CX-4945 (Silmitasertib)

Catalog No.S2248

CX-4945 (Silmitasertib) Chemical Structure

Molecular Weight(MW): 349.77

CX-4945 (Silmitasertib) 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.

Size Price Stock Quantity  
In DMSO USD 291 In stock
USD 170 In stock
USD 320 In stock

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4 Customer Reviews

  • Nat Commun 2014 5, 3393. CX-4945 (Silmitasertib) 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. CX-4945 (Silmitasertib) purchased from Selleck.

  • Cell Signal 2014 26(7), 1567-75. CX-4945 (Silmitasertib) purchased from Selleck.

    Cell Signal 2014 26(7), 1567-75. CX-4945 (Silmitasertib) purchased from Selleck.

Purity & Quality Control

Choose Selective Casein Kinase Inhibitors

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description CX-4945 (Silmitasertib) 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 MVvLbY5ie2ViQYPzZZk> M1L6e|EwPS9zMDFOwG0> Mk\mNE42KGh? MlqxSG1UVw>? M2LM[pJm\HWlZYOgR2szKGurbnHz[UBi[3Srdnn0fUBidmRicHzheIVt\XRiYXfndoVo[XSrb36= MXmyOlM5OTR|Nx?=
HDMEC NHG5cm5McW6jc3WgRZN{[Xl? NX30XZJxOC5{NT:wMlUwOSEQvF2= NUTpZ2hnOjRiaB?= MlTxSG1UVw>? NH;FbpJz\WS3Y3XzJGNMOiCtaX7hd4Uh[WO2aY\peJktKH[ZRjDlfJBz\XO|aX;uJIFv\CC|ZXPy[ZRqd25? NVvzUZFoOjZ|OEG0N|c>
HDMEC M4HKe2Z2dmO2aX;uJGF{e2G7 NXTWcGVGOC5{NT:wMlUwOSEQvF2= Mn;JNlQhcA>? M4jm[2ROW09? NFXnOG5z\WS3Y3XzJIV5eHKnc4Ppc44hd2ZiVlPBUU0yKGK3dDDuc5QhUUODTT2x NYPUWYFiOjZ|OEG0N|c>
HDMEC M1Lqc2Z2dmO2aX;uJGF{e2G7 MnXaNUDPxE1? MmW1NlQhcA>? MVjEUXNQ MYfh[oZm[3S|IIP1ZoNmdGy3bHHyJIxw[2GuaYrheIlwdiCxZjDOSmFV[zFiYX7kJJBpd3OyaH:tdFY2 MmXQNlY{QDF2M{e=
A549  NFnwTGNHfW6ldHnvckBCe3OjeR?= M1rrXFMwOTEEoN88US=> NYXEemp3PDhiaB?= NGLNfZB{fXCycnXzd4V{KHSqZTDtbYNzd3CrbHzhdk1qdmS3Y3XkJIV5eHKnc4Ppc44hd2ZicD3GRWs> M{W1SFI3OzF6OECw
HDMEC NXWwW|NzU2mwYYPlJGF{e2G7 MXKxMVUxKM7:TR?= MknGOUBp M1XnemROW09? MUPk[YNz\WG|ZYOgR2szKGurbnHz[UBi[3Srdnn0fUB4cXSqb4X0JIFn\mWldHnu[{Bk\WyuII\pZYJqdGm2eR?= MUiyOlE5QTV6Nh?=
HDMEC NV[4NndWTnWwY4Tpc44hSXO|YYm= NWixNIZxPTBizszN NUj4UGU5OS93IHi= NYHhTpVRTE2VTx?= NWrJNmk4\GWlcnXhd4V{KHSqZTDueYNt\WG{IIPp[45idCCxZjDwbI9{eGixconsZZRm\CCyNkWgbY4hXE6ILd8xMZN1cW23bHH0[YQhUESPRVRCpC=> MVuyOlE5QTV6Nh?=
HEK293 NEDiTo9McW6jc3WgRZN{[Xl? NHP5SZYxNjYEoN88US=> M4flSVE2KG2rbh?= MXrEUXNQ M13jVpJm\HWlZYOgR2szKGurbnHz[UBi[3Srdnn0fS=> M{TGW|I2QDh5NkK2
