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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Cited by 15 Publications

7 Customer Reviews

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

    CX-4945 (5 μM) induced a time-dependent dephosphorylation of Thr308 p-Akt and Ser235/236 p-S6RP.

    Leukemia, 2014, 28(3):543-53. 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 MkPjT4lv[XOnIFHzd4F6 MYqxM|UwOTBizszN MWiwMlUhcA>? NU\tbHRRTE2VTx?= M2DyZ5Jm\HWlZYOgR2szKGurbnHz[UBi[3Srdnn0fUBidmRicHzheIVt\XRiYXfndoVo[XSrb36= MV[yOlM5OTR|Nx?=
HDMEC MkKyT4lv[XOnIFHzd4F6 MVqwMlI2NzBwNT:xJO69VQ>? NXKxOpgxOjRiaB?= M4D6PGROW09? M3vnVZJm\HWlZYOgR2szKGurbnHz[UBi[3Srdnn0fUwhfleIIHX4dJJme3Orb36gZY5lKHOnY4LleIlwdg>? MXeyOlM5OTR|Nx?=
HDMEC MWLGeY5kfGmxbjDBd5NigQ>? Ml74NE4zPS9yLkWvNUDPxE1? M1e5UVI1KGh? MnrQSG1UVw>? Mn\adoVlfWOnczDlfJBz\XO|aX;uJI9nKF[FQV2tNUBjfXRibn;0JGlESU1vMR?= NHXrXmMzPjN6MUSzOy=>
HDMEC NFW4bGJHfW6ldHnvckBCe3OjeR?= MUGxJO69VQ>? Ml34NlQhcA>? MlLXSG1UVw>? Ml32ZYZn\WO2czDzeYJk\WyudXzhdkBtd2OjbHn6ZZRqd25ib3[gUmZCXGNzIHHu[EBxcG:|cHjvMZA3PQ>? NIXMb|MzPjN6MUSzOy=>
A549  MmjVSpVv[3Srb36gRZN{[Xl? M4\Vb|MwOTEEoN88US=> MmK5OFghcA>? M2jTO5N2eHC{ZYPz[ZMhfGinIH3pZ5JweGmubHHyMYlv\HWlZXSg[ZhxemW|c3nvckBw\iCyLV\BTy=> M{Cyd|I3OzF6OECw
HDMEC M4HUOWtqdmG|ZTDBd5NigQ>? M1jhWlEuPTBizszN NVTVOIRNPSCq NELaTlBFVVOR NX22V3l2\GWlcnXhd4V{KEONMjDrbY5ie2ViYXP0bZZqfHlid3n0bI92fCCjZn\lZ5RqdmdiY3XscEB3cWGkaXzpeJk> MYmyOlE5QTV6Nh?=
HDMEC NH3MPYRHfW6ldHnvckBCe3OjeR?= NVW5dWFyPTBizszN NXrRRWY5OS93IHi= NV;WdYlQTE2VTx?= M4DzcoRm[3KnYYPld{B1cGViboXjcIVieiC|aXfuZYwhd2ZicHjvd5Bpd3K7bHH0[YQheDZ3IHnuJHRPTi4QsT3zeIlufWyjdHXkJGhFVUWFwrC= NXHCTotiOjZzOEm1PFY>
HEK293 MWLLbY5ie2ViQYPzZZk> MYGwMlXDqM7:TR?= NYfH[2FnOTVibXnu NX73TVQ6TE2VTx?= NFT3fHlz\WS3Y3XzJGNMOiCtaX7hd4Uh[WO2aY\peJk> MnrHNlU5QDd4Mk[=
Hela MYHLbY5ie2ViQYPzZZk> MVuwMlXDqM7:TR?= M1LF[VE2KG2rbh?= NEPrVFdFVVOR M{TwcZJm\HWlZYOgR2szKGurbnHz[UBi[3Srdnn0fS=> NHrVfYszPTh6N{[yOi=>
LAMA84 Mmf1T4lv[XOnIFHzd4F6 MXGwMlXDqM7:TR?= NGf0NYIyPSCvaX6= NHXYPFVFVVOR MkKwdoVlfWOnczDDT|Ihc2mwYYPlJIFkfGm4aYT5 NUnYVXQyOjV6OEe2NlY>
HEK293 NGLQR3JHfW6ldHnvckBCe3OjeR?= MWmzJO69VQ>? NWLFPGNvPSCq MmC0SG1UVw>? M1zoWWNMOiCyaH;zdIhwenmuYYTld{BmUUZ|ajDheEBU\XJzMke= MWOyOVg5PzZ{Nh?=
