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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USD 320 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 MlvFT4lv[XOnIFHzd4F6 M2LmdVEwPS9zMDFOwG0> NFO2dHUxNjViaB?= NHPlbWpFVVOR NXP3OFNmemWmdXPld{BEUzJia3nuZZNmKGGldHn2bZR6KGGwZDDwcIF1\WyndDDh[4dz\WejdHnvci=> M4DpTVI3OzhzNEO3
HDMEC MWLLbY5ie2ViQYPzZZk> MnfiNE4zPS9yLkWvNUDPxE1? NIi4cWkzPCCq M{HYbGROW09? MULy[YR2[2W|IFPLNkBscW6jc3WgZYN1cX[rdImsJJZYTiCneIDy[ZN{cW:wIHHu[EB{\WO{ZYTpc44> NFjpRXczPjN6MUSzOy=>
HDMEC MUnGeY5kfGmxbjDBd5NigQ>? MkLJNE4zPS9yLkWvNUDPxE1? MXuyOEBp NEewNmNFVVOR NWroV3ZyemWmdXPld{BmgHC{ZYPzbY9vKG:oIG\DRW0uOSCkdYSgco91KEmFQV2tNS=> MUmyOlM5OTR|Nx?=
HDMEC MmTrSpVv[3Srb36gRZN{[Xl? MWCxJO69VQ>? NXLkVHI1OjRiaB?= M{TpO2ROW09? M4i3TIFn\mWldIOgd5Vj[2WubIXsZZIhdG:lYXzpfoF1cW:wIH;mJG5HSVSlMTDhcoQheGixc4Doc{1xPjV? MYeyOlM5OTR|Nx?=
A549  NY\DOFBGTnWwY4Tpc44hSXO|YYm= M{DKdVMwOTEEoN88US=> MUC0PEBp Monmd5VxeHKnc4Pld{B1cGVibXnjdo9xcWyuYYKtbY5lfWOnZDDlfJBz\XO|aX;uJI9nKHBvRlHL MUmyOlMyQDhyMB?=
HDMEC NXLGb3QyU2mwYYPlJGF{e2G7 MkjONU02OCEQvF2= M2nPVFUhcA>? NVrobIpWTE2VTx?= NV;6cFFU\GWlcnXhd4V{KEONMjDrbY5ie2ViYXP0bZZqfHlid3n0bI92fCCjZn\lZ5RqdmdiY3XscEB3cWGkaXzpeJk> MX[yOlE5QTV6Nh?=
HDMEC MX7GeY5kfGmxbjDBd5NigQ>? MkfQOVAh|ryP MlLBNU82KGh? M1HlOGROW09? M4nPW4Rm[3KnYYPld{B1cGViboXjcIVieiC|aXfuZYwhd2ZicHjvd5Bpd3K7bHH0[YQheDZ3IHnuJHRPTi4QsT3zeIlufWyjdHXkJGhFVUWFwrC= NYLyNWZsOjZzOEm1PFY>
HEK293 NYHzcWZMU2mwYYPlJGF{e2G7 MlPxNE42yqEQvF2= NIrBPY4yPSCvaX6= M{\Nc2ROW09? MlvNdoVlfWOnczDDT|Ihc2mwYYPlJIFkfGm4aYT5 M{TCblI2QDh5NkK2
Hela NHXLT25McW6jc3WgRZN{[Xl? MWiwMlXDqM7:TR?= MnvRNVUhdWmw NUO2W3cyTE2VTx?= Moe3doVlfWOnczDDT|Ihc2mwYYPlJIFkfGm4aYT5 Mkj3NlU5QDd4Mk[=
LAMA84 MW\LbY5ie2ViQYPzZZk> M1:5[lAvPcLizszN MmeyNVUhdWmw MVzEUXNQ NEXHfHVz\WS3Y3XzJGNMOiCtaX7hd4Uh[WO2aY\peJk> M33hfFI2QDh5NkK2
HEK293 NGrJZmNHfW6ldHnvckBCe3OjeR?= Ml\TN{DPxE1? M2rLV|UhcA>? NXe3V3ppTE2VTx?= MXXDT|IheGixc4Doc5J6dGG2ZYOg[WlHO2piYYSgV4VzOTJ5 NYnnRnhXOjV6OEe2NlY>
UM-SCC1 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXz6fJlROC5zLUOwJO69VQ>? NV3MWY9oOS13IHS= NULPeph{UUN3ME20MlEh|ryP NWPBO|NKOjV5OUiwOlE>
