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 Mk\HT4lv[XOnIFHzd4F6 NHvnbFAyNzVxMUCg{txO MViwMlUhcA>? NWS2XnNJTE2VTx?= MVjy[YR2[2W|IFPLNkBscW6jc3WgZYN1cX[rdImgZY5lKHCuYYTlcIV1KGGpZ4Ll[4F1cW:w Mn\JNlY{QDF2M{e=
HDMEC M2\KSWtqdmG|ZTDBd5NigQ>? M{HCWFAvOjVxMD61M|Eh|ryP NGfS[VMzPCCq M4Pn[mROW09? NFrybJlz\WS3Y3XzJGNMOiCtaX7hd4Uh[WO2aY\peJktKH[ZRjDlfJBz\XO|aX;uJIFv\CC|ZXPy[ZRqd25? NIfveYUzPjN6MUSzOy=>
HDMEC M4e1cmZ2dmO2aX;uJGF{e2G7 NWX6fJZJOC5{NT:wMlUwOSEQvF2= NVrDNYF2OjRiaB?= NIPjUWZFVVOR MYXy[YR2[2W|IHX4dJJme3Orb36gc4YhXkODTT2xJIJ2fCCwb4SgTWNCVS1z M3TWRVI3OzhzNEO3
HDMEC MWfGeY5kfGmxbjDBd5NigQ>? MUCxJO69VQ>? M1nHSFI1KGh? MUjEUXNQ MlvUZYZn\WO2czDzeYJk\WyudXzhdkBtd2OjbHn6ZZRqd25ib3[gUmZCXGNzIHHu[EBxcG:|cHjvMZA3PQ>? MY[yOlM5OTR|Nx?=
A549  NHvMfHFHfW6ldHnvckBCe3OjeR?= NHPE[5U{NzFywrFOwG0> MliyOFghcA>? NHvITFV{fXCycnXzd4V{KHSqZTDtbYNzd3CrbHzhdk1qdmS3Y3XkJIV5eHKnc4Ppc44hd2ZicD3GRWs> NVnmZ3h3OjZ|MUi4NFA>
HDMEC MWLLbY5ie2ViQYPzZZk> NIqxbHEyNTVyIN88US=> M4HTe|UhcA>? NWfBXml1TE2VTx?= M4TnNoRm[3KnYYPld{BEUzJia3nuZZNmKGGldHn2bZR6KHerdHjveZQh[W[oZXP0bY5oKGOnbHygeoli[mmuaYT5 NYK4[Wo4OjZzOEm1PFY>
HDMEC MljlSpVv[3Srb36gRZN{[Xl? NIXTNG42OCEQvF2= NHjibYMyNzViaB?= M{KxfmROW09? M17VN4Rm[3KnYYPld{B1cGViboXjcIVieiC|aXfuZYwhd2ZicHjvd5Bpd3K7bHH0[YQheDZ3IHnuJHRPTi4QsT3zeIlufWyjdHXkJGhFVUWFwrC= NXH5[mE{OjZzOEm1PFY>
HEK293 MY\LbY5ie2ViQYPzZZk> NHj2Ro0xNjYEoN88US=> MXuxOUBucW5? M1zyO2ROW09? NGDPb5pz\WS3Y3XzJGNMOiCtaX7hd4Uh[WO2aY\peJk> NIKx[|YzPTh6N{[yOi=>
Hela Mn\BT4lv[XOnIFHzd4F6 NIWwTGYxNjYEoN88US=> MnLWNVUhdWmw Ml\ISG1UVw>? NUj2cmN2emWmdXPld{BEUzJia3nuZZNmKGGldHn2bZR6 M3nTeVI2QDh5NkK2
LAMA84 MmHHT4lv[XOnIFHzd4F6 NYfNNG5MOC53wrFOwG0> MWSxOUBucW5? M3vkVGROW09? NWPjVWxKemWmdXPld{BEUzJia3nuZZNmKGGldHn2bZR6 NWn6VGI1OjV6OEe2NlY>
HEK293 NEjpVopHfW6ldHnvckBCe3OjeR?= NITxSXU{KM7:TR?= MonuOUBp NIO4bWlFVVOR MWTDT|IheGixc4Doc5J6dGG2ZYOg[WlHO2piYYSgV4VzOTJ5 NGexOYkzPTh6N{[yOi=>
UM-SCC1 NGHC[Y1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWfrW5ZtOC5zLUOwJO69VQ>? NH\RO2kyNTViZB?= MXPJR|UxRTRwMTFOwG0> MVeyOVc6QDB4MR?=
UM-SCC46 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGr6OXUxNjFvM{Cg{txO MXexMVUh\A>? M1LDWWlEPTB;Mz60JO69VQ>? MViyOVc6QDB4MR?=
UM-SCC1 MYjGeY5kfGmxbjDBd5NigQ>? NXT6cm91OC53L{SvNVAh|ryP MX[3NkBp NX3qT4dR\G:5bj3y[Yd2dGG2ZYOgeIhmKGW6cILld5Nqd25ib3[gUmYuzLiELDDCZ4wuYExiYX7kJJVxNXKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCyNUOsJJAzOSxiQWCtNUBidmRiSVytPEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 NWO5[W9uOjV5OUiwOlE>