UM-SCC1 NWH2bZF3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHmNE4yNTNyIN88US=> M3WyflEuPSCm M{jG[WlEPTB;ND6xJO69VQ>? NEizU3gzPTd7OEC2NS=>
UM-SCC46 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV[zO4xVOC5zLUOwJO69VQ>? M1K5eVEuPSCm NY\vTWk1UUN3ME2zMlQh|ryP MYWyOVc6QDB4MR?=
UM-SCC1 M{\VUWZ2dmO2aX;uJGF{e2G7 M{\oSVAvPS92L{GwJO69VQ>? M13wPFczKGh? MX3kc5dvNXKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCQRj5EvGItKEKlbD3YUEBidmRidYCtdoVofWyjdHXzJJRp\SCneIDy[ZN{cW:wIH;mJJA2OyxicEKxMEBCWC1zIHHu[EBKVC16IHPvcoNmdnS{YYTpc44h\GWyZX7k[Y51dHl? NFj2UGUzPTd7OEC2NS=>
UM-SCC46 NG\rVGVHfW6ldHnvckBCe3OjeR?= MUCwMlUwPC9zMDFOwG0> NGDMW4Q4OiCq NVzT[5hy\G:5bj3y[Yd2dGG2ZYOgeIhmKGW6cILld5Nqd25ib3[gUmYuzLiELDDCZ4wuYExuIIC1N{wheDJzLDDBVE0yKGGwZDD1dE1z\We3bHH0[ZMhfGinIHX4dJJme3Orb36gTWwuQCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 M1;RPFI2Pzl6ME[x
NU-DUL NH\veo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXO1MVI2KM7:TR?= MWq0PEBp NVP3RY9PcW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? M33WeFI2Pzh6Mk[5
Oci Ly 3 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX61MVI2KM7:TR?= NFjxfpA1QCCq M3XPe4lvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> NFTKSGgzPTd6OEK2PS=>
Oci Ly 10 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFv6VXI2NTJ3IN88US=> MXu0PEBp M{LVfYlvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> NI[1TWgzPTd6OEK2PS=>
Oci Ly 1 M{jROGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHvOU0zPSEQvF2= MWG0PEBp M1jycolvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> MXqyOVc5QDJ4OR?=
Oci Ly 18 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUSyWpNTPS1{NTFOwG0> M3nRelQ5KGh? MYLpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 NHL2[nozPTd6OEK2PS=>
Oci Ly 19  M{HVXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrTS3BqPS1{NTFOwG0> MlnFOFghcA>? MlztbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> NHTQb2UzPTd6OEK2PS=>
Raji M3nVUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HsZVUuOjVizszN MonVOFghcA>? M4PicYlvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> MojFNlU4QDh{Nkm=
H1299 MlLVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYX4Wmx[OS93L{GwJO69VQ>? NYrIU2VCPzJiaB?= MkfGbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> MWeyOVc2ODNyOB?=