UM-SCC46 NFvBeZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPMcGlTOC5zLUOwJO69VQ>? NYG3TYdtOS13IHS= M{Kxb2lEPTB;Mz60JO69VQ>? NGe3XWEzPTd7OEC2NS=>
UM-SCC1 NHj1dYRHfW6ldHnvckBCe3OjeR?= M1LqfVAvPS92L{GwJO69VQ>? M4LWPVczKGh? Mknl[I94di2{ZXf1cIF1\XNidHjlJIV5eHKnc4Ppc44hd2ZiTl[tyNhDNCCEY3ytXGwh[W6mIIXwMZJm\3WuYYTld{B1cGViZYjwdoV{e2mxbjDv[kBxPTNuIICyNUwhSVBvMTDhcoQhUUxvODDjc45k\W62cnH0bY9vKGSncHXu[IVvfGy7 M1zSUlI2Pzl6ME[x
UM-SCC46 MWrGeY5kfGmxbjDBd5NigQ>? MoHsNE42NzRxMUCg{txO M17O[lczKGh? NGTCSZZld3ewLYLl[5Vt[XSnczD0bIUh\XiycnXzd4lwdiCxZjDOSk3FwEJuIFLjcE1ZVCxicEWzMEBxOjFuIFHQMVEh[W6mIIXwMZJm\3WuYYTld{B1cGViZYjwdoV{e2mxbjDJUE05KGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> M1HQ[lI2Pzl6ME[x
NU-DUL MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWO1MVI2KM7:TR?= NYPoXGo5PDhiaB?= M2rmb4lvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> Mmn3NlU4QDh{Nkm=
Oci Ly 3 M1G2VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HBNFUuOjVizszN M3y1VVQ5KGh? NIC4PZhqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 MWWyOVc5QDJ4OR?=
Oci Ly 10 MmTXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Moe0OU0zPSEQvF2= NIfF[oM1QCCq NGTISHVqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NVO0OXd[OjV5OEiyOlk>
Oci Ly 1 NETYPW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFriV4U2NTJ3IN88US=> MknvOFghcA>? Mn3wbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> MnrWNlU4QDh{Nkm=
Oci Ly 18 NX;wPWI5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vzdVUuOjVizszN MmTrOFghcA>? NIXLbWNqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NHWwb5MzPTd6OEK2PS=>
Oci Ly 19  NXqxS|hrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPoOU0zPSEQvF2= NH60cmQ1QCCq M4fDTolvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> MknaNlU4QDh{Nkm=
Raji NVPycnlRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHiS2Y2NTJ3IN88US=> MVO0PEBp MoC5bY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> NYnx[Y45OjV5OEiyOlk>
H1299 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\wbFEwPS9zMDFOwG0> M2KxUFczKGh? MYnpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 NGH6[Y4zPTd3MEOwPC=>
Calu-1  MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXsNU82NzFyIN88US=> NVfhZZM4PzJiaB?= MUfpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 M4fDbVI2PzVyM{C4
