
DND-41 MmfWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnz5NU0yOCEQvF2= M3m5O|Q5KGh? NF75VoZKSzVyPUmg{txO MVSyOFI2OzB{NB?=
ALL-SIL NWe4Um1NSXCxcITvd4l{KEG|c3H5 NHrV[YU2KM7:TR?= NGL6emYzPC92ODDo M{HDN4lv\HWlZYOgZZBweHSxc3nz Mme2NlQzPTNyMkS=
DND-41 MlqzRZBweHSxc3nzJGF{e2G7 MVO1JO69VQ>? MkT4NlQwPDhiaB?= MWTpcoR2[2W|IHHwc5B1d3Orcx?= NWi1XXdWOjR{NUOwNlQ>
MOLT-4 NYrjNVdESXCxcITvd4l{KEG|c3H5 NHrCWGc2KM7:TR?= NFX3V|czPC92ODDo M4D5folv\HWlZYOgZZBweHSxc3nz NFjtWZIzPDJ3M{CyOC=>
U-266 M1XoWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zhdVAuPDBizszN MkjUOFghcA>? NYOyOHY3UUN3ME2xPU45KML3TdMg NH7IUZkzPDB6NkS5OC=>
INA-6 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XISlAuPDBizszN M2m4SVQ5KGh? MWfJR|UxRTJwNEKgxtVO Ml\hNlQxQDZ2OUS=
Jeko-1 NHfjV3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\0bVAuPDBizszN NGjHNnc1QCCq NHnD[3BKSzVyPUKuOEDDvU4EoB?= M13seVI1ODh4NEm0
Rec-1 M4nKU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkW0NE01OCEQvF2= NFfx[pI1QCCq M4izWmlEPTB;MT60OkDDvU4EoB?= NXPscIo{OjRyOE[0PVQ>
A549 Moe5SpVv[3Srb36gRZN{[Xl? M{m1clExKM7:TR?= MWmxNk8zPC92ODDo MWfpcohq[mm2czDUS2Yu|rJzLXnu[JVk\WRibXnndoF1cW:wIHHu[EBqdn[jc3nvci=> M4rqeVI1ODJ|OUO4
A549 MYjGeY5kfGmxbjDBd5NigQ>? NHv0cGI{KM7:TR?= NWLFPIFSPDhiaB?= MmrabY5pcWKrdIOgWGdHNc7{MT3pcoR2[2WmIHHjeIl3[XSrb36gc4YhW22jZDDhcoQh\XiycnXzd4lwdiCxZjDTcoFqdCCjbnSgWJdqe3R? M3PXNVI1ODJ|OUO4
S-LAMA84 NXnTfYtPTnWwY4Tpc44hSXO|YYm= NH\JbGQ{yqEQvF2= M2nVXlI1KGh? NHnucYFFVVOR NV;rcmk1emWmdXPld{BEUzJiYXP0bZZqfHl? MYmyOFAyOjFyOR?=
R-LAMA84 NUPmTGgzTnWwY4Tpc44hSXO|YYm= MVKzxsDPxE1? M1nnTFI1KGh? MkfySG1UVw>? MWjy[YR2[2W|IFPLNkBi[3Srdnn0fS=> M2rxblI1ODF{MUC5
S-LAMA84 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjpd|czNjVvMUCg{txO NVHiUmNsPDhiaB?= NWPjcYJ7TE2VTx?= M2q3SIlvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> NGiyO4czPDBzMkGwPS=>
R-LAMA84 NYPsRppIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLzcHFEOi53LUGwJO69VQ>? MlPKOFghcA>? M{HqeWROW09? NUDsdZJ6cW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? M1rqWlI1ODF{MUC5
A549 MoLXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXKdoVjOC1|MDFOwG0> MUW3NkBp M4TRbmROW09? M2HZ[WlEPTB;ND6xOUDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJINwdmOnboTyZZRqd25iZHXw[Y5l\W62bIm= NFjK[ZozOzZ3MUS0Ny=>
H1299 MkHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUO2c2RZOC1|MDFOwG0> M4jzXVczKGh? M3jJfWROW09? NXf5[mhUUUN3ME2xMlgxKM7:TTygbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> M1n3WVI{PjVzNESz
A549 NVqwUYttTnWwY4Tpc44hSXO|YYm= NEWybWcyNzFyIN88US=> MkHMOFghcA>? MUfEUXNQ NGXmWmNt\WGmczD0c{BiKGSxc3Wt[IVx\W6mZX70JIRm[3KnYYPlJIlvKE6xdHPoJJJmeG:{dHXyJIFkfGm4aYT5 NXvvRlg1OjN4NUG0OFM>
LNCap NULU[WM2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrUZYFwOC1|MDFOwG0> NWLHdVZ3PCCm NIrJS5ZKSzVyPUSuOVnDqM7:TR?= NEOxcJkzOjh|MkOxOi=>
A431  MWfGeY5kfGmxbjDBd5NigQ>? Mn3RNVAh|ryP NVfjfWgyOzBibXnu MVLheJRmdnWjdHXzJHBKO0tvQXv0MY1VV1Jic3nncoFtcW6p Mo[xNlI{QDd7OEi=
H2170  M1S3dmZ2dmO2aX;uJGF{e2G7 NFn2cVAyOCEQvF2= NYXaOpZQOzBibXnu M2DIPYF1fGWwdXH0[ZMhWEl|Sz3Bb5QudVSRUjDzbYdv[Wyrbne= MmrPNlI{QDd7OEi=
A431  MV\GeY5kfGmxbjDBd5NigQ>? M1fWZ|ExKM7:TR?= NEi0VHk1NTJ2IHi= NV7m[oE6\W6qYX7j[ZMh[XCxcITvd4l{KHerdHig[ZJtd3Srbnni NFrkdJMzOjN6N{m4PC=>
H2170  M3;1SmZ2dmO2aX;uJGF{e2G7 MWexNEDPxE1? M2TzWVQuOjRiaB?= NEXlXXZmdmijbnPld{BieG:ydH;zbZMhf2m2aDDldoxwfGmwaXK= NVjvVVB3OjJ|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 <1 mg/mL
Ethanol <1 mg/mL
In vivo

* 1 mg/ml means slightly soluble or 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
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
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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