Calu-1  Mn7aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfBR3FzOS93L{GwJO69VQ>? NUnTemo{PzJiaB?= M1uyPYlvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> M3jKNlI2PzVyM{C4
H358 Mn;HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\vXVEwPS9zMDFOwG0> M{DEUlczKGh? M4\UXolvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> Mkf0NlU4PTB|MEi=
H1299 MnzDRZBweHSxc3nzJGF{e2G7 Ml7NNVAh|ryP NV\1[WRUPzJiaB?= MVnpcoR2[2W|IHHwc5B1d3Orcx?= NXvwVodwOjV5NUCzNFg>
Calu-1  MYfBdI9xfG:|aYOgRZN{[Xl? NILxN44yOCEQvF2= NGXGZXM4OiCq MVfpcoR2[2W|IHHwc5B1d3Orcx?= NGK1WpIzPTd3MEOwPC=>
H358 MUXBdI9xfG:|aYOgRZN{[Xl? NIP4O3kyOCEQvF2= Mn71O|IhcA>? NFGzV5BqdmS3Y3XzJIFxd3C2b4Ppdy=> MlryNlU4PTB|MEi=
PC9/GR NXnHU5hXTnWwY4Tpc44hSXO|YYm= M4nPR|UhyrWP MUG0PEBp MoTNbY5lfWOnczDheZRweGijZ4m= NIjRN2ozPTR6NkSwPS=>
PC9/ER NGO2TI1HfW6ldHnvckBCe3OjeR?= NFLhTYw2KML3TR?= NHuxNJo1QCCq NEX6Xo5qdmS3Y3XzJIF2fG:yaHHnfS=> M{TtT|I2PDh4NEC5
H28 M1e0R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3fUV|AvODFvM{Cg{txO M4\CfFczKGh? NUfqdWRHTE2VTx?= M{CyfGlEPTB;Nz6yJO69VQ>? Mlv3NlU1OjJyOEG=
H2052 MmfQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrrNE4xOS1|MDFOwG0> NWT2d2NyPzJiaB?= NX\PSZh4TE2VTx?= M1LrcWlEPTB;Mj6wJO69VQ>? NX23Ood7OjV2MkKwPFE>
UM-SCC-1 NInBb2hEdG:wb3flcolkKEG|c3H5 NGSwTXAxNjVvNTFOwG0> NELzc3IyPCCm MofSSG1UVw>? MYFCpIlvcGmkaYTzJINtd26xZ3XubYMhe3W{dnn2ZYwh[W6mIIPwbIVz\SCob4LtZZRqd25? MkPTNlU{PzlyMU[=
UM-SCC-46 NIDDU|lEdG:wb3flcolkKEG|c3H5 MlT2NE42NTVizszN M1nqWVE1KGR? NX;y[JR2TE2VTx?= MV1CpIlvcGmkaYTzJINtd26xZ3XubYMhe3W{dnn2ZYwh[W6mIIPwbIVz\SCob4LtZZRqd25? NX;a[WVlOjV|N{mwNVY>
U87-MG NHv0WoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHJUGoyNzVxMUCg{txO NHm0cHUzPC92OD:3NkBp MkfYSG1UVw>? NX;OVI0zcW6qaXLpeJMh[2WubDDndo94fGhiYn;0bEBkd26lZX70doF1cW:wIHHu[EB1cW2nIHTldIVv\GWwdHz5 MnGwNlUzPDF6OUe=
MDA-MB-231 NXLyV3BLTnWwY4Tpc44hSXO|YYm= M1PJdVIwPS9zMDFOwG0> M{D1flQhcA>? MVTk[YNz\WG|ZYOgeIhmKGOxboP0bZR2fGm4ZTDwbI9{eGixconsZZRqd25ib3[gZo91cCBicD3TOVI6NXB4NTDhcoQheC2VMUK5MWFsfA>? M1PQUVI2OTV|N{K1
MDA-MB-231 Mn\4SpVv[3Srb36gRZN{[Xl? NFLRNnkzNzVxMUCg{txO NWLPcIFrPCCq M2XGfolvcGmkaYTzJJNmemmwZTC1NlkheGixc4Doc5J6dGG2aX;uJIFv\CC2aHWg[ZhxemW|c3nvckBw\iCLTD22MEBKVC16 MV6yOVE2Ozd{NR?=
ARPE-19 M2\wcmtqdmG|ZTDBd5NigQ>? NUG5dm1nPS9zMD:yNEDPxE1? MXmyOE81QCCq M1;le4lvcGmkaYTzJGNMOiCtaX7hd4Uh[WO2aY\peJkh[XRiYTDjc45k\W62cnH0bY9vKG:oIEZCpO69VQ>? M33TVVI1Pjh4MEiw
ARPE-19 MkP5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\5ZmcyOCEQvF2= NUfZWmpNOjRvOU[gbC=> NUDvfYlzTE2VTx?= MV\pcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 NILreWwzPDZ6NkC4NC=>
HCT116  MlTIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LqdFExKM7:TR?= NIGxPFkzPC17NjDo M2niTWROW09? NIDGc|lqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 NUT5TWZVOjR4OE[wPFA>
ARPE-19 NIXjWopHfW6ldHnvckBCe3OjeR?= MnjDNVAh|ryP MV[0JIg> M1XkUWROW09? MXrjZZV{\XNiRWKtd5Rz\XO|IILld5BwdnOnIH;2[ZIhfGinIICt[WlHOs7zIHLyZY5kcCxiYoX0JIRw\XNibn;0JIlv\HWlZTDDTG9RyqB? MlzvNlQ3QDZyOEC=
HCT116  NUW1ZpQyTnWwY4Tpc44hSXO|YYm= MXSxNEDPxE1? MV[0JIg> M3jufGROW09? MWHjZZV{\XNiRWKtd5Rz\XO|IILld5BwdnOnIH;2[ZIhfGinIICt[WlHOs7zIHLyZY5kcCxiYoX0JIRw\XNibn;0JIlv\HWlZTDDTG9RyqB? NHr2Z3ozPDZ6NkC4NC=>
HCT116  M2DkUGFxd3C2b4Ppd{BCe3OjeR?= MUOxNEDPxE1? MkPkNlQwPDhiaB?= M3Ti[2ROW09? NITzNZlqdmS3Y3XzJIFxd3C2b4Ppdy=> MX[yOFY5PjB6MB?=
Nalm6  NXT0do5nTnWwY4Tpc44hSXO|YYm= M1HyZlExNzJyIN88US=> NFjuZ4wzPCCq MWXy[ZN2dHS|IHnuJIRm[3KnYYPl[EBRXEWQIIDoc5NxcG:{eXzheIlwdiCjdDD0bIUhS0t{IIThdodmfCC{ZYPp[JVmKFN|OECgZY5lKGOxbnPvcYl1[W62IHTve45z\We3bHH0bY9vKG:oIGDUSW4heHKxdHXpckBmgHC{ZYPzbY9v NYXhRYZMOjR3NkG3PVI>
SUP-B15 MY\GeY5kfGmxbjDBd5NigQ>? MUmxNE8zOCEQvF2= NEH6UVYzPCCq NYXSdmMzemW|dXz0d{BqdiCmZXPy[YF{\WRiUGTFUkBxcG:|cHjvdplt[XSrb36gZZQhfGinIFPLNkB1[XKpZYSgdoV{cWS3ZTDTN|gxKGGwZDDjc45kd22rdHHueEBld3ewcnXneYxifGmxbjDv[kBRXEWQIIDyc5RmcW5iZYjwdoV{e2mxbh?= MXeyOFU3OTd7Mh?=
Nalm6  MV;BdI9xfG:|aYOgRZN{[Xl? M13YcFYwOTBizszN M3fEUFQ5KGh? NEHxWFNqdmS3Y3XzJIFxd3C2b4Ppdy=> MUSyOFU3OTd7Mh?=
SUP-B15 NF;lVHRCeG:ydH;zbZMhSXO|YYm= MYC2M|ExKM7:TR?= MlS2OFghcA>? NHfOU5NqdmS3Y3XzJIFxd3C2b4Ppdy=> NWrxW2Z6OjR3NkG3PVI>
C2C12 MnPlSpVv[3Srb36gRZN{[Xl? NID0fWE{KM7:TR?= NG\TVowyOi9{ND:0PEBp M37Ie4lvcGmkaYTzJJRp\SCneIDy[ZN{cW:wIH;mJI9{fGWxY3zhd5Qh\GmoZnXy[Y51cWG2aX;uJI1iemuncoOgZY5lKEGtdDDwbI9{eGixconsZZRqd25? MYGyOFI6OzBzMR?=
Jurkat NITVbVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DielEuOTBizszN Ml;WOFghcA>? NYH6c2VoUUN3ME20Mlkh|ryP MYCyOFI2OzB{NB?=
CEM-R MkLLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLhS3UyNTFyIN88US=> NUHpR4JnPDhiaB?= MU\JR|UxRTRizszN MoTiNlQzPTNyMkS=
CEM-S NVTFTYNCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV:xMVExKM7:TR?= NYr0ZYxRPDhiaB?= MUTJR|UxRTRwNjFOwG0> MYOyOFI2OzB{NB?=
MOLT-4 NFPjWVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUOxMVExKM7:TR?= NUDMcXkyPDhiaB?= M{jGfWlEPTB;NT63JO69VQ>? MX:yOFI2OzB{NB?=
PF-382 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnLSNU0yOCEQvF2= M1e5VVQ5KGh? NWPSeHRCUUN3ME20MlUh|ryP MlXrNlQzPTNyMkS=
ALL-SIL M{j0UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVmxMVExKM7:TR?= M1P6OlQ5KGh? NWmw[Ig1UUN3ME21Mlch|ryP M3PlTlI1OjV|MEK0
HPB-ALL MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;6V3hmOS1zMDFOwG0> NIjOUnI1QCCq NYH4VYN3UUN3ME22MlEh|ryP M2XlOFI1OjV|MEK0
DND-41 NEXIV41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEP3UmEyNTFyIN88US=> Ml7aOFghcA>? MVvJR|UxRTlizszN NIfEeXczPDJ3M{CyOC=>
ALL-SIL MmDMRZBweHSxc3nzJGF{e2G7 MnrWOUDPxE1? MXOyOE81QCCq MYPpcoR2[2W|IHHwc5B1d3Orcx?= NWDUXWozOjR{NUOwNlQ>
DND-41 MlHaRZBweHSxc3nzJGF{e2G7 MVe1JO69VQ>? M4K4T|I1NzR6IHi= M1KyOYlv\HWlZYOgZZBweHSxc3nz NWXPWplxOjR{NUOwNlQ>
MOLT-4 NX7YbFl2SXCxcITvd4l{KEG|c3H5 MnfNOUDPxE1? NEnmXGszPC92ODDo NGSzdVFqdmS3Y3XzJIFxd3C2b4Ppdy=> MmDKNlQzPTNyMkS=
U-266 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUiwMVQxKM7:TR?= MoXCOFghcA>? MVrJR|UxRTF7LkigxtVOyqB? MXGyOFA5PjR7NB?=
INA-6 NIH2RXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPHU4IxNTRyIN88US=> NILZdFg1QCCq NIjvcmlKSzVyPUKuOFIhyrWP M3\w[|I1ODh4NEm0
Jeko-1 NYHqdohsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXyRXJOOC12MDFOwG0> NILPUYs1QCCq Ml:4TWM2OD1{LkSgxtVOyqB? Mn\1NlQxQDZ2OUS=
Rec-1 Mn[zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYmwMVQxKM7:TR?= Mki0OFghcA>? NEfvdXJKSzVyPUGuOFYhyrWPwrC= M2H1O|I1ODh4NEm0
A549 MkfGSpVv[3Srb36gRZN{[Xl? MmPHNVAh|ryP MVKxNk8zPC92ODDo NXj2VpBNcW6qaXLpeJMhXEeILd8yNU1qdmS3Y3XkJI1q\3KjdHnvckBidmRiaX72ZZNqd25? MVGyOFAzOzl|OB?=
A549 NFnxcXVHfW6ldHnvckBCe3OjeR?= NHm3TGg{KM7:TR?= Mm\oOFghcA>? M4HB[4lvcGmkaYTzJHRITi4QskGtbY5lfWOnZDDhZ5RqfmG2aX;uJI9nKFOvYXSgZY5lKGW6cILld5Nqd25ib3[gV45icWxiYX7kJHR4cXO2 MXKyOFAzOzl|OB?=
S-LAMA84 M{PPZmZ2dmO2aX;uJGF{e2G7 NX[xN21[O8LizszN NFGyfpEzPCCq NFmyOoJFVVOR MV;y[YR2[2W|IFPLNkBi[3Srdnn0fS=> M3;OVlI1ODF{MUC5
R-LAMA84 NHfZeoNHfW6ldHnvckBCe3OjeR?= NF7xenc{yqEQvF2= M3i1cFI1KGh? MkW3SG1UVw>? MmOzdoVlfWOnczDDT|Ih[WO2aY\peJk> MonGNlQxOTJzMEm=
S-LAMA84 NV60O3JLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\ab3IzNjVvMUCg{txO NVjreZd2PDhiaB?= NXTqWZl6TE2VTx?= M13KPYlvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> MXiyOFAyOjFyOR?=
R-LAMA84 NVPZclFXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXmNk42NTFyIN88US=> NVn6NWk1PDhiaB?= NWW5bYg6TE2VTx?= MXrpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 M{TjNlI1ODF{MUC5
A549 NVX5[5d2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXteFBWOC1|MDFOwG0> NVriZohVPzJiaB?= M1zO[GROW09? NXfDRZlsUUN3ME20MlE2KM7:TTygbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> MVuyN|Y2OTR2Mx?=
H1299 M2Pqe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mme2NE0{OCEQvF2= MVm3NkBp MUfEUXNQ MoDPTWM2OD1zLkiwJO69VSxiaX7obYJqfHNiY3XscEBoem:5dHigZ49v[2WwdILheIlwdiCmZYDlcoRmdnSueR?= MmDRNlM3PTF2NEO=
A549 NUjzZ4dyTnWwY4Tpc44hSXO|YYm= NIDQPIoyNzFyIN88US=> NFTHS2Q1QCCq NE\OepNFVVOR M{TuV4xm[WS|IITvJIEh\G:|ZT3k[ZBmdmSnboSg[IVkemWjc3WgbY4hVm:2Y3igdoVxd3K2ZYKgZYN1cX[rdIm= NITPPYgzOzZ3MUS0Ny=>
LNCap MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrCNE0{OCEQvF2= MmPmOEBl NISyempKSzVyPUSuOVnDqM7:TR?= MXGyNlg{OjNzNh?=
A431  NHTHSmRHfW6ldHnvckBCe3OjeR?= NULl[XdjOTBizszN Mlq2N|AhdWmw NGfRcWxifHSnboXheIV{KFCLM1utRYt1NW2WT2Kgd4lodmGuaX7n M{Pr[FIzOzh5OUi4
H2170  MojkSpVv[3Srb36gRZN{[Xl? MmnVNVAh|ryP MoPuN|AhdWmw NVr1PIpi[XS2ZX71ZZRmeyCSSUPLMWFsfC2vVF;SJJNq\26jbHnu[y=> Ml3sNlI{QDd7OEi=
A431  Mn76SpVv[3Srb36gRZN{[Xl? NEi0VVkyOCEQvF2= MmPqOE0zPCCq NVHjVIYy\W6qYX7j[ZMh[XCxcITvd4l{KHerdHig[ZJtd3Srbnni MYmyNlM5Pzl6OB?=
H2170  MUXGeY5kfGmxbjDBd5NigQ>? NFzGSpIyOCEQvF2= MWW0MVI1KGh? NXrOeWx4\W6qYX7j[ZMh[XCxcITvd4l{KHerdHig[ZJtd3Srbnni NX\N[YlROjJ|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 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
NCT02128282 Recruiting Cholangiocarcinoma Senhwa Biosciences Inc. June 2014 Phase 1|Phase 2
NCT01199718 Unknown status Multiple Myeloma Cylene Pharmaceuticals September 2010 Phase 1
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
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