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
USD 170 In stock
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 M3v0d2tqdmG|ZTDBd5NigQ>? MmDDNU82NzFyIN88US=> NVnnSlhmOC53IHi= M1SxT2ROW09? NH63d45z\WS3Y3XzJGNMOiCtaX7hd4Uh[WO2aY\peJkh[W6mIIDsZZRmdGW2IHHn[5Jm\2G2aX;u NEPhfpEzPjN6MUSzOy=>
HDMEC NEPKPYhMcW6jc3WgRZN{[Xl? NXnwSlA3OC5{NT:wMlUwOSEQvF2= M2\ndFI1KGh? M{j5eWROW09? MX\y[YR2[2W|IFPLNkBscW6jc3WgZYN1cX[rdImsJJZYTiCneIDy[ZN{cW:wIHHu[EB{\WO{ZYTpc44> NGn0e3czPjN6MUSzOy=>
HDMEC NUfnO5JvTnWwY4Tpc44hSXO|YYm= NFvocIExNjJ3L{CuOU8yKM7:TR?= MlH6NlQhcA>? M4fzW2ROW09? M1\yWpJm\HWlZYOg[ZhxemW|c3nvckBw\iCYQ1HNMVEh[nW2IH7veEBKS0GPLUG= MUKyOlM5OTR|Nx?=
HDMEC M13KRWZ2dmO2aX;uJGF{e2G7 MnHxNUDPxE1? NFL2W3IzPCCq NF7uXJVFVVOR MUnh[oZm[3S|IIP1ZoNmdGy3bHHyJIxw[2GuaYrheIlwdiCxZjDOSmFV[zFiYX7kJJBpd3OyaH:tdFY2 M1vGRVI3OzhzNEO3
A549  MonDSpVv[3Srb36gRZN{[Xl? NVf3fY43Oy9zMNMg{txO NVywZlFvPDhiaB?= NEDmSHR{fXCycnXzd4V{KHSqZTDtbYNzd3CrbHzhdk1qdmS3Y3XkJIV5eHKnc4Ppc44hd2ZicD3GRWs> NV7mR2J{OjZ|MUi4NFA>
HDMEC MVjLbY5ie2ViQYPzZZk> MlXVNU02OCEQvF2= Mn25OUBp NEDq[JZFVVOR MW\k[YNz\WG|ZYOgR2szKGurbnHz[UBi[3Srdnn0fUB4cXSqb4X0JIFn\mWldHnu[{Bk\WyuII\pZYJqdGm2eR?= MWCyOlE5QTV6Nh?=
HDMEC M{XqOmZ2dmO2aX;uJGF{e2G7 Mnv5OVAh|ryP NWr5VoM2OS93IHi= NWq5W2dVTE2VTx?= NFrk[3Vl\WO{ZXHz[ZMhfGinIH71Z4xm[XJic3nncoFtKG:oIIDoc5NxcG:{eXzheIVlKHB4NTDpckBVVkZvzsGtd5RqdXWuYYTl[EBJTE2HQ9Mg NV7UZnNiOjZzOEm1PFY>
HEK293 NF\JXIxMcW6jc3WgRZN{[Xl? NIHIb4sxNjYEoN88US=> MXOxOUBucW5? M2jISWROW09? M4HoTJJm\HWlZYOgR2szKGurbnHz[UBi[3Srdnn0fS=> MViyOVg5PzZ{Nh?=
Hela MlnhT4lv[XOnIFHzd4F6 M1HJblAvPcLizszN M3PYblE2KG2rbh?= NGjESFFFVVOR NFPCTXdz\WS3Y3XzJGNMOiCtaX7hd4Uh[WO2aY\peJk> M1zMUlI2QDh5NkK2
LAMA84 M3jjWGtqdmG|ZTDBd5NigQ>? NXPaNZBLOC53wrFOwG0> M1O4eVE2KG2rbh?= M4LoR2ROW09? NXXLOGh6emWmdXPld{BEUzJia3nuZZNmKGGldHn2bZR6 NH;0XHAzPTh6N{[yOi=>
HEK293 MYXGeY5kfGmxbjDBd5NigQ>? NVOzNXJlOyEQvF2= M1TVeFUhcA>? NUL0[VFKTE2VTx?= NGW4d|hEUzJicHjvd5Bpd3K7bHH0[ZMh\UmIM3qgZZQhW2W{MUK3 MlLtNlU5QDd4Mk[=
UM-SCC1 NIjCXohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlG2NE4yNTNyIN88US=> NEPIOVcyNTViZB?= M3rON2lEPTB;ND6xJO69VQ>? NIDsPHUzPTd7OEC2NS=>
UM-SCC46 NHf1V4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3WT5IxNjFvM{Cg{txO MWixMVUh\A>? MojXTWM2OD1|LkSg{txO M{SwVVI2Pzl6ME[x
UM-SCC1 NX;Wb2p{TnWwY4Tpc44hSXO|YYm= NV;XTohFOC53L{SvNVAh|ryP NFTmWYo4OiCq MYHkc5dvNXKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCQRj5EvGItKEKlbD3YUEBidmRidYCtdoVofWyjdHXzJJRp\SCneIDy[ZN{cW:wIH;mJJA2OyxicEKxMEBCWC1zIHHu[EBKVC16IHPvcoNmdnS{YYTpc44h\GWyZX7k[Y51dHl? MYSyOVc6QDB4MR?=
UM-SCC46 NILLXnJHfW6ldHnvckBCe3OjeR?= NXXjb4JmOC53L{SvNVAh|ryP M4PkfVczKGh? MkDw[I94di2{ZXf1cIF1\XNidHjlJIV5eHKnc4Ppc44hd2ZiTl[tyNhDNCCEY3ytXGwtKHB3MzygdFIyNCCDUD2xJIFv\CC3cD3y[Yd2dGG2ZYOgeIhmKGW6cILld5Nqd25iSVytPEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 NHvOWY8zPTd7OEC2NS=>
NU-DUL NXvmNIE3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPxWXY2NTJ3IN88US=> NGf1NZo1QCCq NIW4VmZqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NG\j[pIzPTd6OEK2PS=>
Oci Ly 3 M2DPNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYG1MVI2KM7:TR?= MXu0PEBp M2KyO4lvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> NYjDNJRuOjV5OEiyOlk>
Oci Ly 10 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjtRZVRPS1{NTFOwG0> M3P6fVQ5KGh? Mm\TbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> NVjNcpdCOjV5OEiyOlk>
Oci Ly 1 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX61MVI2KM7:TR?= M1\0VlQ5KGh? M{H2[4lvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> NEPXfWIzPTd6OEK2PS=>
Oci Ly 18 MnLIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX61MVI2KM7:TR?= NYTWcGFnPDhiaB?= Ml\HbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> NGXjW5UzPTd6OEK2PS=>
Oci Ly 19  M3Oy[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PQWFUuOjVizszN M{HaTVQ5KGh? NH25bWJqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NYLWOG94OjV5OEiyOlk>
Raji MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYG1MVI2KM7:TR?= NFuxVFQ1QCCq NGm5Z2RqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NIfOb20zPTd6OEK2PS=>
H1299 NGCwUGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTP[GRwOS93L{GwJO69VQ>? NV\6RnliPzJiaB?= MmGxbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> NGfZOXIzPTd3MEOwPC=>
Calu-1  NUS5cWxMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mkn1NU82NzFyIN88US=> NGfLXIw4OiCq M2LxVIlvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> M2S0OFI2PzVyM{C4
H358 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPKTYsyNzVxMUCg{txO M1TW[|czKGh? NUnXfFc{cW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? MUKyOVc2ODNyOB?=
H1299 MmrRRZBweHSxc3nzJGF{e2G7 MmqyNVAh|ryP MnzCO|IhcA>? Ml\IbY5lfWOnczDhdI9xfG:|aYO= MWWyOVc2ODNyOB?=
Calu-1  MYjBdI9xfG:|aYOgRZN{[Xl? MnO3NVAh|ryP M13URlczKGh? NYXwdFdxcW6mdXPld{BieG:ydH;zbZM> MWqyOVc2ODNyOB?=
H358 NGO1UppCeG:ydH;zbZMhSXO|YYm= NETLVYkyOCEQvF2= MYG3NkBp M2TvXIlv\HWlZYOgZZBweHSxc3nz MYSyOVc2ODNyOB?=
PC9/GR Mn\pSpVv[3Srb36gRZN{[Xl? MWi1JOK2VQ>? M4[2NVQ5KGh? MU\pcoR2[2W|IHH1eI9xcGGpeR?= NFHiSnYzPTR6NkSwPS=>
PC9/ER MXzGeY5kfGmxbjDBd5NigQ>? MXW1JOK2VQ>? M1HBXlQ5KGh? NUj5Z4R1cW6mdXPld{BifXSxcHjh[5k> MXeyOVQ5PjRyOR?=
H28 NVfHRok6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\xVIMxNjBzLUOwJO69VQ>? M{jkO|czKGh? NVfrW4hlTE2VTx?= M3WycGlEPTB;Nz6yJO69VQ>? MmfJNlU1OjJyOEG=
H2052 NELJeYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3K5clAvODFvM{Cg{txO MkG5O|IhcA>? M3LOV2ROW09? M4DDXGlEPTB;Mj6wJO69VQ>? MkP6NlU1OjJyOEG=
UM-SCC-1 MlPTR4xwdm:pZX7pZ{BCe3OjeR?= MXuwMlUuPSEQvF2= NFfpfoYyPCCm NIey[2ZFVVOR MoL2xsBqdmirYnn0d{BkdG:wb3flcolkKHO3co\peoFtKGGwZDDzdIhmemViZn;ycYF1cW:w NU\le5piOjV|N{mwNVY>
UM-SCC-46 M3LZdGNtd26xZ3XubYMhSXO|YYm= NHWzOYIxNjVvNTFOwG0> Ml7INVQh\A>? MYrEUXNQ MkWxxsBqdmirYnn0d{BkdG:wb3flcolkKHO3co\peoFtKGGwZDDzdIhmemViZn;ycYF1cW:w NWr0ZlZIOjV|N{mwNVY>
U87-MG MoDCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\JcVcyNzVxMUCg{txO NIr1emQzPC92OD:3NkBp NH7X[VNFVVOR NYLLWFlucW6qaXLpeJMh[2WubDDndo94fGhiYn;0bEBkd26lZX70doF1cW:wIHHu[EB1cW2nIHTldIVv\GWwdHz5 NUL0eJlZOjV{NEG4PVc>
MDA-MB-231 MWXGeY5kfGmxbjDBd5NigQ>? MmXBNk82NzFyIN88US=> NG\keoo1KGh? M1TzdoRm[3KnYYPld{B1cGViY3;ud5RqfHW2aY\lJJBpd3OyaH;yfYxifGmxbjDv[kBjd3SqIDDwMXM2OjlvcE[1JIFv\CCyLWOxNlkuSWu2 Mmn6NlUyPTN5MkW=
MDA-MB-231 Mm\QSpVv[3Srb36gRZN{[Xl? NWXFRXNLOi93L{GwJO69VQ>? MljZOEBp NHPTZVRqdmirYnn0d{B{\XKrbnWgOVI6KHCqb4PwbI9zgWyjdHnvckBidmRidHjlJIV5eHKnc4Ppc44hd2ZiSVytOkwhUUxvOB?= MX[yOVE2Ozd{NR?=
ARPE-19 MmS3T4lv[XOnIFHzd4F6 MXG1M|ExNzJyIN88US=> MojDNlQwPDhiaB?= MVPpcohq[mm2czDDT|Ihc2mwYYPlJIFkfGm4aYT5JIF1KGFiY3;uZ4VvfHKjdHnvckBw\iB3wrFOwG0> NETtNlMzPDZ6NkC4NC=>
ARPE-19 MmLRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVGxNEDPxE1? NHHqN2EzPC17NjDo MnHISG1UVw>? NWDXbo9WcW6qaXLpeJMh[2WubDDndo94fGhidHnt[UBl\XCnbnTlcpRtgQ>? M{nB[|I1Pjh4MEiw
HCT116  MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFX3OVIyOCEQvF2= NV;BOm5UOjRvOU[gbC=> MVHEUXNQ MorrbY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> MlfvNlQ3QDZyOEC=
ARPE-19 M4PH[GZ2dmO2aX;uJGF{e2G7 MWexNEDPxE1? M{XWfVQhcA>? NFLjSFdFVVOR MU\jZZV{\XNiRWKtd5Rz\XO|IILld5BwdnOnIH;2[ZIhfGinIICt[WlHOs7zIHLyZY5kcCxiYoX0JIRw\XNibn;0JIlv\HWlZTDDTG9RyqB? MkC3NlQ3QDZyOEC=
HCT116  MkHrSpVv[3Srb36gRZN{[Xl? NHz1VI0yOCEQvF2= NXHMeHQ4PCCq Ml7OSG1UVw>? M{nwRYNifXOnczDFVk1{fHKnc4OgdoV{eG:wc3Wgc5ZmeiC2aHWgdE1mUUZ{zsGgZpJidmOqLDDieZQh\G:nczDuc5QhcW6mdXPlJGNJV1EEoB?= MkeyNlQ3QDZyOEC=
HCT116  MVTBdI9xfG:|aYOgRZN{[Xl? NHW5RYYyOCEQvF2= MonmNlQwPDhiaB?= NGr4ZYNFVVOR NXv6WZlScW6mdXPld{BieG:ydH;zbZM> MkfCNlQ3QDZyOEC=
Nalm6  MXnGeY5kfGmxbjDBd5NigQ>? NWDYW3pDOTBxMkCg{txO MVWyOEBp MXny[ZN2dHS|IHnuJIRm[3KnYYPl[EBRXEWQIIDoc5NxcG:{eXzheIlwdiCjdDD0bIUhS0t{IIThdodmfCC{ZYPp[JVmKFN|OECgZY5lKGOxbnPvcYl1[W62IHTve45z\We3bHH0bY9vKG:oIGDUSW4heHKxdHXpckBmgHC{ZYPzbY9v NYK2XVV3OjR3NkG3PVI>
SUP-B15 MWHGeY5kfGmxbjDBd5NigQ>? NWXNNYdHOTBxMkCg{txO NXTHWINKOjRiaB?= M{\N[pJme3WudIOgbY4h\GWlcnXhd4VlKFCWRV6gdIhwe3Cqb4L5cIF1cW:wIHH0JJRp\SCFS{KgeIFz\2W2IILld4llfWViU{O4NEBidmRiY3;uZ49ucXSjboSg[I94dnKnZ4XsZZRqd25ib3[gVHRGViCycn;0[YlvKGW6cILld5Nqd25? NIC3b|AzPDV4MUe5Ni=>
Nalm6  NXf1[XdkSXCxcITvd4l{KEG|c3H5 NXS5cW1TPi9zMDFOwG0> MnKwOFghcA>? NXvyTGhLcW6mdXPld{BieG:ydH;zbZM> NImxdIszPDV4MUe5Ni=>
SUP-B15 NWCyeG1zSXCxcITvd4l{KEG|c3H5 M{LZVFYwOTBizszN MknuOFghcA>? M2X2colv\HWlZYOgZZBweHSxc3nz MmrhNlQ2PjF5OUK=
C2C12 M364fWZ2dmO2aX;uJGF{e2G7 NUHHXpZ7OyEQvF2= M4XpbFEzNzJ2L{S4JIg> M{PGTolvcGmkaYTzJJRp\SCneIDy[ZN{cW:wIH;mJI9{fGWxY3zhd5Qh\GmoZnXy[Y51cWG2aX;uJI1iemuncoOgZY5lKEGtdDDwbI9{eGixconsZZRqd25? Ml72NlQzQTNyMUG=
Jurkat MmniS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHhe3c5OS1zMDFOwG0> MVK0PEBp M1nuZ2lEPTB;ND65JO69VQ>? NWPKUWUxOjR{NUOwNlQ>
CEM-R M1rXUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLxNU0yOCEQvF2= NFvRVYM1QCCq NWLXZ415UUN3ME20JO69VQ>? NF71bXgzPDJ3M{CyOC=>
CEM-S MoTCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\kbpJpOS1zMDFOwG0> MUK0PEBp M3fmSGlEPTB;ND62JO69VQ>? M2HxS|I1OjV|MEK0
MOLT-4 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPwNU0yOCEQvF2= M3nF[FQ5KGh? M4rlPGlEPTB;NT63JO69VQ>? NHu1TJAzPDJ3M{CyOC=>
PF-382 MoftS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\lOXBUOS1zMDFOwG0> MonlOFghcA>? NWLYPWo5UUN3ME20MlUh|ryP Mme1NlQzPTNyMkS=
ALL-SIL NF;j[JNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTiVo1TOS1zMDFOwG0> NEizdXI1QCCq NGXwVoxKSzVyPUWuO{DPxE1? NHj2RmYzPDJ3M{CyOC=>
HPB-ALL MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\Id5dvOS1zMDFOwG0> NGTSfGk1QCCq NYn3ZZU4UUN3ME22MlEh|ryP MYOyOFI2OzB{NB?=
DND-41 NFG5cZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\yOJkyOS1zMDFOwG0> NXK2eWJbPDhiaB?= M2PnUmlEPTB;OTFOwG0> NHPscGkzPDJ3M{CyOC=>
ALL-SIL M3rkcWFxd3C2b4Ppd{BCe3OjeR?= MlSwOUDPxE1? NGfheYczPC92ODDo NFXw[otqdmS3Y3XzJIFxd3C2b4Ppdy=> NVfrT4FTOjR{NUOwNlQ>
DND-41 MWfBdI9xfG:|aYOgRZN{[Xl? NX3jWWZJPSEQvF2= MUGyOE81QCCq Ml35bY5lfWOnczDhdI9xfG:|aYO= M{ja[|I1OjV|MEK0
MOLT-4 NYC5VHI{SXCxcITvd4l{KEG|c3H5 MmHkOUDPxE1? MX2yOE81QCCq MmDDbY5lfWOnczDhdI9xfG:|aYO= NETaXXIzPDJ3M{CyOC=>
U-266 MoHiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;uVIIxNTRyIN88US=> MYK0PEBp MV\JR|UxRTF7LkigxtVOyqB? MWGyOFA5PjR7NB?=
INA-6 M1;rOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV[wMVQxKM7:TR?= NGrweW41QCCq NGC4NHhKSzVyPUKuOFIhyrWP NV\BV4NyOjRyOE[0PVQ>
Jeko-1 MlnxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVe5OpV[OC12MDFOwG0> MoDoOFghcA>? NGXyT|lKSzVyPUKuOEDDvU4EoB?= MnL1NlQxQDZ2OUS=
Rec-1 M{TNcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fFW|AuPDBizszN M{K2XFQ5KGh? MoLoTWM2OD1zLkS2JOK2VcLi MUKyOFA5PjR7NB?=
A549 NUPDNWczTnWwY4Tpc44hSXO|YYm= NXLkVGhROTBizszN M{HNdFEzNzJ2L{S4JIg> NWDDXXhCcW6qaXLpeJMhXEeILd8yNU1qdmS3Y3XkJI1q\3KjdHnvckBidmRiaX72ZZNqd25? M3jiOFI1ODJ|OUO4
A549 MkDDSpVv[3Srb36gRZN{[Xl? MXuzJO69VQ>? NGPqVlk1QCCq NETKfG1qdmirYnn0d{BVT0ZvzsKxMYlv\HWlZXSgZYN1cX[jdHnvckBw\iCVbXHkJIFv\CCneIDy[ZN{cW:wIH;mJHNv[WmuIHHu[EBVf2m|dB?= Ml7YNlQxOjN7M{i=
S-LAMA84 MnfHSpVv[3Srb36gRZN{[Xl? NEPzZ3Y{yqEQvF2= MXKyOEBp MlHBSG1UVw>? NYOyfGI5emWmdXPld{BEUzJiYXP0bZZqfHl? MWeyOFAyOjFyOR?=
R-LAMA84 MnHmSpVv[3Srb36gRZN{[Xl? NWTEVFF1O8LizszN M4HWc|I1KGh? NFznbXlFVVOR NHXHNIlz\WS3Y3XzJGNMOiCjY4Tpeol1gQ>? MorHNlQxOTJzMEm=
S-LAMA84 MmqxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUG2emRnOi53LUGwJO69VQ>? MX20PEBp MkPDSG1UVw>? MXrpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 NED5O5ozPDBzMkGwPS=>
R-LAMA84 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTuNk42NTFyIN88US=> NEe3R5A1QCCq NX7aZmU2TE2VTx?= Mn7vbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> NGm0ZYEzPDBzMkGwPS=>
A549 NHi0b3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\sd|AuOzBizszN MmrtO|IhcA>? NVzKeG1NTE2VTx?= MYnJR|UxRTRwMUWg{txONCCrbnjpZol1eyClZXzsJIdzd3e2aDDjc45k\W62cnH0bY9vKGSncHXu[IVvfGy7 MnnONlM3PTF2NEO=
H1299 Ml;2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPoNE0{OCEQvF2= M4PlWVczKGh? MY\EUXNQ M3rZW2lEPTB;MT64NEDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJINwdmOnboTyZZRqd25iZHXw[Y5l\W62bIm= NGnDdHczOzZ3MUS0Ny=>
A549 MY\GeY5kfGmxbjDBd5NigQ>? NXvGXY02OS9zMDFOwG0> MnP1OFghcA>? M4TnbGROW09? NYTW[WoydGWjZIOgeI8h[SCmb4PlMYRmeGWwZHXueEBl\WO{ZXHz[UBqdiCQb4TjbEBz\XCxcoTldkBi[3Srdnn0fS=> NYP0dpk2OjN4NUG0OFM>
LNCap Mn7OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7JdJJrOC1|MDFOwG0> MYm0JIQ> M{LxNmlEPTB;ND61PeKh|ryP NHfyRXAzOjh|MkOxOi=>
A431  NWG2XnVJTnWwY4Tpc44hSXO|YYm= NFLXdIYyOCEQvF2= NXqxW3NsOzBibXnu MYLheJRmdnWjdHXzJHBKO0tvQXv0MY1VV1Jic3nncoFtcW6p NWDreIpjOjJ|OEe5PFg>
H2170  M{K3b2Z2dmO2aX;uJGF{e2G7 M2j5TFExKM7:TR?= NXrNbmJYOzBibXnu NHjGVo9ifHSnboXheIV{KFCLM1utRYt1NW2WT2Kgd4lodmGuaX7n NX\icYxVOjJ|OEe5PFg>
A431  NFTBPYlHfW6ldHnvckBCe3OjeR?= M17SUFExKM7:TR?= NIrs[|A1NTJ2IHi= MoW5[Y5p[W6lZYOgZZBweHSxc3nzJJdqfGhiZYLsc5Rqdmmk Mmr3NlI{QDd7OEi=
H2170  NYXu[mZQTnWwY4Tpc44hSXO|YYm= NGfjcGEyOCEQvF2= MV:0MVI1KGh? M4qwZYVvcGGwY3XzJIFxd3C2b4Ppd{B4cXSqIHXycI91cW6rYh?= MW[yNlM5Pzl6OB?=

... 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:
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
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):
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    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
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    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|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.

  • * 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