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 NGjzNnFMcW6jc3WgRZN{[Xl? NIP3TlgyNzVxMUCg{txO MWSwMlUhcA>? NHLWOnlFVVOR M2rjNZJm\HWlZYOgR2szKGurbnHz[UBi[3Srdnn0fUBidmRicHzheIVt\XRiYXfndoVo[XSrb36= NXe5c|JoOjZ|OEG0N|c>
HDMEC MXzLbY5ie2ViQYPzZZk> M3TyTFAvOjVxMD61M|Eh|ryP NVrKb40zOjRiaB?= NGTCNWFFVVOR MXzy[YR2[2W|IFPLNkBscW6jc3WgZYN1cX[rdImsJJZYTiCneIDy[ZN{cW:wIHHu[EB{\WO{ZYTpc44> NXz1dZQzOjZ|OEG0N|c>
HDMEC NEjGXGhHfW6ldHnvckBCe3OjeR?= MXqwMlI2NzBwNT:xJO69VQ>? M2PqWFI1KGh? MYDEUXNQ MofIdoVlfWOnczDlfJBz\XO|aX;uJI9nKF[FQV2tNUBjfXRibn;0JGlESU1vMR?= M{fCXVI3OzhzNEO3
HDMEC Ml32SpVv[3Srb36gRZN{[Xl? M3\4cVEh|ryP M2e4dlI1KGh? NXXKSHRWTE2VTx?= M3LEbIFn\mWldIOgd5Vj[2WubIXsZZIhdG:lYXzpfoF1cW:wIH;mJG5HSVSlMTDhcoQheGixc4Doc{1xPjV? MlzYNlY{QDF2M{e=
A549  M3fTemZ2dmO2aX;uJGF{e2G7 M17m[lMwOTEEoN88US=> M3TBNFQ5KGh? M3;Bd5N2eHC{ZYPz[ZMhfGinIH3pZ5JweGmubHHyMYlv\HWlZXSg[ZhxemW|c3nvckBw\iCyLV\BTy=> M17WZ|I3OzF6OECw
HDMEC M{fDVGtqdmG|ZTDBd5NigQ>? MlP3NU02OCEQvF2= NXjwdYFrPSCq NH7USHVFVVOR MYLk[YNz\WG|ZYOgR2szKGurbnHz[UBi[3Srdnn0fUB4cXSqb4X0JIFn\mWldHnu[{Bk\WyuII\pZYJqdGm2eR?= NYm1[4ZVOjZzOEm1PFY>
HDMEC M1fLWWZ2dmO2aX;uJGF{e2G7 Mnr1OVAh|ryP MmHtNU82KGh? NGiwcGdFVVOR MX3k[YNz\WG|ZYOgeIhmKG63Y3zlZZIhe2mpbnHsJI9nKHCqb4PwbI9zgWyjdHXkJJA3PSCrbjDUUmYu|rFvc4TpcZVt[XSnZDDISG1GS8Li MlH1NlYyQDl3OE[=
HEK293 MkjtT4lv[XOnIFHzd4F6 MnzxNE42yqEQvF2= MWqxOUBucW5? NV7WblVPTE2VTx?= MkfYdoVlfWOnczDDT|Ihc2mwYYPlJIFkfGm4aYT5 MY[yOVg5PzZ{Nh?=
Hela M3HtUWtqdmG|ZTDBd5NigQ>? MoixNE42yqEQvF2= NFjrTYIyPSCvaX6= MYrEUXNQ MUTy[YR2[2W|IFPLNkBscW6jc3WgZYN1cX[rdIm= MoHLNlU5QDd4Mk[=
LAMA84 MkTJT4lv[XOnIFHzd4F6 NFf0Zo0xNjYEoN88US=> MkPrNVUhdWmw MkjmSG1UVw>? MUXy[YR2[2W|IFPLNkBscW6jc3WgZYN1cX[rdIm= NIDKfnkzPTh6N{[yOi=>
HEK293 NIDz[IFHfW6ldHnvckBCe3OjeR?= M{\ZblMh|ryP MojqOUBp NVS1TG9XTE2VTx?= MmjhR2szKHCqb4PwbI9zgWyjdHXzJIVKTjOsIHH0JHNmejF{Nx?= MYqyOVg5PzZ{Nh?=
UM-SCC1 NVnQU2d[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLlU|dnOC5zLUOwJO69VQ>? NH;n[3cyNTViZB?= NYPmNIQ{UUN3ME20MlEh|ryP NF\aU4wzPTd7OEC2NS=>
UM-SCC46 M1HYUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\tcYdQOC5zLUOwJO69VQ>? NGeybW0yNTViZB?= NXz6N2diUUN3ME2zMlQh|ryP NH3IVZozPTd7OEC2NS=>
UM-SCC1 NFnpT5FHfW6ldHnvckBCe3OjeR?= NXzNRpN2OC53L{SvNVAh|ryP NWjZcYhvPzJiaB?= NFrjSFhld3ewLYLl[5Vt[XSnczD0bIUh\XiycnXzd4lwdiCxZjDOSk3FwEJuIFLjcE1ZVCCjbnSgeZAuemWpdXzheIV{KHSqZTDlfJBz\XO|aX;uJI9nKHB3MzygdFIyNCCDUD2xJIFv\CCLTD24JINwdmOnboTyZZRqd25iZHXw[Y5l\W62bIm= MWSyOVc6QDB4MR?=
UM-SCC46 MmXBSpVv[3Srb36gRZN{[Xl? NVrHc3ZbOC53L{SvNVAh|ryP MUW3NkBp MX3kc5dvNXKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCQRj5EvGItKEKlbD3YUEwheDV|LDDwNlEtKEGSLUGgZY5lKHWyLYLl[5Vt[XSnczD0bIUh\XiycnXzd4lwdiCLTD24JINwdmOnboTyZZRqd25iZHXw[Y5l\W62bIm= NEnxZWczPTd7OEC2NS=>
NU-DUL MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLxXlE2NTJ3IN88US=> M3vp[lQ5KGh? MnPWbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> M3LqdVI2Pzh6Mk[5
Oci Ly 3 NX3UR5c4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{fYSVUuOjVizszN NVuzNmttPDhiaB?= M3XQUYlvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> M4nC[lI2Pzh6Mk[5
Oci Ly 10 NGDDd5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4T0flUuOjVizszN NWDrVXg4PDhiaB?= MUnpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 M1vzfVI2Pzh6Mk[5
Oci Ly 1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fXOFUuOjVizszN M2PxWlQ5KGh? NV;YfFd[cW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? MWOyOVc5QDJ4OR?=
Oci Ly 18 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXrPRWtFPS1{NTFOwG0> NYPJfYRFPDhiaB?= M3P6colvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> NHHid4IzPTd6OEK2PS=>
Oci Ly 19  MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnKyOU0zPSEQvF2= Mn\4OFghcA>? NEH5SmRqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NEfBeGUzPTd6OEK2PS=>
Raji NVrLN2xxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYW1MVI2KM7:TR?= NYnu[3MyPDhiaB?= MmXVbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> M2\5RlI2Pzh6Mk[5
H1299 NFrzSJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPmNU82NzFyIN88US=> M4PIOFczKGh? MYnpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 Ml\vNlU4PTB|MEi=
Calu-1  Ml\RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M17rVlEwPS9zMDFOwG0> MlPjO|IhcA>? MX;pcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 MWCyOVc2ODNyOB?=
H358 MnfMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fPd|EwPS9zMDFOwG0> NG\Wc|M4OiCq NUD5foRpcW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? NGPZeHEzPTd3MEOwPC=>
H1299 NUXJW5Q1SXCxcITvd4l{KEG|c3H5 NED4bmsyOCEQvF2= M2fIVVczKGh? NYDuXHZYcW6mdXPld{BieG:ydH;zbZM> MkXUNlU4PTB|MEi=
Calu-1  NIf4NlZCeG:ydH;zbZMhSXO|YYm= MV[xNEDPxE1? NEjsRpg4OiCq NHfLUpJqdmS3Y3XzJIFxd3C2b4Ppdy=> M4Hq[VI2PzVyM{C4
H358 NF7VOHhCeG:ydH;zbZMhSXO|YYm= NYfkPG5VOTBizszN NGHETGg4OiCq MWPpcoR2[2W|IHHwc5B1d3Orcx?= NInreoozPTd3MEOwPC=>
PC9/GR NIK0TGxHfW6ldHnvckBCe3OjeR?= NUHMZYcxPSEEtV2= M{jlcVQ5KGh? NYrKdGRkcW6mdXPld{BifXSxcHjh[5k> NE[xNlgzPTR6NkSwPS=>
PC9/ER MYjGeY5kfGmxbjDBd5NigQ>? NFXvSpk2KML3TR?= MWe0PEBp NETaflBqdmS3Y3XzJIF2fG:yaHHnfS=> NXzNOYZZOjV2OE[0NFk>
H28 NG\jbWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnvcnAxNjBzLUOwJO69VQ>? NH60VJQ4OiCq MWHEUXNQ NFP2RZZKSzVyPUeuNkDPxE1? M1L2RVI2PDJ{MEix
H2052 NXLWR4tHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWmwMlAyNTNyIN88US=> MWW3NkBp M2r0[2ROW09? NEHyeIVKSzVyPUKuNEDPxE1? NYj6fHp{OjV2MkKwPFE>
UM-SCC-1 M1TXVWNtd26xZ3XubYMhSXO|YYm= NYfJW3VyOC53LUWg{txO MXexOEBl MWXEUXNQ NXzDUGh2yqCrbnjpZol1eyClbH;uc4dmdmmlIIP1dpZqfmGuIHHu[EB{eGincnWg[o9zdWG2aX;u NGqxcnYzPTN5OUCxOi=>
UM-SCC-46 NIe1b2REdG:wb3flcolkKEG|c3H5 MYiwMlUuPSEQvF2= M{LMU|E1KGR? NXnXdlZITE2VTx?= MmnDxsBqdmirYnn0d{BkdG:wb3flcolkKHO3co\peoFtKGGwZDDzdIhmemViZn;ycYF1cW:w NXK2SXRwOjV|N{mwNVY>
U87-MG M2jKWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2L3UlEwPS9zMDFOwG0> NGruZlgzPC92OD:3NkBp MW\EUXNQ M{i5eolvcGmkaYTzJINmdGxiZ4Lve5RpKGKxdHigZ49v[2WwdILheIlwdiCjbnSgeIlu\SCmZYDlcoRmdnSueR?= NX36SYQ1OjV{NEG4PVc>
MDA-MB-231 NU\tRo5xTnWwY4Tpc44hSXO|YYm= MU[yM|UwOTBizszN MUe0JIg> MkPO[IVkemWjc3XzJJRp\SClb37zeIl1fXSrdnWgdIhwe3Cqb4L5cIF1cW:wIH;mJIJwfGhiIICtV|UzQS2yNkWgZY5lKHBvU{GyPU1Cc3R? NV7SN|l2OjVzNUO3NlU>
MDA-MB-231 Mmq4SpVv[3Srb36gRZN{[Xl? M1P4NlIwPS9zMDFOwG0> NUTaO2JTPCCq MmfSbY5pcWKrdIOgd4VzcW6nIEWyPUBxcG:|cHjvdplt[XSrb36gZY5lKHSqZTDlfJBz\XO|aX;uJI9nKEmOLU[sJGlNNTh? M2LZdVI2OTV|N{K1
ARPE-19 MYfLbY5ie2ViQYPzZZk> M3jkXlUwOTBxMkCg{txO Mni1NlQwPDhiaB?= NHS2[5VqdmirYnn0d{BEUzJia3nuZZNmKGGldHn2bZR6KGG2IHGgZ49v[2WwdILheIlwdiCxZjC1xsDPxE1? M2DD[VI1Pjh4MEiw
ARPE-19 MlPDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmnNNVAh|ryP NYnaXIk3OjRvOU[gbC=> Mo\VSG1UVw>? M4jtNolvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk> NYnHfYFJOjR4OE[wPFA>
HCT116  Mn;QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXu0PGNFOTBizszN Mof4NlQuQTZiaB?= NX7zTmdTTE2VTx?= M4ftN4lvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk> NVj2N4R3OjR4OE[wPFA>
ARPE-19 Ml7rSpVv[3Srb36gRZN{[Xl? NYnpNnpFOTBizszN M{jKNFQhcA>? M4fYWGROW09? MWPjZZV{\XNiRWKtd5Rz\XO|IILld5BwdnOnIH;2[ZIhfGinIICt[WlHOs7zIHLyZY5kcCxiYoX0JIRw\XNibn;0JIlv\HWlZTDDTG9RyqB? MUKyOFY5PjB6MB?=
HCT116  MnHrSpVv[3Srb36gRZN{[Xl? M3HPeVExKM7:TR?= NV:0d|BIPCCq NIO0T2xFVVOR MkDNZ4F2e2W|IFXSMZN1emW|czDy[ZNxd26|ZTDveoVzKHSqZTDwMYVKTjMQsTDidoFv[2huIHL1eEBld2W|IH7veEBqdmS3Y3WgR2hQWMLi NGLHT2wzPDZ6NkC4NC=>
HCT116  Mm[5RZBweHSxc3nzJGF{e2G7 NVy0V28xOTBizszN MkC3NlQwPDhiaB?= NXrjSFFLTE2VTx?= M{XmTYlv\HWlZYOgZZBweHSxc3nz NV\oeWNwOjR4OE[wPFA>
Nalm6  MWjGeY5kfGmxbjDBd5NigQ>? MnjCNVAwOjBizszN NFKweoMzPCCq NV\IUopWemW|dXz0d{BqdiCmZXPy[YF{\WRiUGTFUkBxcG:|cHjvdplt[XSrb36gZZQhfGinIFPLNkB1[XKpZYSgdoV{cWS3ZTDTN|gxKGGwZDDjc45kd22rdHHueEBld3ewcnXneYxifGmxbjDv[kBRXEWQIIDyc5RmcW5iZYjwdoV{e2mxbh?= NGG2WpMzPDV4MUe5Ni=>
SUP-B15 Mln4SpVv[3Srb36gRZN{[Xl? NX;mVllSOTBxMkCg{txO MVmyOEBp NXzvb4RQemW|dXz0d{BqdiCmZXPy[YF{\WRiUGTFUkBxcG:|cHjvdplt[XSrb36gZZQhfGinIFPLNkB1[XKpZYSgdoV{cWS3ZTDTN|gxKGGwZDDjc45kd22rdHHueEBld3ewcnXneYxifGmxbjDv[kBRXEWQIIDyc5RmcW5iZYjwdoV{e2mxbh?= M{ju[FI1PTZzN{my
Nalm6  MnfZRZBweHSxc3nzJGF{e2G7 MnHqOk8yOCEQvF2= NIX0cpY1QCCq MoPIbY5lfWOnczDhdI9xfG:|aYO= NVzySmZZOjR3NkG3PVI>
SUP-B15 MXvBdI9xfG:|aYOgRZN{[Xl? NHLqNHQ3NzFyIN88US=> M{TyR|Q5KGh? MYHpcoR2[2W|IHHwc5B1d3Orcx?= NGDwe3AzPDV4MUe5Ni=>
C2C12 M4XXe2Z2dmO2aX;uJGF{e2G7 M{DLUVMh|ryP MVqxNk8zPC92ODDo NYLPO25lcW6qaXLpeJMhfGinIHX4dJJme3Orb36gc4Yhd3O2ZX;jcIF{fCCmaX\m[ZJmdnSrYYTpc44hdWG{a3Xyd{BidmRiQXv0JJBpd3OyaH;yfYxifGmxbh?= MYGyOFI6OzBzMR?=
Jurkat NXHGUXFzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU\ZPWxzOS1zMDFOwG0> MVW0PEBp MXLJR|UxRTRwOTFOwG0> NEPIO2wzPDJ3M{CyOC=>
CEM-R NVfOUXlRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTTNU0yOCEQvF2= NULwZ3lGPDhiaB?= NIO5d45KSzVyPUSg{txO NVPkWmFxOjR{NUOwNlQ>
CEM-S M{XiSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV[xMVExKM7:TR?= M3HaZVQ5KGh? M{C2NGlEPTB;ND62JO69VQ>? M2LvfVI1OjV|MEK0
MOLT-4 NIj3TI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPvNU0yOCEQvF2= NFjtd281QCCq NID0NoZKSzVyPUWuO{DPxE1? MXuyOFI2OzB{NB?=
PF-382 NX7zcFBwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYSxMVExKM7:TR?= MkWzOFghcA>? MWnJR|UxRTRwNTFOwG0> M4ntOlI1OjV|MEK0
ALL-SIL NX3CNlFZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUCxMVExKM7:TR?= NYX4OVNqPDhiaB?= NGj4SFJKSzVyPUWuO{DPxE1? NVvqdY9yOjR{NUOwNlQ>
HPB-ALL NWj3PHNYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjkOGdZOS1zMDFOwG0> NGXvOIw1QCCq Mk\FTWM2OD14LkGg{txO M4XDRVI1OjV|MEK0
DND-41 Mn\NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jmXVEuOTBizszN MkiyOFghcA>? NH\h[3lKSzVyPUmg{txO MWKyOFI2OzB{NB?=
ALL-SIL M3P5UGFxd3C2b4Ppd{BCe3OjeR?= NYfnVHJ1PSEQvF2= MmfzNlQwPDhiaB?= NFnIOnVqdmS3Y3XzJIFxd3C2b4Ppdy=> NVjyUnRYOjR{NUOwNlQ>
DND-41 M4HM[WFxd3C2b4Ppd{BCe3OjeR?= NUfWVGZyPSEQvF2= M2\wRlI1NzR6IHi= MlPQbY5lfWOnczDhdI9xfG:|aYO= MUmyOFI2OzB{NB?=
MOLT-4 NIDWRpZCeG:ydH;zbZMhSXO|YYm= M3zSW|Uh|ryP MYiyOE81QCCq MkPjbY5lfWOnczDhdI9xfG:|aYO= M3\q[|I1OjV|MEK0
U-266 NH7OcWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXOwMVQxKM7:TR?= NUfuSIlrPDhiaB?= NGryXZBKSzVyPUG5MlghyrWPwrC= M{ftOlI1ODh4NEm0
INA-6 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPqWXFuOC12MDFOwG0> MXW0PEBp NYTFZ2FrUUN3ME2yMlQzKML3TR?= NGrFfVgzPDB6NkS5OC=>
Jeko-1 MlrOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXXdIoxNTRyIN88US=> MnjiOFghcA>? M1jPRmlEPTB;Mj60JOK2VcLi NGqzZoEzPDB6NkS5OC=>
Rec-1 MkLPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjkeWIxNTRyIN88US=> NYLINllDPDhiaB?= MXrJR|UxRTFwNE[gxtVOyqB? MYqyOFA5PjR7NB?=
A549 MWDGeY5kfGmxbjDBd5NigQ>? MX2xNEDPxE1? MorENVIwOjRxNEigbC=> M4LCeYlvcGmkaYTzJHRITi4QskGtbY5lfWOnZDDtbYdz[XSrb36gZY5lKGmwdnHzbY9v Mnj4NlQxOjN7M{i=
A549 NYnnb2NETnWwY4Tpc44hSXO|YYm= M3vPfFMh|ryP MUC0PEBp MnTEbY5pcWKrdIOgWGdHNc7{MT3pcoR2[2WmIHHjeIl3[XSrb36gc4YhW22jZDDhcoQh\XiycnXzd4lwdiCxZjDTcoFqdCCjbnSgWJdqe3R? MXyyOFAzOzl|OB?=
S-LAMA84 NWL5eWJ{TnWwY4Tpc44hSXO|YYm= NVLybI81O8LizszN MY[yOEBp Mm[0SG1UVw>? NGLpb41z\WS3Y3XzJGNMOiCjY4Tpeol1gQ>? NWnPTFVQOjRyMUKxNFk>
R-LAMA84 NWGw[Wl5TnWwY4Tpc44hSXO|YYm= NXf0ZlR{O8LizszN M1;oc|I1KGh? M4riPWROW09? M3jsSpJm\HWlZYOgR2szKGGldHn2bZR6 NILGcZgzPDBzMkGwPS=>
S-LAMA84 NXO1coRpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFj5b4kzNjVvMUCg{txO MmrhOFghcA>? M3zGVWROW09? NHfkNnNqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 MYeyOFAyOjFyOR?=
R-LAMA84 NHPD[G9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXleWgzNjVvMUCg{txO MUO0PEBp NV7ibFhYTE2VTx?= NXrkWJNJcW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? MWKyOFAyOjFyOR?=
A549 M2fjRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVzJNnJbOC1|MDFOwG0> MUi3NkBp MV7EUXNQ M1zZNWlEPTB;ND6xOUDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJINwdmOnboTyZZRqd25iZHXw[Y5l\W62bIm= MWGyN|Y2OTR2Mx?=
H1299 MmnYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXlUo4xNTNyIN88US=> MXe3NkBp NGrvU2JFVVOR NEDhfolKSzVyPUGuPFAh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 MmLrNlM3PTF2NEO=
A549 M1G1d2Z2dmO2aX;uJGF{e2G7 MmLwNU8yOCEQvF2= NV3DeId4PDhiaB?= NH7GSXpFVVOR NF3pWnNt\WGmczD0c{BiKGSxc3Wt[IVx\W6mZX70JIRm[3KnYYPlJIlvKE6xdHPoJJJmeG:{dHXyJIFkfGm4aYT5 NWqw[4xwOjN4NUG0OFM>
LNCap MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LKNVAuOzBizszN NGPp[3U1KGR? MmjwTWM2OD12LkW5xsDPxE1? MoqxNlI5OzJ|MU[=
A431  MUHGeY5kfGmxbjDBd5NigQ>? NIDDO3AyOCEQvF2= MXGzNEBucW5? Ml2yZZR1\W63YYTld{BRUTONLVHreE1uXE:UIIPp[45idGmwZx?= MkjDNlI{QDd7OEi=
H2170  NFHlNWVHfW6ldHnvckBCe3OjeR?= M3jVO|ExKM7:TR?= MWKzNEBucW5? MXfheJRmdnWjdHXzJHBKO0tvQXv0MY1VV1Jic3nncoFtcW6p M2riVlIzOzh5OUi4
A431  MmHLSpVv[3Srb36gRZN{[Xl? M370XFExKM7:TR?= NF;idoI1NTJ2IHi= NX;2bYZq\W6qYX7j[ZMh[XCxcITvd4l{KHerdHig[ZJtd3Srbnni MnPZNlI{QDd7OEi=
H2170  MnXxSpVv[3Srb36gRZN{[Xl? MlrXNVAh|ryP M1L6[VQuOjRiaB?= MXnlcohidmOnczDhdI9xfG:|aYOge4l1cCCncnzveIlvcWJ? MXGyNlM5Pzl6OB?=

... 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
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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
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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
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  • 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
    V1
    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 Recruiting Multiple Myeloma Cylene Pharmaceuticals September 2010 Phase 1
NCT00891280 Recruiting 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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID