Silmitasertib (CX-4945)

For research use only.

Catalog No.S2248

54 publications

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). Silmitasertib induces autophagy and promotes apoptosis. Phase 1/2.

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Selleck's Silmitasertib (CX-4945) has been cited by 54 publications

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). Silmitasertib induces autophagy and promotes apoptosis. 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 MXXLbY5ie2ViQYPzZZk> NGiwclkyNzVxMUCg{txO NXH2W5d[OC53IHi= MWHEUXNQ MUHy[YR2[2W|IFPLNkBscW6jc3WgZYN1cX[rdImgZY5lKHCuYYTlcIV1KGGpZ4Ll[4F1cW:w NEjaU4QzPjN6MUSzOy=>
HDMEC NVW4N|FXU2mwYYPlJGF{e2G7 M{Dv[|AvOjVxMD61M|Eh|ryP Mnz0NlQhcA>? NGXnb4ZFVVOR M{PoSZJm\HWlZYOgR2szKGurbnHz[UBi[3Srdnn0fUwhfleIIHX4dJJme3Orb36gZY5lKHOnY4LleIlwdg>? M{P6fFI3OzhzNEO3
HDMEC NHT0NXpHfW6ldHnvckBCe3OjeR?= NX2zc2o2OC5{NT:wMlUwOSEQvF2= NXTBR2NDOjRiaB?= NXHjR2Y3TE2VTx?= NFXxO|Bz\WS3Y3XzJIV5eHKnc4Ppc44hd2ZiVlPBUU0yKGK3dDDuc5QhUUODTT2x NGf1RVgzPjN6MUSzOy=>
HDMEC NFuxe2VHfW6ldHnvckBCe3OjeR?= MUexJO69VQ>? NUj6[|ZLOjRiaB?= M3f5emROW09? MWXh[oZm[3S|IIP1ZoNmdGy3bHHyJIxw[2GuaYrheIlwdiCxZjDOSmFV[zFiYX7kJJBpd3OyaH:tdFY2 MonxNlY{QDF2M{e=
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HEK293 NV\5O4F3U2mwYYPlJGF{e2G7 MViwMlXDqM7:TR?= NVnHVoJYOTVibXnu M4XKeWROW09? M4HkPJJm\HWlZYOgR2szKGurbnHz[UBi[3Srdnn0fS=> NHPKd2gzPTh6N{[yOi=>
Hela MXfLbY5ie2ViQYPzZZk> NH;iXVgxNjYEoN88US=> NW[2eY57OTVibXnu MV7EUXNQ M{jibpJm\HWlZYOgR2szKGurbnHz[UBi[3Srdnn0fS=> M33Y[lI2QDh5NkK2
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NU-DUL M1y0bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfEeHc2NTJ3IN88US=> NVL0fnRzPDhiaB?= NFu0VZpqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NV2yR2tZOjV5OEiyOlk>
Oci Ly 3 Mn;MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3zZN|UuOjVizszN MX:0PEBp NGX3TJhqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 MlLENlU4QDh{Nkm=
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Oci Ly 1 NUK3NlNkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;NOU0zPSEQvF2= M{XiRlQ5KGh? MWDpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 MXmyOVc5QDJ4OR?=
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Oci Ly 19  MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWG1MVI2KM7:TR?= MojVOFghcA>? MYjpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 M{\m[lI2Pzh6Mk[5
Raji NVTBWXJyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnu5OU0zPSEQvF2= NFPxfFM1QCCq NVLCTIRYcW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? MojINlU4QDh{Nkm=
H1299 NXrLSpgzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjz[HcyNzVxMUCg{txO MWO3NkBp NHrDeHdqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NVPBcYM4OjV5NUCzNFg>
Calu-1  MlLCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV:xM|UwOTBizszN NX\INYl4PzJiaB?= NH;6U5RqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NX;5OGs1OjV5NUCzNFg>
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H1299 NV7Fd4JFSXCxcITvd4l{KEG|c3H5 NWDUVnRWOTBizszN MmnlO|IhcA>? NXfLdY5mcW6mdXPld{BieG:ydH;zbZM> MnH3NlU4PTB|MEi=
Calu-1  NGrnSGVCeG:ydH;zbZMhSXO|YYm= M4rUblExKM7:TR?= MmriO|IhcA>? Ml7NbY5lfWOnczDhdI9xfG:|aYO= MXiyOVc2ODNyOB?=
H358 NGrmcXhCeG:ydH;zbZMhSXO|YYm= NUXLUo9tOTBizszN M2LFWVczKGh? M3PuOIlv\HWlZYOgZZBweHSxc3nz Mlr5NlU4PTB|MEi=
PC9/GR NVL6XXVpTnWwY4Tpc44hSXO|YYm= NE\sV2M2KML3TR?= M17HOFQ5KGh? NXHvS4JScW6mdXPld{BifXSxcHjh[5k> M1vUZ|I2PDh4NEC5
PC9/ER NGXIdopHfW6ldHnvckBCe3OjeR?= M2HMRVUhyrWP MXW0PEBp MlfZbY5lfWOnczDheZRweGijZ4m= NUH1Z|IyOjV2OE[0NFk>
H28 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUK4Z2FVOC5yMT2zNEDPxE1? M{LCXlczKGh? MoTzSG1UVw>? MXfJR|UxRTdwMjFOwG0> NHm2W2IzPTR{MkC4NS=>
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MDA-MB-231 NX2wTWlrTnWwY4Tpc44hSXO|YYm= NXu5VXBROi93L{GwJO69VQ>? NXSwd5NtPCCq NGLUcGll\WO{ZXHz[ZMhfGinIHPvcpN1cXS3dHn2[UBxcG:|cHjvdplt[XSrb36gc4Yh[m:2aDCgdE1UPTJ7LYC2OUBidmRicD3TNVI6NUGtdB?= NHzyVVgzPTF3M{eyOS=>
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ARPE-19 NHfrdXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TEO|ExKM7:TR?= NXHp[3JYOjRvOU[gbC=> NFq4dnpFVVOR NYThfIM1cW6qaXLpeJMh[2WubDDndo94fGhidHnt[UBl\XCnbnTlcpRtgQ>? M1vmVVI1Pjh4MEiw
HCT116  NGXOVHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2K3UlExKM7:TR?= Mm\oNlQuQTZiaB?= MVHEUXNQ M{fJeolvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk> MkD4NlQ3QDZyOEC=
ARPE-19 MlHTSpVv[3Srb36gRZN{[Xl? MWmxNEDPxE1? MkG0OEBp M4\6eGROW09? M2LrcoNifXOnczDFVk1{fHKnc4OgdoV{eG:wc3Wgc5ZmeiC2aHWgdE1mUUZ{zsGgZpJidmOqLDDieZQh\G:nczDuc5QhcW6mdXPlJGNJV1EEoB?= M{nsdVI1Pjh4MEiw
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HCT116  NHLPRnBCeG:ydH;zbZMhSXO|YYm= Mn;uNVAh|ryP NV[5WY06OjRxNEigbC=> NWrsVYc1TE2VTx?= NE\1b5hqdmS3Y3XzJIFxd3C2b4Ppdy=> MYGyOFY5PjB6MB?=
Nalm6  Mo\YSpVv[3Srb36gRZN{[Xl? MXuxNE8zOCEQvF2= NIjxWGQzPCCq MXXy[ZN2dHS|IHnuJIRm[3KnYYPl[EBRXEWQIIDoc5NxcG:{eXzheIlwdiCjdDD0bIUhS0t{IIThdodmfCC{ZYPp[JVmKFN|OECgZY5lKGOxbnPvcYl1[W62IHTve45z\We3bHH0bY9vKG:oIGDUSW4heHKxdHXpckBmgHC{ZYPzbY9v MlKxNlQ2PjF5OUK=
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C2C12 M3LCTGZ2dmO2aX;uJGF{e2G7 NFfBSVQ{KM7:TR?= MWexNk8zPC92ODDo Mnv2bY5pcWKrdIOgeIhmKGW6cILld5Nqd25ib3[gc5N1\W:lbHHzeEBlcW[oZYLlcpRq[XSrb36gcYFzc2W{czDhcoQhSWu2IIDoc5NxcG:{eXzheIlwdg>? M4\QZlI1Ojl|MEGx
Jurkat Ml3NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3DUlAyNTFyIN88US=> MUG0PEBp M4PJXGlEPTB;ND65JO69VQ>? M3PI[FI1OjV|MEK0
CEM-R NFfOSIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWSxMVExKM7:TR?= MYW0PEBp NFr4XppKSzVyPUSg{txO MYGyOFI2OzB{NB?=
CEM-S NW[ycGR6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnkV|BiOS1zMDFOwG0> NWry[oh6PDhiaB?= Mny0TWM2OD12Lk[g{txO MU[yOFI2OzB{NB?=
MOLT-4 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVOxMVExKM7:TR?= MXi0PEBp Moj2TWM2OD13Lkeg{txO MX2yOFI2OzB{NB?=
PF-382 M1;mTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvjeGsyNTFyIN88US=> NIPEfm01QCCq MYfJR|UxRTRwNTFOwG0> NVnh[HpkOjR{NUOwNlQ>
ALL-SIL M4TaUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFi0clgyNTFyIN88US=> NEjnN4c1QCCq MXnJR|UxRTVwNzFOwG0> MXmyOFI2OzB{NB?=
HPB-ALL NVSydm8xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HYVlEuOTBizszN MkPlOFghcA>? M{LicWlEPTB;Nj6xJO69VQ>? NVLwNZlKOjR{NUOwNlQ>
DND-41 NIrWZWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWfS[4N7OS1zMDFOwG0> MYm0PEBp M1;iU2lEPTB;OTFOwG0> MXOyOFI2OzB{NB?=
ALL-SIL NUfhNGdbSXCxcITvd4l{KEG|c3H5 Mn3xOUDPxE1? NWradZc1OjRxNEigbC=> MkLzbY5lfWOnczDhdI9xfG:|aYO= M1zCZlI1OjV|MEK0
DND-41 NITMeYxCeG:ydH;zbZMhSXO|YYm= MWi1JO69VQ>? MoPVNlQwPDhiaB?= NGPiPXZqdmS3Y3XzJIFxd3C2b4Ppdy=> NGSzcFkzPDJ3M{CyOC=>
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U-266 NY\tcng1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{j1bVAuPDBizszN MkT2OFghcA>? M1iwbWlEPTB;MUmuPEDDvU4EoB?= M2nvNlI1ODh4NEm0
INA-6 M3\2Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXy3c2hbOC12MDFOwG0> NVS5NHpWPDhiaB?= M3i2R2lEPTB;Mj60NkDDvU1? NH7Dc4YzPDB6NkS5OC=>
Jeko-1 M4r3dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPVNE01OCEQvF2= M2rKSFQ5KGh? M1r1[WlEPTB;Mj60JOK2VcLi NE[0V|IzPDB6NkS5OC=>
Rec-1 NUi3XYoyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrpb|RZOC12MDFOwG0> MYe0PEBp NHnNe2ZKSzVyPUGuOFYhyrWPwrC= NIDFRpYzPDB6NkS5OC=>
A549 NVu3U2lzTnWwY4Tpc44hSXO|YYm= MX:xNEDPxE1? NV;ZUYcyOTJxMkSvOFghcA>? M1n2ZYlvcGmkaYTzJHRITi4QskGtbY5lfWOnZDDtbYdz[XSrb36gZY5lKGmwdnHzbY9v M1zlT|I1ODJ|OUO4
A549 MXrGeY5kfGmxbjDBd5NigQ>? MWezJO69VQ>? Mkn1OFghcA>? NGPQW4NqdmirYnn0d{BVT0ZvzsKxMYlv\HWlZXSgZYN1cX[jdHnvckBw\iCVbXHkJIFv\CCneIDy[ZN{cW:wIH;mJHNv[WmuIHHu[EBVf2m|dB?= M1;pUVI1ODJ|OUO4
S-LAMA84 M2jseGZ2dmO2aX;uJGF{e2G7 Mn3KN:Kh|ryP MoT2NlQhcA>? MlTiSG1UVw>? NIq2W5Rz\WS3Y3XzJGNMOiCjY4Tpeol1gQ>? MkTTNlQxOTJzMEm=
R-LAMA84 NETjU21HfW6ldHnvckBCe3OjeR?= M13VO|PDqM7:TR?= NV[zeHpjOjRiaB?= NYq0VItiTE2VTx?= MnPvdoVlfWOnczDDT|Ih[WO2aY\peJk> NHP2XIQzPDBzMkGwPS=>
S-LAMA84 M{nKfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofmNk42NTFyIN88US=> M{WyXVQ5KGh? M{DKSmROW09? M3f3RolvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> MYeyOFAyOjFyOR?=
R-LAMA84 NGXD[5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jQNVIvPS1zMDFOwG0> NEjtNXE1QCCq M4roZ2ROW09? MYXpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 MnK5NlQxOTJzMEm=
A549 NHvnN5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVOwMVMxKM7:TR?= MYK3NkBp NF;UUmRFVVOR M3vhfGlEPTB;ND6xOUDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJINwdmOnboTyZZRqd25iZHXw[Y5l\W62bIm= MkLONlM3PTF2NEO=
H1299 NH61OpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWGwMVMxKM7:TR?= NGDNWms4OiCq MonsSG1UVw>? NIjBemRKSzVyPUGuPFAh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 NWK5[m5tOjN4NUG0OFM>
A549 NYn5R49xTnWwY4Tpc44hSXO|YYm= MlXYNU8yOCEQvF2= M{T0OFQ5KGh? MmeySG1UVw>? M4\DSoxm[WS|IITvJIEh\G:|ZT3k[ZBmdmSnboSg[IVkemWjc3WgbY4hVm:2Y3igdoVxd3K2ZYKgZYN1cX[rdIm= MWOyN|Y2OTR2Mx?=
LNCap M{nocmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vBclAuOzBizszN NU\s[XA4PCCm M2LoXGlEPTB;ND61PeKh|ryP MXmyNlg{OjNzNh?=
A431  MoDNSpVv[3Srb36gRZN{[Xl? NFHwR5UyOCEQvF2= MmG5N|AhdWmw MULheJRmdnWjdHXzJHBKO0tvQXv0MY1VV1Jic3nncoFtcW6p Mn:wNlI{QDd7OEi=
H2170  MlzISpVv[3Srb36gRZN{[Xl? NILme2syOCEQvF2= M4LtdlMxKG2rbh?= NGL1RpFifHSnboXheIV{KFCLM1utRYt1NW2WT2Kgd4lodmGuaX7n M3;CR|IzOzh5OUi4
A431  NVe4Z|h[TnWwY4Tpc44hSXO|YYm= M3eyclExKM7:TR?= M1rrV|QuOjRiaB?= NWC2[opv\W6qYX7j[ZMh[XCxcITvd4l{KHerdHig[ZJtd3Srbnni NU\OV|Q{OjJ|OEe5PFg>
H2170  M2XJTWZ2dmO2aX;uJGF{e2G7 MX2xNEDPxE1? Mki4OE0zPCCq NWn2[FJ5\W6qYX7j[ZMh[XCxcITvd4l{KHerdHig[ZJtd3Srbnni M3;zUVIzOzh5OUi4

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-S6K1(T389) / S6K1 / p-S6(S235/236) / S6; 

PubMed: 30683840     


DLD-1 cells were incubated with 25 μM silmitasertib for 16 h. The levels of the indicated proteins were analyzed by western blot.

p-AKT(S129) / p-AKT(T308) / p-AKT(S473) / AKT / p-ERK / ERK / TP53 / p-p21(Th145) / p21 / Bcl-xl; 

PubMed: 25798061     


CX-4945 altered PI3K/AKT/Bcl-XL, ERK/AP-1 and TP53/p21proteins in HNSCC. UM-SCC-1 (left) and UM-SCC-46 (right) cell lines were treated with 4 and 10 μM CX-4945, whole cell lysates were harvested 6 and 24 hours after treatment, and subjected to SDS-PAGE and Western blot of indicated proteins. β-action was used as a loading control.

p-Smad2 (Cytosol) / Smad2/3 (Cytosol) / Smad2/3 (Nucleus) / Twist / Snail; 

PubMed: 24023938     


The effect of CX-4945 on TGF-β1-induced activation of Smad and expression of Snail and Twist was evaluated using Western blot analysis. Briefly, after 24 h serum starvation, A549 cells were treated with TGF-β1 (5 ng/ml) alone or in combination with CX-4945 in media containing 0.1% FBS for 48 h. Cytosolic and Nuclear fractions were obtained. Actin and histone H3 were used as internal control of cytosolic and nuclear fraction, respectively. The relative, normalized ratio between p-Smad2 and actin was presented. 

30683840 25798061 24023938
Immunofluorescence
β-catenin; 

PubMed: 24023938     


Nuclear translocation of β-catenin and its inhibition by CX-4945 were confirmed by immunocytochemistry. Nuclei were counterstained with Hoechst 33342. All scale bars represent 20 µm.

E-cadherin / Vimentin; 

PubMed: 24023938     


The effect of CX-4945 on the TGF-β1-induced expression of epithelial and mesenchymal markers was evaluated by immunocytochemistry. Briefly, after 24 h serum starvation, A549 cells were treated with TGF-β1 (5 ng/ml) alone or in combination with CX-4945 in media containing 0.1% FBS for 72 h. All scale bars represent 200 µm.

24023938
Growth inhibition assay
Cell viability; 

PubMed: 30316146     


CX-4945 decreases cell viability of HuCCT1, EGI-1, and Liv27 CCA cell lines in dose-dependent manner (IC50of 7.3, 9.5, and 9.4 μM, respectively) (A)

30316146
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]
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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:[1]
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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:[1]
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  • Animal Models: Female immunocompromised mice CrTac:Ncr-Foxn1nu injected with BxPC-3 or BT-474 cells
  • 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
Smiles OC(=O)C1=CC2=C(C=C1)C3=CN=CC=C3C(=N2)NC4=CC(=CC=C4)Cl

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
% DMSO % % Tween 80 % ddH2O
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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 (mg) = Concentration (mM) × Volume (mL) × 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 )

  • C1
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    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
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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:

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

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