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NU-DUL MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2C4OlUuOjVizszN MW[0PEBp MYPpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 NWrtdJd2OjV5OEiyOlk>
Oci Ly 3 M1j3WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2[yb|UuOjVizszN NHHwSVM1QCCq MlnVbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> M13TelI2Pzh6Mk[5
Oci Ly 10 NUTaVINbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfQcmRRPS1{NTFOwG0> MkLSOFghcA>? MlvGbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> MUSyOVc5QDJ4OR?=
Oci Ly 1 NXvWVmROT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPCdlA2NTJ3IN88US=> NHT1bnk1QCCq MljBbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> NHXaR5QzPTd6OEK2PS=>
Oci Ly 18 M{TUVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPYOU0zPSEQvF2= MW[0PEBp NIjv[GFqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 M2G2dlI2Pzh6Mk[5
Oci Ly 19  MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PwbFUuOjVizszN NI\YS2k1QCCq NHfmOWtqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 MXKyOVc5QDJ4OR?=
Raji NX3JdFJTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\uNGF3PS1{NTFOwG0> MnH3OFghcA>? M3K5dolvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> NGj6U2EzPTd6OEK2PS=>
H1299 NXH6VINuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPkU5F1OS93L{GwJO69VQ>? NH7rRXk4OiCq Mki0bY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> Mn3HNlU4PTB|MEi=
Calu-1  MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYSxM|UwOTBizszN M{SzOlczKGh? M1vvZYlvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> MUiyOVc2ODNyOB?=
H358 NInJRWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{LJUlEwPS9zMDFOwG0> MXK3NkBp MkLjbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> MVeyOVc2ODNyOB?=
H1299 MknDRZBweHSxc3nzJGF{e2G7 NXHL[ohQOTBizszN MWq3NkBp NYLsV5VVcW6mdXPld{BieG:ydH;zbZM> NWXjb|dkOjV5NUCzNFg>
Calu-1  MWLBdI9xfG:|aYOgRZN{[Xl? NYHCZmEyOTBizszN MnHkO|IhcA>? MWnpcoR2[2W|IHHwc5B1d3Orcx?= MWWyOVc2ODNyOB?=
H358 MV7BdI9xfG:|aYOgRZN{[Xl? NH3OfmgyOCEQvF2= NH7ueHk4OiCq MVLpcoR2[2W|IHHwc5B1d3Orcx?= MXuyOVc2ODNyOB?=
PC9/GR MnuwSpVv[3Srb36gRZN{[Xl? M3[1U|UhyrWP MX[0PEBp MXHpcoR2[2W|IHH1eI9xcGGpeR?= Mm\hNlU1QDZ2MEm=
PC9/ER NV3pNJBJTnWwY4Tpc44hSXO|YYm= M1\TdlUhyrWP M4r4VFQ5KGh? MYnpcoR2[2W|IHH1eI9xcGGpeR?= NXjRSWxDOjV2OE[0NFk>
H28 MmPUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LMSVAvODFvM{Cg{txO MWC3NkBp NXXhc3Y{TE2VTx?= M1HtRWlEPTB;Nz6yJO69VQ>? M1TvWFI2PDJ{MEix