Hela M2XJOmtqdmG|ZTDBd5NigQ>? Mk\lNE42yqEQvF2= MUixOUBucW5? NF3sVXJFVVOR NX22OotGemWmdXPld{BEUzJia3nuZZNmKGGldHn2bZR6 NX20W5RsOjV6OEe2NlY>
LAMA84 NHq5UllMcW6jc3WgRZN{[Xl? NVXjVHN4OC53wrFOwG0> NU\od41YOTVibXnu Mom5SG1UVw>? MnLRdoVlfWOnczDDT|Ihc2mwYYPlJIFkfGm4aYT5 MmPxNlU5QDd4Mk[=
HEK293 MVXGeY5kfGmxbjDBd5NigQ>? NVWxcI44OyEQvF2= Mne0OUBp NHzQUZVFVVOR MV;DT|IheGixc4Doc5J6dGG2ZYOg[WlHO2piYYSgV4VzOTJ5 NIntTIgzPTh6N{[yOi=>
UM-SCC1 NInyXYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYOwMlEuOzBizszN NYn5e4FZOS13IHS= NFHXdXNKSzVyPUSuNUDPxE1? MYWyOVc6QDB4MR?=
UM-SCC46 MmDxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LQNlAvOS1|MDFOwG0> MYixMVUh\A>? NUnYZoQ3UUN3ME2zMlQh|ryP Mmn6NlU4QThyNkG=
UM-SCC1 MoDiSpVv[3Srb36gRZN{[Xl? MYKwMlUwPC9zMDFOwG0> M{n5b|czKGh? NVfTVWll\G:5bj3y[Yd2dGG2ZYOgeIhmKGW6cILld5Nqd25ib3[gUmYuzLiELDDCZ4wuYExiYX7kJJVxNXKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCyNUOsJJAzOSxiQWCtNUBidmRiSVytPEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 MmjuNlU4QThyNkG=
UM-SCC46 Mne5SpVv[3Srb36gRZN{[Xl? Mn7KNE42NzRxMUCg{txO MkPnO|IhcA>? NX\GPZpM\G:5bj3y[Yd2dGG2ZYOgeIhmKGW6cILld5Nqd25ib3[gUmYuzLiELDDCZ4wuYExuIIC1N{wheDJzLDDBVE0yKGGwZDD1dE1z\We3bHH0[ZMhfGinIHX4dJJme3Orb36gTWwuQCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 MlzHNlU4QThyNkG=
NU-DUL MljsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmW0OU0zPSEQvF2= M4nwVVQ5KGh? NYL0O5BNcW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? M3PaelI2Pzh6Mk[5
Oci Ly 3 MkS0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfTOU0zPSEQvF2= M3PCcVQ5KGh? M1rpfYlvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> MmfrNlU4QDh{Nkm=
Oci Ly 10 NXzuSWViT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPaOU0zPSEQvF2= NW\aOolnPDhiaB?= Mmr4bY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> M3LPZVI2Pzh6Mk[5
Oci Ly 1 NECxU2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV61MVI2KM7:TR?= MWO0PEBp NGrDW2JqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 MoPrNlU4QDh{Nkm=
Oci Ly 18 MkX4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVK1MVI2KM7:TR?= MmGyOFghcA>? NVLPfIlqcW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? M1;JNlI2Pzh6Mk[5