H358 MlTUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzpOJIyNzVxMUCg{txO NYqyS|Z4PzJiaB?= MYDpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 NIX4d4ozPTd3MEOwPC=>
H1299 MVXBdI9xfG:|aYOgRZN{[Xl? M2D4UlExKM7:TR?= MlvyO|IhcA>? MVvpcoR2[2W|IHHwc5B1d3Orcx?= MnTwNlU4PTB|MEi=
Calu-1  M2rRTWFxd3C2b4Ppd{BCe3OjeR?= MoLNNVAh|ryP M{jQPVczKGh? NVTJNmV5cW6mdXPld{BieG:ydH;zbZM> MUWyOVc2ODNyOB?=
H358 MV;BdI9xfG:|aYOgRZN{[Xl? NYHtTIk4OTBizszN M4PkNlczKGh? M3HpZ4lv\HWlZYOgZZBweHSxc3nz MWKyOVc2ODNyOB?=
PC9/GR M4\F[2Z2dmO2aX;uJGF{e2G7 MkXtOUDDvU1? MUO0PEBp NEe2[GxqdmS3Y3XzJIF2fG:yaHHnfS=> MX[yOVQ5PjRyOR?=
PC9/ER MWnGeY5kfGmxbjDBd5NigQ>? M3;2WFUhyrWP NFrSeVY1QCCq MkCzbY5lfWOnczDheZRweGijZ4m= NUXTZVlZOjV2OE[0NFk>
H28 M2L6Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmj5NE4xOS1|MDFOwG0> MmPVO|IhcA>? MXrEUXNQ NXq4ZodzUUN3ME23MlIh|ryP MoPMNlU1OjJyOEG=
H2052 NF61ZppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYGwMlAyNTNyIN88US=> NGnKPHg4OiCq NILqcINFVVOR M4jN[WlEPTB;Mj6wJO69VQ>? MontNlU1OjJyOEG=
UM-SCC-1 M{fFPWNtd26xZ3XubYMhSXO|YYm= NH7IOJQxNjVvNTFOwG0> MoW4NVQh\A>? MXjEUXNQ NVLhN4NVyqCrbnjpZol1eyClbH;uc4dmdmmlIIP1dpZqfmGuIHHu[EB{eGincnWg[o9zdWG2aX;u M2\t[|I2Ozd7MEG2
UM-SCC-46 NEPCd3JEdG:wb3flcolkKEG|c3H5 NFnQe2kxNjVvNTFOwG0> NXTzW|RCOTRiZB?= NGDDVpdFVVOR NUjWOG9KyqCrbnjpZol1eyClbH;uc4dmdmmlIIP1dpZqfmGuIHHu[EB{eGincnWg[o9zdWG2aX;u M1Wyc|I2Ozd7MEG2
U87-MG NWfINHhNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rtfFEwPS9zMDFOwG0> M12wTlI1NzR6L{eyJIg> MWXEUXNQ NGPBcYVqdmirYnn0d{Bk\WyuIHfyc5d1cCCkb4ToJINwdmOnboTyZZRqd25iYX7kJJRqdWViZHXw[Y5l\W62bIm= MlzhNlUzPDF6OUe=
MDA-MB-231 MoS4SpVv[3Srb36gRZN{[Xl? M4nSUVIwPS9zMDFOwG0> M1PCOVQhcA>? NYDtOZA6\GWlcnXhd4V{KHSqZTDjc45{fGm2dYTpeoUheGixc4Doc5J6dGG2aX;uJI9nKGKxdHigJJAuWzV{OT3wOlUh[W6mIICtV|EzQS2Da4S= NWHGXo5HOjVzNUO3NlU>
MDA-MB-231 NEXZO2JHfW6ldHnvckBCe3OjeR?= MnH3Nk82NzFyIN88US=> MmrYOEBp MXXpcohq[mm2czDz[ZJqdmViNUK5JJBpd3OyaH;yfYxifGmxbjDhcoQhfGinIHX4dJJme3Orb36gc4YhUUxvNjygTWwuQA>? NGnVbmszPTF3M{eyOS=>
ARPE-19 NWG2clhlU2mwYYPlJGF{e2G7 MYG1M|ExNzJyIN88US=> MYGyOE81QCCq MlLPbY5pcWKrdIOgR2szKGurbnHz[UBi[3Srdnn0fUBifCCjIHPvcoNmdnS{YYTpc44hd2ZiNdMg{txO MlPaNlQ3QDZyOEC=
ARPE-19 M17Ncmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGW1NZUyOCEQvF2= MoPNNlQuQTZiaB?= MUnEUXNQ NFX0S2hqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 MWeyOFY5PjB6MB?=
HCT116  MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXn4OYl2OTBizszN MXqyOE06PiCq M1jxd2ROW09? NVnkcJVvcW6qaXLpeJMh[2WubDDndo94fGhidHnt[UBl\XCnbnTlcpRtgQ>? MkfmNlQ3QDZyOEC=
ARPE-19 NWfYcmlLTnWwY4Tpc44hSXO|YYm= NHLKWIEyOCEQvF2= NFywflc1KGh? MYfEUXNQ M1XQRoNifXOnczDFVk1{fHKnc4OgdoV{eG:wc3Wgc5ZmeiC2aHWgdE1mUUZ{zsGgZpJidmOqLDDieZQh\G:nczDuc5QhcW6mdXPlJGNJV1EEoB?= M2HHflI1Pjh4MEiw
HCT116  MmH0SpVv[3Srb36gRZN{[Xl? NXns[YJMOTBizszN MUW0JIg> NVPCXmFmTE2VTx?= MXrjZZV{\XNiRWKtd5Rz\XO|IILld5BwdnOnIH;2[ZIhfGinIICt[WlHOs7zIHLyZY5kcCxiYoX0JIRw\XNibn;0JIlv\HWlZTDDTG9RyqB? MUGyOFY5PjB6MB?=
HCT116  NUTZNIU1SXCxcITvd4l{KEG|c3H5 MWWxNEDPxE1? M3vBblI1NzR6IHi= NYXjVVhRTE2VTx?= NFjEcVFqdmS3Y3XzJIFxd3C2b4Ppdy=> MUGyOFY5PjB6MB?=
Nalm6  MmjuSpVv[3Srb36gRZN{[Xl? MYSxNE8zOCEQvF2= M3jGW|I1KGh? MkKzdoV{fWy2czDpckBl\WO{ZXHz[YQhWFSHTjDwbI9{eGixconsZZRqd25iYYSgeIhmKEONMjD0ZZJo\XRicnXzbYR2\SCVM{iwJIFv\CClb37jc41qfGGwdDDkc5dvemWpdXzheIlwdiCxZjDQWGVPKHC{b4TlbY4h\XiycnXzd4lwdg>? NGDQPXUzPDV4MUe5Ni=>
SUP-B15 NU\5fFB5TnWwY4Tpc44hSXO|YYm= Mm\LNVAwOjBizszN NGLoU3gzPCCq MoXadoV{fWy2czDpckBl\WO{ZXHz[YQhWFSHTjDwbI9{eGixconsZZRqd25iYYSgeIhmKEONMjD0ZZJo\XRicnXzbYR2\SCVM{iwJIFv\CClb37jc41qfGGwdDDkc5dvemWpdXzheIlwdiCxZjDQWGVPKHC{b4TlbY4h\XiycnXzd4lwdg>? NXfZO5NEOjR3NkG3PVI>
Nalm6  NF3T[lNCeG:ydH;zbZMhSXO|YYm= NHyxbng3NzFyIN88US=> MUK0PEBp MXPpcoR2[2W|IHHwc5B1d3Orcx?= MnHqNlQ2PjF5OUK=
SUP-B15 M4TBU2Fxd3C2b4Ppd{BCe3OjeR?= NWH2SmlXPi9zMDFOwG0> MXe0PEBp NVjaPYxKcW6mdXPld{BieG:ydH;zbZM> M{DaOlI1PTZzN{my
C2C12 NHLjTFBHfW6ldHnvckBCe3OjeR?= M2fWeFMh|ryP NF\CfY8yOi9{ND:0PEBp MWLpcohq[mm2czD0bIUh\XiycnXzd4lwdiCxZjDvd5Rmd2OuYYP0JIRq\m[ncnXueIlifGmxbjDtZZJs\XK|IHHu[EBCc3RicHjvd5Bpd3K7bHH0bY9v MmXhNlQzQTNyMUG=
Jurkat MmfqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XodFEuOTBizszN NVLlXpd{PDhiaB?= Ml;4TWM2OD12Lkmg{txO M2\VV|I1OjV|MEK0
CEM-R NGDVTolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVzxNZlzOS1zMDFOwG0> MXy0PEBp MVjJR|UxRTRizszN MWeyOFI2OzB{NB?=