H2052 NHfES|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHUNE4xOS1|MDFOwG0> NVHsdmc{PzJiaB?= MYfEUXNQ M3PISmlEPTB;Mj6wJO69VQ>? MWWyOVQzOjB6MR?=
UM-SCC-1 MlHHR4xwdm:pZX7pZ{BCe3OjeR?= MWOwMlUuPSEQvF2= NIX1[ZMyPCCm M{nQV2ROW09? MVpCpIlvcGmkaYTzJINtd26xZ3XubYMhe3W{dnn2ZYwh[W6mIIPwbIVz\SCob4LtZZRqd25? MnHENlU{PzlyMU[=
UM-SCC-46 Ml3iR4xwdm:pZX7pZ{BCe3OjeR?= MnzzNE42NTVizszN NFK4fpMyPCCm NEfEc5dFVVOR Mm\TxsBqdmirYnn0d{BkdG:wb3flcolkKHO3co\peoFtKGGwZDDzdIhmemViZn;ycYF1cW:w NVPFZWtPOjV|N{mwNVY>
U87-MG M3PnWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\Efm4{OS93L{GwJO69VQ>? NWXvOpBxOjRxNEivO|IhcA>? MYjEUXNQ M3HNWolvcGmkaYTzJINmdGxiZ4Lve5RpKGKxdHigZ49v[2WwdILheIlwdiCjbnSgeIlu\SCmZYDlcoRmdnSueR?= NVrPZYFGOjV{NEG4PVc>
MDA-MB-231 MVvGeY5kfGmxbjDBd5NigQ>? NESyTnozNzVxMUCg{txO NEf1cYo1KGh? NWTwTYVu\GWlcnXhd4V{KHSqZTDjc45{fGm2dYTpeoUheGixc4Doc5J6dGG2aX;uJI9nKGKxdHigJJAuWzV{OT3wOlUh[W6mIICtV|EzQS2Da4S= MlTiNlUyPTN5MkW=
MDA-MB-231 MlvqSpVv[3Srb36gRZN{[Xl? MVmyM|UwOTBizszN M3PEdVQhcA>? MVHpcohq[mm2czDz[ZJqdmViNUK5JJBpd3OyaH;yfYxifGmxbjDhcoQhfGinIHX4dJJme3Orb36gc4YhUUxvNjygTWwuQA>? MUSyOVE2Ozd{NR?=
ARPE-19 M4LwWGtqdmG|ZTDBd5NigQ>? NFTq[|U2NzFyL{KwJO69VQ>? MkfTNlQwPDhiaB?= NXjBVnJDcW6qaXLpeJMhS0t{IHvpcoF{\SCjY4Tpeol1gSCjdDDhJINwdmOnboTyZZRqd25ib3[gOeKh|ryP NGLyZ|QzPDZ6NkC4NC=>
ARPE-19 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV7BNFRCOTBizszN MWKyOE06PiCq MV7EUXNQ MkPqbY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> NULI[WF3OjR4OE[wPFA>
HCT116  NUT0TWtKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXhTYEyOCEQvF2= MmW2NlQuQTZiaB?= M4fXdWROW09? MlLLbY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> M1HHOFI1Pjh4MEiw
ARPE-19 NUHJdnZiTnWwY4Tpc44hSXO|YYm= MYexNEDPxE1? MYO0JIg> MV;EUXNQ NEGzUHhk[XW|ZYOgSXIue3S{ZYPzJJJme3CxboPlJI93\XJidHjlJJAu\UmIMt8xJIJz[W6laDygZpV1KGSxZYOgco91KGmwZIXj[UBEUE:SwrC= MXeyOFY5PjB6MB?=
HCT116  NUfyVXJTTnWwY4Tpc44hSXO|YYm= MlzuNVAh|ryP MXO0JIg> MWLEUXNQ MnHlZ4F2e2W|IFXSMZN1emW|czDy[ZNxd26|ZTDveoVzKHSqZTDwMYVKTjMQsTDidoFv[2huIHL1eEBld2W|IH7veEBqdmS3Y3WgR2hQWMLi MYOyOFY5PjB6MB?=
HCT116  MmHiRZBweHSxc3nzJGF{e2G7 Mn\RNVAh|ryP NIXlTGczPC92ODDo MXfEUXNQ M3j5b4lv\HWlZYOgZZBweHSxc3nz MVeyOFY5PjB6MB?=
Nalm6  NF;hN49HfW6ldHnvckBCe3OjeR?= MnzONVAwOjBizszN NHWwcWwzPCCq NX\HSm5CemW|dXz0d{BqdiCmZXPy[YF{\WRiUGTFUkBxcG:|cHjvdplt[XSrb36gZZQhfGinIFPLNkB1[XKpZYSgdoV{cWS3ZTDTN|gxKGGwZDDjc45kd22rdHHueEBld3ewcnXneYxifGmxbjDv[kBRXEWQIIDyc5RmcW5iZYjwdoV{e2mxbh?= NWLOR21lOjR3NkG3PVI>
SUP-B15 NXTMPG17TnWwY4Tpc44hSXO|YYm= MU[xNE8zOCEQvF2= NICwRoUzPCCq MV\y[ZN2dHS|IHnuJIRm[3KnYYPl[EBRXEWQIIDoc5NxcG:{eXzheIlwdiCjdDD0bIUhS0t{IIThdodmfCC{ZYPp[JVmKFN|OECgZY5lKGOxbnPvcYl1[W62IHTve45z\We3bHH0bY9vKG:oIGDUSW4heHKxdHXpckBmgHC{ZYPzbY9v MofZNlQ2PjF5OUK=