Oci Ly 19  NF3JOo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWTzU|hUPS1{NTFOwG0> MVe0PEBp MWLpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 MWqyOVc5QDJ4OR?=
Raji M1TPPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFvLTZg2NTJ3IN88US=> NGrZbI81QCCq NYXHXIx4cW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? MojmNlU4QDh{Nkm=
H1299 NFznVItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfwNU82NzFyIN88US=> M4HPZVczKGh? M{\DR4lvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> MlHXNlU4PTB|MEi=
Calu-1  MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWCxM|UwOTBizszN M{jnNVczKGh? NGXXfW1qdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NFnafpgzPTd3MEOwPC=>
H358 Ml3FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVz2R2czOS93L{GwJO69VQ>? NXfmTGxyPzJiaB?= MVHpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 MV2yOVc2ODNyOB?=
H1299 Ml7zRZBweHSxc3nzJGF{e2G7 M{S4T|ExKM7:TR?= NH7KcXU4OiCq M4Cx[Ilv\HWlZYOgZZBweHSxc3nz NUizW3dZOjV5NUCzNFg>
Calu-1  M3LRV2Fxd3C2b4Ppd{BCe3OjeR?= NXTSd|Y1OTBizszN NF3uS3A4OiCq MmPXbY5lfWOnczDhdI9xfG:|aYO= NVLHe3lCOjV5NUCzNFg>
H358 MUPBdI9xfG:|aYOgRZN{[Xl? MUixNEDPxE1? MUe3NkBp MXTpcoR2[2W|IHHwc5B1d3Orcx?= MnHBNlU4PTB|MEi=
PC9/GR MXrGeY5kfGmxbjDBd5NigQ>? MX:1JOK2VQ>? MXS0PEBp MVHpcoR2[2W|IHH1eI9xcGGpeR?= M3nNfVI2PDh4NEC5
PC9/ER NGe3XoFHfW6ldHnvckBCe3OjeR?= NUT1[Y1RPSEEtV2= NEfxeZU1QCCq NFHkU2hqdmS3Y3XzJIF2fG:yaHHnfS=> NXPBNIMyOjV2OE[0NFk>
H28 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnrbWsxNjBzLUOwJO69VQ>? NFvqXZc4OiCq NFrDfYxFVVOR NV;oOGZ[UUN3ME23MlIh|ryP NX\LbJkzOjV2MkKwPFE>
H2052 NEO4ZYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnObXcxNjBzLUOwJO69VQ>? NVG0WINqPzJiaB?= M3v6TWROW09? NX35d|dMUUN3ME2yMlAh|ryP MVOyOVQzOjB6MR?=
UM-SCC-1 MV;DcI9vd2enbnnjJGF{e2G7 MlLvNE42NTVizszN M1TZdFE1KGR? M2q5NmROW09? NV;WPFVuyqCrbnjpZol1eyClbH;uc4dmdmmlIIP1dpZqfmGuIHHu[EB{eGincnWg[o9zdWG2aX;u M2TlUFI2Ozd7MEG2
UM-SCC-46 NW[xNYdxS2yxbn;n[Y5q[yCDc4PhfS=> M3q5XVAvPS13IN88US=> M4HmRlE1KGR? MkL5SG1UVw>? MVJCpIlvcGmkaYTzJINtd26xZ3XubYMhe3W{dnn2ZYwh[W6mIIPwbIVz\SCob4LtZZRqd25? MUWyOVM4QTBzNh?=
U87-MG NW\2bIkzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDUNU82NzFyIN88US=> NFHp[VgzPC92OD:3NkBp M1KzNWROW09? M3fDcolvcGmkaYTzJINmdGxiZ4Lve5RpKGKxdHigZ49v[2WwdILheIlwdiCjbnSgeIlu\SCmZYDlcoRmdnSueR?= MmXBNlUzPDF6OUe=