CEM-S NW\Leo41T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTpTFJ5OS1zMDFOwG0> NULxNXd6PDhiaB?= NV7vTWg2UUN3ME20MlYh|ryP Mkm5NlQzPTNyMkS=
MOLT-4 M3\D[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV2xMVExKM7:TR?= NIjpOmY1QCCq MU\JR|UxRTVwNzFOwG0> NULR[JoxOjR{NUOwNlQ>
PF-382 MknDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzMPXcyNTFyIN88US=> MYC0PEBp M3naXmlEPTB;ND61JO69VQ>? NXnNSVl1OjR{NUOwNlQ>
ALL-SIL NFHpXJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfiNU0yOCEQvF2= Mnj0OFghcA>? NU[4[ZdsUUN3ME21Mlch|ryP MlX0NlQzPTNyMkS=
HPB-ALL MmH2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFH1ZmkyNTFyIN88US=> M1jrT|Q5KGh? NEjVenJKSzVyPU[uNUDPxE1? MVGyOFI2OzB{NB?=
DND-41 Ml2wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnqdJEyNTFyIN88US=> M{WycVQ5KGh? NFjkTVRKSzVyPUmg{txO NYPvcVdFOjR{NUOwNlQ>
ALL-SIL MXfBdI9xfG:|aYOgRZN{[Xl? NFu5NXo2KM7:TR?= NWnOWZdJOjRxNEigbC=> MYrpcoR2[2W|IHHwc5B1d3Orcx?= NHHObZgzPDJ3M{CyOC=>
DND-41 NXvueplWSXCxcITvd4l{KEG|c3H5 NGr5d|Y2KM7:TR?= M2XybFI1NzR6IHi= NHjybpNqdmS3Y3XzJIFxd3C2b4Ppdy=> NXHyc4FqOjR{NUOwNlQ>
MOLT-4 Mm\rRZBweHSxc3nzJGF{e2G7 NF3sRVk2KM7:TR?= NXe3SJFEOjRxNEigbC=> NVfFO2ZVcW6mdXPld{BieG:ydH;zbZM> NULIR3o1OjR{NUOwNlQ>
U-266 NFfwVIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XOTFAuPDBizszN MUi0PEBp MX;JR|UxRTF7LkigxtVOyqB? MVqyOFA5PjR7NB?=
INA-6 M1nPSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH31WIMxNTRyIN88US=> MW[0PEBp NVPZWoQ{UUN3ME2yMlQzKML3TR?= NUHufFlSOjRyOE[0PVQ>
Jeko-1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXsWo55OC12MDFOwG0> MnP6OFghcA>? MlHqTWM2OD1{LkSgxtVOyqB? M1\JT|I1ODh4NEm0
Rec-1 NIruZm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTTR3I4OC12MDFOwG0> MmDHOFghcA>? NX;vOWRLUUN3ME2xMlQ3KML3TdMg NYnMS5M1OjRyOE[0PVQ>
A549 M{WyW2Z2dmO2aX;uJGF{e2G7 M2r1RVExKM7:TR?= MkmwNVIwOjRxNEigbC=> Mo\NbY5pcWKrdIOgWGdHNc7{MT3pcoR2[2WmIH3p[5JifGmxbjDhcoQhcW64YYPpc44> MljWNlQxOjN7M{i=
A549 MXvGeY5kfGmxbjDBd5NigQ>? M1HLNlMh|ryP NF\oO201QCCq MlvMbY5pcWKrdIOgWGdHNc7{MT3pcoR2[2WmIHHjeIl3[XSrb36gc4YhW22jZDDhcoQh\XiycnXzd4lwdiCxZjDTcoFqdCCjbnSgWJdqe3R? NIrnc|EzPDB{M{mzPC=>