Nalm6  NYDzSFF5SXCxcITvd4l{KEG|c3H5 MljnOk8yOCEQvF2= M4HsWFQ5KGh? MU\pcoR2[2W|IHHwc5B1d3Orcx?= MX2yOFU3OTd7Mh?=
SUP-B15 M3zCR2Fxd3C2b4Ppd{BCe3OjeR?= M3TG[|YwOTBizszN NX61bmoyPDhiaB?= MlLubY5lfWOnczDhdI9xfG:|aYO= NEDNfWMzPDV4MUe5Ni=>
C2C12 NVLSc5dQTnWwY4Tpc44hSXO|YYm= MV6zJO69VQ>? NUnGeFRFOTJxMkSvOFghcA>? NYnhW5pZcW6qaXLpeJMhfGinIHX4dJJme3Orb36gc4Yhd3O2ZX;jcIF{fCCmaX\m[ZJmdnSrYYTpc44hdWG{a3Xyd{BidmRiQXv0JJBpd3OyaH;yfYxifGmxbh?= MVeyOFI6OzBzMR?=
Jurkat NEj6SZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmDxNU0yOCEQvF2= Ml\ROFghcA>? M2m3[2lEPTB;ND65JO69VQ>? MkPpNlQzPTNyMkS=
CEM-R MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjlc28yNTFyIN88US=> NVyzfHpUPDhiaB?= NYW2Wo1YUUN3ME20JO69VQ>? NVfLZYZ2OjR{NUOwNlQ>
CEM-S NXnHXG9LT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfJWJJuOS1zMDFOwG0> NYXoU4NqPDhiaB?= NH7ucZZKSzVyPUSuOkDPxE1? MW[yOFI2OzB{NB?=
MOLT-4 Mn\BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUmxMVExKM7:TR?= M3nKcVQ5KGh? MUPJR|UxRTVwNzFOwG0> M1XsPVI1OjV|MEK0
PF-382 NXPQbnM{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUGxMVExKM7:TR?= MYO0PEBp NVfablNOUUN3ME20MlUh|ryP NID5WVEzPDJ3M{CyOC=>
ALL-SIL NHfL[mxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\ne4RGOS1zMDFOwG0> NYPUOVFtPDhiaB?= M{j1VmlEPTB;NT63JO69VQ>? MlrVNlQzPTNyMkS=
HPB-ALL NHznZWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXkS|lPOS1zMDFOwG0> M3HYZlQ5KGh? MkWyTWM2OD14LkGg{txO NETCSpozPDJ3M{CyOC=>
DND-41 MlS4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHL5TVgyNTFyIN88US=> MnXVOFghcA>? NHHmTHpKSzVyPUmg{txO NYPVUYpYOjR{NUOwNlQ>
ALL-SIL MVTBdI9xfG:|aYOgRZN{[Xl? NGr5b4Q2KM7:TR?= NHG2PXUzPC92ODDo MmH2bY5lfWOnczDhdI9xfG:|aYO= M4G1W|I1OjV|MEK0
DND-41 MnzXRZBweHSxc3nzJGF{e2G7 NFrKT482KM7:TR?= NFn1U3EzPC92ODDo NWP3[IM{cW6mdXPld{BieG:ydH;zbZM> M4fLVFI1OjV|MEK0
MOLT-4 MV\BdI9xfG:|aYOgRZN{[Xl? NHXFV2I2KM7:TR?= NEHaeoEzPC92ODDo MkTKbY5lfWOnczDhdI9xfG:|aYO= NInG[3EzPDJ3M{CyOC=>
U-266 M2nk[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmG0NE01OCEQvF2= MkTIOFghcA>? MkTQTWM2OD1zOT64JOK2VcLi NVvlcW5wOjRyOE[0PVQ>
INA-6 NH\QNIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUj2SJRXOC12MDFOwG0> MmXaOFghcA>? M3PofGlEPTB;Mj60NkDDvU1? NFzZcWIzPDB6NkS5OC=>
Jeko-1 MoDkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYiwMVQxKM7:TR?= NFTibm41QCCq MkXWTWM2OD1{LkSgxtVOyqB? MlXLNlQxQDZ2OUS=
Rec-1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfuUlZlOC12MDFOwG0> M4rsZlQ5KGh? NITnd2VKSzVyPUGuOFYhyrWPwrC= M{iwUFI1ODh4NEm0
A549 MmK2SpVv[3Srb36gRZN{[Xl? NFfzRY0yOCEQvF2= MVqxNk8zPC92ODDo NGjyWpRqdmirYnn0d{BVT0ZvzsKxMYlv\HWlZXSgcYloemG2aX;uJIFv\CCrbo\hd4lwdg>? MXeyOFAzOzl|OB?=
A549 MkT3SpVv[3Srb36gRZN{[Xl? MlXQN{DPxE1? MYG0PEBp NV[xNWJRcW6qaXLpeJMhXEeILd8yNU1qdmS3Y3XkJIFkfGm4YYTpc44hd2ZiU33h[EBidmRiZYjwdoV{e2mxbjDv[kBUdmGrbDDhcoQhXHerc4S= M4H1[|I1ODJ|OUO4
S-LAMA84 MV\GeY5kfGmxbjDBd5NigQ>? NXLqXm9vO8LizszN MUCyOEBp MUjEUXNQ MknXdoVlfWOnczDDT|Ih[WO2aY\peJk> NHrIRVUzPDBzMkGwPS=>
R-LAMA84 NXOzcWZqTnWwY4Tpc44hSXO|YYm= MnfzN:Kh|ryP M4HuNlI1KGh? NYDGcnZqTE2VTx?= M3W1eZJm\HWlZYOgR2szKGGldHn2bZR6 NIHJbmgzPDBzMkGwPS=>
S-LAMA84 NXvGNVVnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjONk42NTFyIN88US=> NGXL[JE1QCCq MlHnSG1UVw>? NHWxPHpqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 MXKyOFAyOjFyOR?=
R-LAMA84 NUTvRppsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVT1Wph4Oi53LUGwJO69VQ>? MmDKOFghcA>? M{XMemROW09? MVTpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 NWX1U|BuOjRyMUKxNFk>
A549 MnfDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\jPFAuOzBizszN NGqzfW84OiCq MVnEUXNQ NXn1N3BkUUN3ME20MlE2KM7:TTygbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> MkfnNlM3PTF2NEO=
H1299 M33WZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jtbVAuOzBizszN NHy0UVU4OiCq MlfjSG1UVw>? MmLYTWM2OD1zLkiwJO69VSxiaX7obYJqfHNiY3XscEBoem:5dHigZ49v[2WwdILheIlwdiCmZYDlcoRmdnSueR?= M{SxV|I{PjVzNESz
A549 M3;zOGZ2dmO2aX;uJGF{e2G7 MXmxM|ExKM7:TR?= MVi0PEBp NUXrdWw{TE2VTx?= Mlv3cIVi\HNidH:gZUBld3OnLXTldIVv\GWwdDDk[YNz\WG|ZTDpckBPd3SlaDDy[ZBwenSncjDhZ5Rqfmm2eR?= M{PzNVI{PjVzNESz
LNCap NWjpdWo5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEfIcJUxNTNyIN88US=> M1XOflQh\A>? NHjBbWtKSzVyPUSuOVnDqM7:TR?= MnG0NlI5OzJ|MU[=
A431  MoLDSpVv[3Srb36gRZN{[Xl? NFPhOW4yOCEQvF2= MUWzNEBucW5? MXfheJRmdnWjdHXzJHBKO0tvQXv0MY1VV1Jic3nncoFtcW6p NVXKSJBNOjJ|OEe5PFg>
H2170  NIfz[3JHfW6ldHnvckBCe3OjeR?= NGXQbYkyOCEQvF2= MX:zNEBucW5? NHzhdZJifHSnboXheIV{KFCLM1utRYt1NW2WT2Kgd4lodmGuaX7n NG\McnozOjN6N{m4PC=>
A431  NF3Je4pHfW6ldHnvckBCe3OjeR?= M{LZelExKM7:TR?= MYS0MVI1KGh? MUXlcohidmOnczDhdI9xfG:|aYOge4l1cCCncnzveIlvcWJ? NIr4W2wzOjN6N{m4PC=>
H2170  MonkSpVv[3Srb36gRZN{[Xl? Ml72NVAh|ryP NGLhUII1NTJ2IHi= NHTz[lZmdmijbnPld{BieG:ydH;zbZMhf2m2aDDldoxwfGmwaXK= MnixNlI{QDd7OEi=

... 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).

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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