MDA-MB-231 M{T1WmZ2dmO2aX;uJGF{e2G7 NVrsPXFPOi93L{GwJO69VQ>? MoPzOEBp Ml7Z[IVkemWjc3XzJJRp\SClb37zeIl1fXSrdnWgdIhwe3Cqb4L5cIF1cW:wIH;mJIJwfGhiIICtV|UzQS2yNkWgZY5lKHBvU{GyPU1Cc3R? MnvSNlUyPTN5MkW=
MDA-MB-231 NVvjOoR7TnWwY4Tpc44hSXO|YYm= M1fZOFIwPS9zMDFOwG0> M3q3OVQhcA>? M3nZOYlvcGmkaYTzJJNmemmwZTC1NlkheGixc4Doc5J6dGG2aX;uJIFv\CC2aHWg[ZhxemW|c3nvckBw\iCLTD22MEBKVC16 NFXOTmQzPTF3M{eyOS=>
ARPE-19 M1H4VGtqdmG|ZTDBd5NigQ>? MWi1M|ExNzJyIN88US=> MV:yOE81QCCq Mn\rbY5pcWKrdIOgR2szKGurbnHz[UBi[3Srdnn0fUBifCCjIHPvcoNmdnS{YYTpc44hd2ZiNdMg{txO NHq4N|AzPDZ6NkC4NC=>
ARPE-19 MmPpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\qTlExKM7:TR?= NFnifFYzPC17NjDo M3vz[GROW09? NF[xWXNqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 NFK3eYkzPDZ6NkC4NC=>
HCT116  M4LxSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVj2d4xzOTBizszN M3jKe|I1NTl4IHi= NH7kZ5FFVVOR NHziSGVqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 NWnHdGJxOjR4OE[wPFA>
ARPE-19 MoTaSpVv[3Srb36gRZN{[Xl? MXGxNEDPxE1? MU[0JIg> MVzEUXNQ MWTjZZV{\XNiRWKtd5Rz\XO|IILld5BwdnOnIH;2[ZIhfGinIICt[WlHOs7zIHLyZY5kcCxiYoX0JIRw\XNibn;0JIlv\HWlZTDDTG9RyqB? MYSyOFY5PjB6MB?=
HCT116  MlHxSpVv[3Srb36gRZN{[Xl? MmGxNVAh|ryP NUiw[WJWPCCq MmDhSG1UVw>? MnTWZ4F2e2W|IFXSMZN1emW|czDy[ZNxd26|ZTDveoVzKHSqZTDwMYVKTjMQsTDidoFv[2huIHL1eEBld2W|IH7veEBqdmS3Y3WgR2hQWMLi NFuz[|YzPDZ6NkC4NC=>
HCT116  NUjRcI1FSXCxcITvd4l{KEG|c3H5 NFn1XGMyOCEQvF2= MUKyOE81QCCq NV\XPXAzTE2VTx?= MVXpcoR2[2W|IHHwc5B1d3Orcx?= MXKyOFY5PjB6MB?=
Nalm6  NWLZe4ZLTnWwY4Tpc44hSXO|YYm= MknxNVAwOjBizszN MWeyOEBp NXOxZoRUemW|dXz0d{BqdiCmZXPy[YF{\WRiUGTFUkBxcG:|cHjvdplt[XSrb36gZZQhfGinIFPLNkB1[XKpZYSgdoV{cWS3ZTDTN|gxKGGwZDDjc45kd22rdHHueEBld3ewcnXneYxifGmxbjDv[kBRXEWQIIDyc5RmcW5iZYjwdoV{e2mxbh?= M33S[FI1PTZzN{my
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Nalm6  NEDvbXNCeG:ydH;zbZMhSXO|YYm= MnfmOk8yOCEQvF2= MX[0PEBp NFTMO4NqdmS3Y3XzJIFxd3C2b4Ppdy=> MUGyOFU3OTd7Mh?=
SUP-B15 MYTBdI9xfG:|aYOgRZN{[Xl? M{PaO|YwOTBizszN NIfiTnQ1QCCq M4DXWIlv\HWlZYOgZZBweHSxc3nz M{PsflI1PTZzN{my
C2C12 NFHLTGpHfW6ldHnvckBCe3OjeR?= MWqzJO69VQ>? M1;uUlEzNzJ2L{S4JIg> NHrIbpNqdmirYnn0d{B1cGViZYjwdoV{e2mxbjDv[kBwe3Snb3PsZZN1KGSrZn\ldoVvfGmjdHnvckBu[XKtZYLzJIFv\CCDa4SgdIhwe3Cqb4L5cIF1cW:w MVKyOFI6OzBzMR?=
