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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6 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.

    (B and C) Jurkat cells were pretreated for 2 h with DES (3 μM) and CX-4945 (10 μM) individually or in combination, and were then treated with PMA (50 ng/mL) plus PHA (1 μg/mL) for 6 and 24 h. IL-2 mRNA expression was detected by qRT-PCR analysis (B) and the amounts of secreted IL-2 in the culture medium were measured by ELISA (C). #p < .01 (vs. the PMA/PHA, DES, and CX-4945 untreated cell population); *p < .01; **p < .001 (vs. the cell population treated with only PMA/PHA).

    Biomed Pharmacother, 2018, 98:357-363. 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 MXPLbY5ie2ViQYPzZZk> M3HGXFEwPS9zMDFOwG0> M3rMNVAvPSCq NUfuVnZbTE2VTx?= M4LPZpJm\HWlZYOgR2szKGurbnHz[UBi[3Srdnn0fUBidmRicHzheIVt\XRiYXfndoVo[XSrb36= M3vRbVI3OzhzNEO3
HDMEC MUDLbY5ie2ViQYPzZZk> MXmwMlI2NzBwNT:xJO69VQ>? M4ji[FI1KGh? Mn3PSG1UVw>? MV7y[YR2[2W|IFPLNkBscW6jc3WgZYN1cX[rdImsJJZYTiCneIDy[ZN{cW:wIHHu[EB{\WO{ZYTpc44> NIHaRmszPjN6MUSzOy=>
HDMEC MorDSpVv[3Srb36gRZN{[Xl? NGruT4sxNjJ3L{CuOU8yKM7:TR?= MkW0NlQhcA>? MV3EUXNQ MkK3doVlfWOnczDlfJBz\XO|aX;uJI9nKF[FQV2tNUBjfXRibn;0JGlESU1vMR?= M1HSWVI3OzhzNEO3
HDMEC MnywSpVv[3Srb36gRZN{[Xl? M2PsNVEh|ryP M1nNe|I1KGh? MUDEUXNQ NFuwZXBi\m[nY4TzJJN2[mOnbHz1cIFzKGyxY3HsbZpifGmxbjDv[kBPTkGWY{GgZY5lKHCqb4PwbI8ueDZ3 M3vxflI3OzhzNEO3
A549  MVXGeY5kfGmxbjDBd5NigQ>? NWnrcJhXOy9zMNMg{txO M{n1T|Q5KGh? M2HmVpN2eHC{ZYPz[ZMhfGinIH3pZ5JweGmubHHyMYlv\HWlZXSg[ZhxemW|c3nvckBw\iCyLV\BTy=> MXmyOlMyQDhyMB?=
HDMEC MVfLbY5ie2ViQYPzZZk> NXrQVmxMOS13MDFOwG0> M4TrfFUhcA>? NUHifpM6TE2VTx?= Mnmx[IVkemWjc3XzJGNMOiCtaX7hd4Uh[WO2aY\peJkhf2m2aH;1eEBi\m[nY4Tpcoch[2WubDD2bYFjcWyrdIm= M3LRbFI3OTh7NUi2
HDMEC NGSyU|BHfW6ldHnvckBCe3OjeR?= MYO1NEDPxE1? NGjLSJEyNzViaB?= Mn35SG1UVw>? M2fEWoRm[3KnYYPld{B1cGViboXjcIVieiC|aXfuZYwhd2ZicHjvd5Bpd3K7bHH0[YQheDZ3IHnuJHRPTi4QsT3zeIlufWyjdHXkJGhFVUWFwrC= M4P4ZlI3OTh7NUi2
HEK293 NXXkfHpHU2mwYYPlJGF{e2G7 MUiwMlXDqM7:TR?= M{nYR|E2KG2rbh?= MljCSG1UVw>? MYPy[YR2[2W|IFPLNkBscW6jc3WgZYN1cX[rdIm= M1rkdFI2QDh5NkK2
Hela NFjROHdMcW6jc3WgRZN{[Xl? NEiydGYxNjYEoN88US=> MlP5NVUhdWmw M4DKZ2ROW09? NFvtUldz\WS3Y3XzJGNMOiCtaX7hd4Uh[WO2aY\peJk> MXqyOVg5PzZ{Nh?=
LAMA84 NF;YTXlMcW6jc3WgRZN{[Xl? NYq2SXJCOC53wrFOwG0> MWOxOUBucW5? M4fXdWROW09? MXXy[YR2[2W|IFPLNkBscW6jc3WgZYN1cX[rdIm= NH7jR4EzPTh6N{[yOi=>
HEK293 MULGeY5kfGmxbjDBd5NigQ>? NV7oZW9lOyEQvF2= MYe1JIg> M4XvfmROW09? NY\mVnFqS0t{IIDoc5NxcG:{eXzheIV{KGWLRkPqJIF1KFOnckGyOy=> NHjIb|UzPTh6N{[yOi=>
UM-SCC1 Mlq4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;UfIVJOC5zLUOwJO69VQ>? MkDqNU02KGR? M1LybmlEPTB;ND6xJO69VQ>? MlnSNlU4QThyNkG=
UM-SCC46 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYGwMlEuOzBizszN M4LWbFEuPSCm MkLZTWM2OD1|LkSg{txO MYSyOVc6QDB4MR?=
UM-SCC1 Mkn1SpVv[3Srb36gRZN{[Xl? M3yxSFAvPS92L{GwJO69VQ>? NVq3WpRXPzJiaB?= MnG4[I94di2{ZXf1cIF1\XNidHjlJIV5eHKnc4Ppc44hd2ZiTl[tyNhDNCCEY3ytXGwh[W6mIIXwMZJm\3WuYYTld{B1cGViZYjwdoV{e2mxbjDv[kBxPTNuIICyNUwhSVBvMTDhcoQhUUxvODDjc45k\W62cnH0bY9vKGSncHXu[IVvfGy7 NUX3N3pIOjV5OUiwOlE>
UM-SCC46 NHL3OZVHfW6ldHnvckBCe3OjeR?= Mof5NE42NzRxMUCg{txO MXy3NkBp MVXkc5dvNXKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCQRj5EvGItKEKlbD3YUEwheDV|LDDwNlEtKEGSLUGgZY5lKHWyLYLl[5Vt[XSnczD0bIUh\XiycnXzd4lwdiCLTD24JINwdmOnboTyZZRqd25iZHXw[Y5l\W62bIm= M4KwXVI2Pzl6ME[x
NU-DUL MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzEPWluPS1{NTFOwG0> NWTUbY1wPDhiaB?= NUjPTnN4cW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? MmjSNlU4QDh{Nkm=
Oci Ly 3 NGHWUmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHpVGFyPS1{NTFOwG0> NFvXVpQ1QCCq M3\jbIlvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> MXyyOVc5QDJ4OR?=
Oci Ly 10 NIXTfVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVi1MVI2KM7:TR?= MV60PEBp NYixd2JrcW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? M373cFI2Pzh6Mk[5
Oci Ly 1 MmjxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWe1MVI2KM7:TR?= MXS0PEBp MYjpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 MlXzNlU4QDh{Nkm=
Oci Ly 18 NIjNNYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlf0OU0zPSEQvF2= MlPNOFghcA>? NF\YNoFqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NHywNJEzPTd6OEK2PS=>
Oci Ly 19  MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmn3OU0zPSEQvF2= M3K4S|Q5KGh? NXP1bVZjcW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? NHntW|AzPTd6OEK2PS=>
Raji NF3PTFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHiRno{PS1{NTFOwG0> MonSOFghcA>? NF\JXnZqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 MlPCNlU4QDh{Nkm=
H1299 MnzhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;PNU82NzFyIN88US=> NGnvXHY4OiCq M2n2[olvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> M4fTR|I2PzVyM{C4
Calu-1  MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYexM|UwOTBizszN NXzXT|VCPzJiaB?= NIDxZYRqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 M3vmR|I2PzVyM{C4
H358 MlnYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rkOlEwPS9zMDFOwG0> NVj1Vok2PzJiaB?= Mmf5bY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> NVjUS4ptOjV5NUCzNFg>
H1299 NF7EVIlCeG:ydH;zbZMhSXO|YYm= MnzXNVAh|ryP NGq5dHk4OiCq NYrVb4VLcW6mdXPld{BieG:ydH;zbZM> MWSyOVc2ODNyOB?=
Calu-1  NYrhPWxCSXCxcITvd4l{KEG|c3H5 MVexNEDPxE1? Mn;iO|IhcA>? NHr1S|RqdmS3Y3XzJIFxd3C2b4Ppdy=> MVeyOVc2ODNyOB?=
H358 MnfuRZBweHSxc3nzJGF{e2G7 NFT3TpkyOCEQvF2= MWm3NkBp MmXKbY5lfWOnczDhdI9xfG:|aYO= MU[yOVc2ODNyOB?=
PC9/GR MXPGeY5kfGmxbjDBd5NigQ>? MmLwOUDDvU1? M1P0d|Q5KGh? Mo\XbY5lfWOnczDheZRweGijZ4m= MnT2NlU1QDZ2MEm=
PC9/ER M3GyTmZ2dmO2aX;uJGF{e2G7 NVfmcFBSPSEEtV2= MnnmOFghcA>? MlrabY5lfWOnczDheZRweGijZ4m= M4O5bFI2PDh4NEC5
H28 M4fWR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlLKNE4xOS1|MDFOwG0> M4TFOFczKGh? NFL3Tm1FVVOR M374ZWlEPTB;Nz6yJO69VQ>? MmS1NlU1OjJyOEG=
H2052 Ml;4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoqzNE4xOS1|MDFOwG0> MlzRO|IhcA>? NYKw[JJTTE2VTx?= M1q3VGlEPTB;Mj6wJO69VQ>? MUOyOVQzOjB6MR?=
UM-SCC-1 Mk[wR4xwdm:pZX7pZ{BCe3OjeR?= NYTMO2M5OC53LUWg{txO NXjuNFJKOTRiZB?= MkPHSG1UVw>? MYhCpIlvcGmkaYTzJINtd26xZ3XubYMhe3W{dnn2ZYwh[W6mIIPwbIVz\SCob4LtZZRqd25? MUSyOVM4QTBzNh?=
UM-SCC-46 MkG1R4xwdm:pZX7pZ{BCe3OjeR?= MmHrNE42NTVizszN M3LH[FE1KGR? MlfZSG1UVw>? NH3DcIzDqGmwaHnibZR{KGOub37v[4VvcWNic4Xyeol3[WxiYX7kJJNxcGW{ZTDmc5Ju[XSrb36= NHTKXmozPTN5OUCxOi=>
U87-MG MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4jKOlEwPS9zMDFOwG0> NWTOblY2OjRxNEivO|IhcA>? MoHUSG1UVw>? MkHYbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[m:2aDDjc45k\W62cnH0bY9vKGGwZDD0bY1mKGSncHXu[IVvfGy7 NWC1Om9mOjV{NEG4PVc>
MDA-MB-231 M1y1dWZ2dmO2aX;uJGF{e2G7 NFjjXHYzNzVxMUCg{txO M3;4ZVQhcA>? NHzrdo9l\WO{ZXHz[ZMhfGinIHPvcpN1cXS3dHn2[UBxcG:|cHjvdplt[XSrb36gc4Yh[m:2aDCgdE1UPTJ7LYC2OUBidmRicD3TNVI6NUGtdB?= NUTPdFZXOjVzNUO3NlU>
MDA-MB-231 NVLDdGc{TnWwY4Tpc44hSXO|YYm= MlXXNk82NzFyIN88US=> MlTIOEBp M{jBeolvcGmkaYTzJJNmemmwZTC1NlkheGixc4Doc5J6dGG2aX;uJIFv\CC2aHWg[ZhxemW|c3nvckBw\iCLTD22MEBKVC16 M{LXRVI2OTV|N{K1
ARPE-19 MYHLbY5ie2ViQYPzZZk> NYr5SnJ7PS9zMD:yNEDPxE1? MWqyOE81QCCq NYO2bo0{cW6qaXLpeJMhS0t{IHvpcoF{\SCjY4Tpeol1gSCjdDDhJINwdmOnboTyZZRqd25ib3[gOeKh|ryP MmTxNlQ3QDZyOEC=
ARPE-19 NIHU[21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXGxNEDPxE1? M1iwS|I1NTl4IHi= M4rkbWROW09? Ml3ZbY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> M1joN|I1Pjh4MEiw
HCT116  NGfzfGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYD3U255OTBizszN MXiyOE06PiCq NHTDfYRFVVOR MWHpcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 MkG2NlQ3QDZyOEC=
ARPE-19 M2XycmZ2dmO2aX;uJGF{e2G7 MXWxNEDPxE1? MnfEOEBp NHLjOIFFVVOR MlnuZ4F2e2W|IFXSMZN1emW|czDy[ZNxd26|ZTDveoVzKHSqZTDwMYVKTjMQsTDidoFv[2huIHL1eEBld2W|IH7veEBqdmS3Y3WgR2hQWMLi NUL3UmZ4OjR4OE[wPFA>
HCT116  Mm\1SpVv[3Srb36gRZN{[Xl? M1;IblExKM7:TR?= MVW0JIg> NVPUPXZyTE2VTx?= NFvENWdk[XW|ZYOgSXIue3S{ZYPzJJJme3CxboPlJI93\XJidHjlJJAu\UmIMt8xJIJz[W6laDygZpV1KGSxZYOgco91KGmwZIXj[UBEUE:SwrC= NXXocJk1OjR4OE[wPFA>
HCT116  MV3BdI9xfG:|aYOgRZN{[Xl? NVfQXYxLOTBizszN M{HIOFI1NzR6IHi= MXjEUXNQ NIHnSJFqdmS3Y3XzJIFxd3C2b4Ppdy=> Mmf3NlQ3QDZyOEC=
Nalm6  NHjaNVdHfW6ldHnvckBCe3OjeR?= NIizOXUyOC9{MDFOwG0> MYWyOEBp MWny[ZN2dHS|IHnuJIRm[3KnYYPl[EBRXEWQIIDoc5NxcG:{eXzheIlwdiCjdDD0bIUhS0t{IIThdodmfCC{ZYPp[JVmKFN|OECgZY5lKGOxbnPvcYl1[W62IHTve45z\We3bHH0bY9vKG:oIGDUSW4heHKxdHXpckBmgHC{ZYPzbY9v M1HkcVI1PTZzN{my
SUP-B15 MnXwSpVv[3Srb36gRZN{[Xl? NWPYR2pqOTBxMkCg{txO MnrLNlQhcA>? NYHObodYemW|dXz0d{BqdiCmZXPy[YF{\WRiUGTFUkBxcG:|cHjvdplt[XSrb36gZZQhfGinIFPLNkB1[XKpZYSgdoV{cWS3ZTDTN|gxKGGwZDDjc45kd22rdHHueEBld3ewcnXneYxifGmxbjDv[kBRXEWQIIDyc5RmcW5iZYjwdoV{e2mxbh?= NHHuPFgzPDV4MUe5Ni=>
Nalm6  MmrnRZBweHSxc3nzJGF{e2G7 NH\nXGE3NzFyIN88US=> NVfhOYJpPDhiaB?= MmPobY5lfWOnczDhdI9xfG:|aYO= M3XXR|I1PTZzN{my
SUP-B15 NWjFTnFWSXCxcITvd4l{KEG|c3H5 M4\OdFYwOTBizszN MWG0PEBp Mmj0bY5lfWOnczDhdI9xfG:|aYO= NVnvfXBIOjR3NkG3PVI>
C2C12 MXrGeY5kfGmxbjDBd5NigQ>? M4\ObFMh|ryP NFHGW|MyOi9{ND:0PEBp MYnpcohq[mm2czD0bIUh\XiycnXzd4lwdiCxZjDvd5Rmd2OuYYP0JIRq\m[ncnXueIlifGmxbjDtZZJs\XK|IHHu[EBCc3RicHjvd5Bpd3K7bHH0bY9v MnniNlQzQTNyMUG=
Jurkat M1XLUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLUOIxvOS1zMDFOwG0> NFq2ZXM1QCCq MVLJR|UxRTRwOTFOwG0> NU\y[2x6OjR{NUOwNlQ>
CEM-R MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjmRXkyNTFyIN88US=> MXy0PEBp NXGzUVhGUUN3ME20JO69VQ>? NV3Yc2lsOjR{NUOwNlQ>
CEM-S MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVWxMVExKM7:TR?= MV20PEBp NGruNpBKSzVyPUSuOkDPxE1? MXmyOFI2OzB{NB?=
MOLT-4 NV21eZFnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnnclNZOS1zMDFOwG0> NGfybpU1QCCq MYfJR|UxRTVwNzFOwG0> MlX2NlQzPTNyMkS=
PF-382 MmXZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjUNU0yOCEQvF2= MV20PEBp M1PtUmlEPTB;ND61JO69VQ>? NHXhPWwzPDJ3M{CyOC=>
ALL-SIL M4XCTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;aS20yNTFyIN88US=> M4TxeFQ5KGh? MUjJR|UxRTVwNzFOwG0> MnnYNlQzPTNyMkS=
HPB-ALL M3TMU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlS2NU0yOCEQvF2= M4n1[lQ5KGh? MoTqTWM2OD14LkGg{txO M2PlVFI1OjV|MEK0
DND-41 M3L0Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rGbVEuOTBizszN NF\qTII1QCCq MlrGTWM2OD17IN88US=> M4i0cVI1OjV|MEK0
ALL-SIL MlnwRZBweHSxc3nzJGF{e2G7 M3jsN|Uh|ryP NXP4dIZ3OjRxNEigbC=> MYTpcoR2[2W|IHHwc5B1d3Orcx?= NVT6S3ZQOjR{NUOwNlQ>
DND-41 Mo\CRZBweHSxc3nzJGF{e2G7 NHXMS5c2KM7:TR?= MUCyOE81QCCq MkKybY5lfWOnczDhdI9xfG:|aYO= MXqyOFI2OzB{NB?=
MOLT-4 MmLoRZBweHSxc3nzJGF{e2G7 NV24U4d6PSEQvF2= NHnPZnIzPC92ODDo NECx[VRqdmS3Y3XzJIFxd3C2b4Ppdy=> NEnrZ3QzPDJ3M{CyOC=>
U-266 MnnwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnT3NE01OCEQvF2= MXq0PEBp NEjhNWxKSzVyPUG5MlghyrWPwrC= NGfTWGYzPDB6NkS5OC=>
INA-6 M{nPOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEPMPVAxNTRyIN88US=> NGD1dnc1QCCq MonkTWM2OD1{LkSyJOK2VQ>? MVGyOFA5PjR7NB?=
Jeko-1 NUi3[Vk1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXUdFdEOC12MDFOwG0> NHr0XnM1QCCq MW\JR|UxRTJwNDFCuW3DqA>? NIj5RWkzPDB6NkS5OC=>
Rec-1 NYjES2Q{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYmwMVQxKM7:TR?= M1;ke|Q5KGh? NI\jS2dKSzVyPUGuOFYhyrWPwrC= M13pc|I1ODh4NEm0
A549 NIT0RmxHfW6ldHnvckBCe3OjeR?= M4rvXFExKM7:TR?= M4rwTlEzNzJ2L{S4JIg> MYPpcohq[mm2czDUS2Yu|rJzLXnu[JVk\WRibXnndoF1cW:wIHHu[EBqdn[jc3nvci=> MkTxNlQxOjN7M{i=
A549 NEP6d4NHfW6ldHnvckBCe3OjeR?= MX2zJO69VQ>? Ml\LOFghcA>? MnjxbY5pcWKrdIOgWGdHNc7{MT3pcoR2[2WmIHHjeIl3[XSrb36gc4YhW22jZDDhcoQh\XiycnXzd4lwdiCxZjDTcoFqdCCjbnSgWJdqe3R? MmTFNlQxOjN7M{i=
S-LAMA84 NYPiTZJzTnWwY4Tpc44hSXO|YYm= NWTMTWk3O8LizszN M{DLdVI1KGh? NIHrfY1FVVOR MU\y[YR2[2W|IFPLNkBi[3Srdnn0fS=> MYSyOFAyOjFyOR?=
R-LAMA84 Ml7VSpVv[3Srb36gRZN{[Xl? M3XYd|PDqM7:TR?= NWjMbo41OjRiaB?= NXK2bYJUTE2VTx?= M{PpU5Jm\HWlZYOgR2szKGGldHn2bZR6 M3TrdVI1ODF{MUC5
S-LAMA84 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13GPVIvPS1zMDFOwG0> MVO0PEBp M4DQdGROW09? MXLpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 M4\mSFI1ODF{MUC5
R-LAMA84 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XSOFIvPS1zMDFOwG0> M{LwOVQ5KGh? M4LYPWROW09? NXzNeWpqcW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? MV[yOFAyOjFyOR?=
A549 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFf5dZAxNTNyIN88US=> NXn0UoZYPzJiaB?= NIHoTItFVVOR M2S4cWlEPTB;ND6xOUDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJINwdmOnboTyZZRqd25iZHXw[Y5l\W62bIm= NV;BNnVUOjN4NUG0OFM>
H1299 NXey[IRUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPRVGQxNTNyIN88US=> NYnJPXFPPzJiaB?= M2Dq[2ROW09? M2jYZWlEPTB;MT64NEDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJINwdmOnboTyZZRqd25iZHXw[Y5l\W62bIm= MmPoNlM3PTF2NEO=
A549 MXnGeY5kfGmxbjDBd5NigQ>? MVexM|ExKM7:TR?= MlHqOFghcA>? NX[4NlRLTE2VTx?= MV7s[YFleyC2bzDhJIRwe2VvZHXw[Y5l\W62IHTlZ5Jm[XOnIHnuJG5wfGOqIILldI9zfGW{IHHjeIl3cXS7 M3fGcVI{PjVzNESz
LNCap MlzKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M373SVAuOzBizszN M1jLT|Qh\A>? NETEXodKSzVyPUSuOVnDqM7:TR?= MV6yNlg{OjNzNh?=
A431  MXjGeY5kfGmxbjDBd5NigQ>? MoLlNVAh|ryP MYWzNEBucW5? MlLnZZR1\W63YYTld{BRUTONLVHreE1uXE:UIIPp[45idGmwZx?= NWXmc2VYOjJ|OEe5PFg>
H2170  MWrGeY5kfGmxbjDBd5NigQ>? Ml3zNVAh|ryP NGTXdG4{OCCvaX6= MmjtZZR1\W63YYTld{BRUTONLVHreE1uXE:UIIPp[45idGmwZx?= NXTwbGl[OjJ|OEe5PFg>
A431  MkXtSpVv[3Srb36gRZN{[Xl? Mo\mNVAh|ryP MmrIOE0zPCCq MXvlcohidmOnczDhdI9xfG:|aYOge4l1cCCncnzveIlvcWJ? MkPGNlI{QDd7OEi=
H2170  NX;qOIZ2TnWwY4Tpc44hSXO|YYm= MYOxNEDPxE1? M3fjN|QuOjRiaB?= NGXXPIpmdmijbnPld{BieG:ydH;zbZMhf2m2aDDldoxwfGmwaXK= NEjYZ4szOjN6N{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 Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1% CMC Na
For best results, use promptly after mixing.
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
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)

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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 )

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* 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

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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|Castleman''s 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