S-LAMA84 M2jnb2Z2dmO2aX;uJGF{e2G7 NVO5NXdEO8LizszN M3XueVI1KGh? MXzEUXNQ M1LwXpJm\HWlZYOgR2szKGGldHn2bZR6 NXOxTWNjOjRyMUKxNFk>
R-LAMA84 NH7UV|VHfW6ldHnvckBCe3OjeR?= NUj2bllSO8LizszN NVvmbllJOjRiaB?= MkC0SG1UVw>? MWHy[YR2[2W|IFPLNkBi[3Srdnn0fS=> Mlm0NlQxOTJzMEm=
S-LAMA84 M{HKNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVe2W2gxOi53LUGwJO69VQ>? MmTFOFghcA>? M3HlRmROW09? MVjpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 MXuyOFAyOjFyOR?=
R-LAMA84 NVLQZpVtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7XZ4IzNjVvMUCg{txO MX60PEBp MXnEUXNQ M1[zdYlvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> Mn3zNlQxOTJzMEm=
A549 NXP1d2hkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVewMVMxKM7:TR?= M37xe|czKGh? M{\xNGROW09? MnnBTWM2OD12LkG1JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHigZ49v[2WwdILheIlwdiCmZYDlcoRmdnSueR?= MmPhNlM3PTF2NEO=
H1299 Mn;0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\ENE0{OCEQvF2= MkHjO|IhcA>? NELvdlhFVVOR NGPCN4NKSzVyPUGuPFAh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 MXyyN|Y2OTR2Mx?=
A549 NVPxT|hyTnWwY4Tpc44hSXO|YYm= MUSxM|ExKM7:TR?= NHjYXHk1QCCq NXzPOGczTE2VTx?= M{Hl[Yxm[WS|IITvJIEh\G:|ZT3k[ZBmdmSnboSg[IVkemWjc3WgbY4hVm:2Y3igdoVxd3K2ZYKgZYN1cX[rdIm= NI\tZmIzOzZ3MUS0Ny=>
LNCap NWiy[pkzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{SxVFAuOzBizszN M{\qXVQh\A>? MXvJR|UxRTRwNUpCpO69VQ>? MVWyNlg{OjNzNh?=
A431  NE\kOmtHfW6ldHnvckBCe3OjeR?= NXrIbG9COTBizszN M{LNN|MxKG2rbh?= NHHabmpifHSnboXheIV{KFCLM1utRYt1NW2WT2Kgd4lodmGuaX7n NXnZclBTOjJ|OEe5PFg>
H2170  MX7GeY5kfGmxbjDBd5NigQ>? NWnlfFVkOTBizszN Mly2N|AhdWmw MWPheJRmdnWjdHXzJHBKO0tvQXv0MY1VV1Jic3nncoFtcW6p MYKyNlM5Pzl6OB?=
A431  NW[wNZgzTnWwY4Tpc44hSXO|YYm= MYSxNEDPxE1? MVG0MVI1KGh? NUS2epJr\W6qYX7j[ZMh[XCxcITvd4l{KHerdHig[ZJtd3Srbnni Mn;lNlI{QDd7OEi=
H2170  NFrMN2NHfW6ldHnvckBCe3OjeR?= M2fUT|ExKM7:TR?= NIGxPVM1NTJ2IHi= NXHZVFlV\W6qYX7j[ZMh[XCxcITvd4l{KHerdHig[ZJtd3Srbnni M3XUbVIzOzh5OUi4

... 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

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    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:

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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