Jurkat M3rU[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHXNVUxOS1zMDFOwG0> NXzKT3JLPDhiaB?= MnL5TWM2OD12Lkmg{txO NXLQWmdNOjR{NUOwNlQ>
CEM-R M4\nN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrNO5JkOS1zMDFOwG0> M3HsOVQ5KGh? Mn\oTWM2OD12IN88US=> MmrMNlQzPTNyMkS=
CEM-S NGLlXYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPRNU0yOCEQvF2= NGnrOWc1QCCq NHfJZ4ZKSzVyPUSuOkDPxE1? M2fXOVI1OjV|MEK0
MOLT-4 NGG1bHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nHS|EuOTBizszN MmPyOFghcA>? MWXJR|UxRTVwNzFOwG0> NF7PTVUzPDJ3M{CyOC=>
PF-382 MnPaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmW2NU0yOCEQvF2= MkDsOFghcA>? MkLkTWM2OD12LkWg{txO Mn3vNlQzPTNyMkS=
ALL-SIL MkDsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mni1NU0yOCEQvF2= MWi0PEBp NWnEXWlMUUN3ME21Mlch|ryP MV2yOFI2OzB{NB?=
HPB-ALL MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDzNU0yOCEQvF2= NXSyPFNoPDhiaB?= M4rDemlEPTB;Nj6xJO69VQ>? MXuyOFI2OzB{NB?=
DND-41 MkDXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPnTHRPOS1zMDFOwG0> M3f1RlQ5KGh? NFvW[3RKSzVyPUmg{txO M2exUVI1OjV|MEK0
ALL-SIL MnToRZBweHSxc3nzJGF{e2G7 MUS1JO69VQ>? MUCyOE81QCCq NHLqTmxqdmS3Y3XzJIFxd3C2b4Ppdy=> NEm1R4YzPDJ3M{CyOC=>
DND-41 M3[x[2Fxd3C2b4Ppd{BCe3OjeR?= MlzHOUDPxE1? M2DOc|I1NzR6IHi= MoXxbY5lfWOnczDhdI9xfG:|aYO= MVGyOFI2OzB{NB?=
MOLT-4 NHHIV3NCeG:ydH;zbZMhSXO|YYm= NWe5R3lsPSEQvF2= NWDocFREOjRxNEigbC=> NX2y[HR{cW6mdXPld{BieG:ydH;zbZM> MV:yOFI2OzB{NB?=
U-266 MlnES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zoOFAuPDBizszN MoTWOFghcA>? M4fHXWlEPTB;MUmuPEDDvU4EoB?= MWCyOFA5PjR7NB?=
INA-6 MnXuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XYTVAuPDBizszN M4jrRVQ5KGh? NGnnbZNKSzVyPUKuOFIhyrWP MnjONlQxQDZ2OUS=
Jeko-1 M3rjNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXkcXYxNTRyIN88US=> NIOweJQ1QCCq MVTJR|UxRTJwNDFCuW3DqA>? NIrVVnYzPDB6NkS5OC=>
Rec-1 NWPtW2t2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV:1NIdUOC12MDFOwG0> NIDnb4E1QCCq MXTJR|UxRTFwNE[gxtVOyqB? NHrq[2UzPDB6NkS5OC=>
A549 MV;GeY5kfGmxbjDBd5NigQ>? NX;OSJJmOTBizszN NXruO2ZJOTJxMkSvOFghcA>? MYTpcohq[mm2czDUS2Yu|rJzLXnu[JVk\WRibXnndoF1cW:wIHHu[EBqdn[jc3nvci=> NWPCV4NVOjRyMkO5N|g>
A549 M1HtcmZ2dmO2aX;uJGF{e2G7 MYOzJO69VQ>? MmPDOFghcA>? NUjlcG82cW6qaXLpeJMhXEeILd8yNU1qdmS3Y3XkJIFkfGm4YYTpc44hd2ZiU33h[EBidmRiZYjwdoV{e2mxbjDv[kBUdmGrbDDhcoQhXHerc4S= NFeyWZgzPDB{M{mzPC=>
S-LAMA84 M{\zfmZ2dmO2aX;uJGF{e2G7 M3vLc|PDqM7:TR?= NGnURpczPCCq MVfEUXNQ MYPy[YR2[2W|IFPLNkBi[3Srdnn0fS=> Mn;rNlQxOTJzMEm=
R-LAMA84 MkPySpVv[3Srb36gRZN{[Xl? MWqzxsDPxE1? NIjTVFczPCCq MUHEUXNQ M3zQO5Jm\HWlZYOgR2szKGGldHn2bZR6 M3HLblI1ODF{MUC5
S-LAMA84 MnfyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXrNk42NTFyIN88US=> MoPzOFghcA>? M3yzUGROW09? NEPiS3lqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 MWWyOFAyOjFyOR?=
R-LAMA84 MoPES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnqRm0zNjVvMUCg{txO M{XnTVQ5KGh? M{XpVmROW09? NYTsSHoycW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? MXOyOFAyOjFyOR?=
A549 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlS3NE0{OCEQvF2= M4TTdFczKGh? NE\KZ4VFVVOR NGfiW2RKSzVyPUSuNVUh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 NVy5OG17OjN4NUG0OFM>
H1299 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXewMVMxKM7:TR?= NX;wR5NMPzJiaB?= NXfYS5BrTE2VTx?= MnPFTWM2OD1zLkiwJO69VSxiaX7obYJqfHNiY3XscEBoem:5dHigZ49v[2WwdILheIlwdiCmZYDlcoRmdnSueR?= NID4VWkzOzZ3MUS0Ny=>
A549 M33mbWZ2dmO2aX;uJGF{e2G7 M33KflEwOTBizszN NVHzSXhtPDhiaB?= M2iwOGROW09? Mn3CcIVi\HNidH:gZUBld3OnLXTldIVv\GWwdDDk[YNz\WG|ZTDpckBPd3SlaDDy[ZBwenSncjDhZ5Rqfmm2eR?= MnjWNlM3PTF2NEO=
LNCap NV72NZBUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVXXUGlZOC1|MDFOwG0> M1Hzd|Qh\A>? NX\UOphQUUN3ME20MlU6yqEQvF2= Mni5NlI5OzJ|MU[=
A431  M1jOfGZ2dmO2aX;uJGF{e2G7 NYnhTXZROTBizszN MonWN|AhdWmw NVuyeZpT[XS2ZX71ZZRmeyCSSUPLMWFsfC2vVF;SJJNq\26jbHnu[y=> MnOxNlI{QDd7OEi=
H2170  M1ywbGZ2dmO2aX;uJGF{e2G7 MojwNVAh|ryP M3K2TFMxKG2rbh?= MVXheJRmdnWjdHXzJHBKO0tvQXv0MY1VV1Jic3nncoFtcW6p M36zWVIzOzh5OUi4
A431  Mm[2SpVv[3Srb36gRZN{[Xl? NYTDcJhwOTBizszN NET1fWs1NTJ2IHi= MYrlcohidmOnczDhdI9xfG:|aYOge4l1cCCncnzveIlvcWJ? NFOxc4MzOjN6N{m4PC=>
H2170  NXjDd3BbTnWwY4Tpc44hSXO|YYm= MWixNEDPxE1? NWX3c2tJPC1{NDDo NHTYRpBmdmijbnPld{BieG:ydH;zbZMhf2m2aDDldoxwfGmwaXK= NF31bZQzOjN6N{m4PC=>

... 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
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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID