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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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 MX\LbY5ie2ViQYPzZZk> MWGxM|UwOTBizszN MmPZNE42KGh? MkHFSG1UVw>? MlzXdoVlfWOnczDDT|Ihc2mwYYPlJIFkfGm4aYT5JIFv\CCybHH0[YxmfCCjZ3fy[YdifGmxbh?= MWqyOlM5OTR|Nx?=
HDMEC NFi1U2JMcW6jc3WgRZN{[Xl? MWmwMlI2NzBwNT:xJO69VQ>? M4TtW|I1KGh? NI\X[G9FVVOR NX;ZSJBMemWmdXPld{BEUzJia3nuZZNmKGGldHn2bZR6NCC4V1[g[ZhxemW|c3nvckBidmRic3XjdoV1cW:w M3HiWVI3OzhzNEO3
HDMEC MV7GeY5kfGmxbjDBd5NigQ>? MkPYNE4zPS9yLkWvNUDPxE1? M{TNWFI1KGh? NVrPW5BLTE2VTx?= NFHmXIlz\WS3Y3XzJIV5eHKnc4Ppc44hd2ZiVlPBUU0yKGK3dDDuc5QhUUODTT2x M3OyN|I3OzhzNEO3
HDMEC MWnGeY5kfGmxbjDBd5NigQ>? NWnibWZzOSEQvF2= MnvtNlQhcA>? M1fEWmROW09? MYTh[oZm[3S|IIP1ZoNmdGy3bHHyJIxw[2GuaYrheIlwdiCxZjDOSmFV[zFiYX7kJJBpd3OyaH:tdFY2 Ml3DNlY{QDF2M{e=
A549  M1;xN2Z2dmO2aX;uJGF{e2G7 NYLndpRJOy9zMNMg{txO MkfhOFghcA>? NUfsdmNEe3WycILld5NmeyC2aHWgcYlkem:yaXzsZZIucW6mdXPl[EBmgHC{ZYPzbY9vKG:oIICtSmFM MVuyOlMyQDhyMB?=
HDMEC NV;G[mFpU2mwYYPlJGF{e2G7 MV2xMVUxKM7:TR?= NVXmcpVbPSCq MojsSG1UVw>? NFr5WlJl\WO{ZXHz[ZMhS0t{IHvpcoF{\SCjY4Tpeol1gSC5aYToc5V1KGGoZnXjeIlv\yClZXzsJJZq[WKrbHn0fS=> MXSyOlE5QTV6Nh?=
HDMEC NVrBOYx2TnWwY4Tpc44hSXO|YYm= NGLZW4Q2OCEQvF2= NIXGfmUyNzViaB?= NY\RVJdSTE2VTx?= M3rGPYRm[3KnYYPld{B1cGViboXjcIVieiC|aXfuZYwhd2ZicHjvd5Bpd3K7bHH0[YQheDZ3IHnuJHRPTi4QsT3zeIlufWyjdHXkJGhFVUWFwrC= MWiyOlE5QTV6Nh?=
HEK293 NWnqNY12U2mwYYPlJGF{e2G7 MomzNE42yqEQvF2= MoHtNVUhdWmw NF3qT21FVVOR MV\y[YR2[2W|IFPLNkBscW6jc3WgZYN1cX[rdIm= NILy[3YzPTh6N{[yOi=>
Hela MULLbY5ie2ViQYPzZZk> MVuwMlXDqM7:TR?= Mni4NVUhdWmw MlyySG1UVw>? MX7y[YR2[2W|IFPLNkBscW6jc3WgZYN1cX[rdIm= MmmzNlU5QDd4Mk[=
LAMA84 MojJT4lv[XOnIFHzd4F6 NELzNI0xNjYEoN88US=> Ml3FNVUhdWmw M4D1TGROW09? NFHGSGRz\WS3Y3XzJGNMOiCtaX7hd4Uh[WO2aY\peJk> NG\yXIIzPTh6N{[yOi=>
HEK293 MV3GeY5kfGmxbjDBd5NigQ>? M4XhTFMh|ryP M{P1fFUhcA>? M2q4d2ROW09? Mm\HR2szKHCqb4PwbI9zgWyjdHXzJIVKTjOsIHH0JHNmejF{Nx?= NGnXbZQzPTh6N{[yOi=>
UM-SCC1 MoLhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlf1NE4yNTNyIN88US=> MV[xMVUh\A>? NFzuNIRKSzVyPUSuNUDPxE1? NU[zSlJ3OjV5OUiwOlE>
UM-SCC46 NFLWNGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\oNE4yNTNyIN88US=> MYixMVUh\A>? NGPIUVlKSzVyPUOuOEDPxE1? Ml[4NlU4QThyNkG=
UM-SCC1 NYrMVmZsTnWwY4Tpc44hSXO|YYm= MkHJNE42NzRxMUCg{txO MnLyO|IhcA>? NWL6OFd4\G:5bj3y[Yd2dGG2ZYOgeIhmKGW6cILld5Nqd25ib3[gUmYuzLiELDDCZ4wuYExiYX7kJJVxNXKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCyNUOsJJAzOSxiQWCtNUBidmRiSVytPEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 NHyxeo0zPTd7OEC2NS=>
UM-SCC46 NHvlZ|hHfW6ldHnvckBCe3OjeR?= NIHPWmYxNjVxND:xNEDPxE1? MmG5O|IhcA>? MYTkc5dvNXKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCQRj5EvGItKEKlbD3YUEwheDV|LDDwNlEtKEGSLUGgZY5lKHWyLYLl[5Vt[XSnczD0bIUh\XiycnXzd4lwdiCLTD24JINwdmOnboTyZZRqd25iZHXw[Y5l\W62bIm= MYqyOVc6QDB4MR?=
NU-DUL NWHDeHpvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUS1MVI2KM7:TR?= MXm0PEBp NGrjVHJqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 M1zoeFI2Pzh6Mk[5
Oci Ly 3 M2S2Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nkT|UuOjVizszN M3e4W|Q5KGh? NYP4TmdScW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? M3nINVI2Pzh6Mk[5
Oci Ly 10 Mn;DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkDlOU0zPSEQvF2= M1rEZlQ5KGh? MlTwbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> NGm0blEzPTd6OEK2PS=>
Oci Ly 1 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXm1MVI2KM7:TR?= NHTYbZA1QCCq M3fzbIlvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> MX:yOVc5QDJ4OR?=
Oci Ly 18 Ml3nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWLKW2ZFPS1{NTFOwG0> NWP4T2ZNPDhiaB?= NHzHPINqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 MUeyOVc5QDJ4OR?=
Oci Ly 19  NF;0UJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2noPVUuOjVizszN M3TYWlQ5KGh? Mnj1bY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> Ml\vNlU4QDh{Nkm=
Raji M3zBcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fBVVUuOjVizszN M1;wOlQ5KGh? M{jvS4lvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> M2q1N|I2Pzh6Mk[5
H1299 NYCxe2NOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHENU82NzFyIN88US=> MVu3NkBp M13wOolvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> MWGyOVc2ODNyOB?=
Calu-1  M3TxXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVKxM|UwOTBizszN NXHVeVF1PzJiaB?= M{\TVYlvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> Mm\CNlU4PTB|MEi=
H358 NIHIWYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7IOotUOS93L{GwJO69VQ>? NIrKeWQ4OiCq M4HSeolvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> MXKyOVc2ODNyOB?=
H1299 M1TjS2Fxd3C2b4Ppd{BCe3OjeR?= NEnsbZUyOCEQvF2= NWT2WHhvPzJiaB?= NHPmXWpqdmS3Y3XzJIFxd3C2b4Ppdy=> MofHNlU4PTB|MEi=
Calu-1  MYfBdI9xfG:|aYOgRZN{[Xl? MkDhNVAh|ryP MX:3NkBp M2\KZYlv\HWlZYOgZZBweHSxc3nz MmrJNlU4PTB|MEi=
H358 MmHwRZBweHSxc3nzJGF{e2G7 NYfSVFIzOTBizszN NHuyXnM4OiCq MWPpcoR2[2W|IHHwc5B1d3Orcx?= MUGyOVc2ODNyOB?=
PC9/GR Mnz3SpVv[3Srb36gRZN{[Xl? M{ewVlUhyrWP M{nVV|Q5KGh? NUXDUmlVcW6mdXPld{BifXSxcHjh[5k> NX\MUZV{OjV2OE[0NFk>
PC9/ER MXLGeY5kfGmxbjDBd5NigQ>? MojJOUDDvU1? NFnqOoQ1QCCq NX7veJBxcW6mdXPld{BifXSxcHjh[5k> MX[yOVQ5PjRyOR?=
H28 NFXMZnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEHCcYwxNjBzLUOwJO69VQ>? MWS3NkBp NVHwU3VTTE2VTx?= NGr6eG5KSzVyPUeuNkDPxE1? NWS4N|VZOjV2MkKwPFE>
H2052 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjFW2cxNjBzLUOwJO69VQ>? M3;3[|czKGh? Ml7VSG1UVw>? NYjIPFRQUUN3ME2yMlAh|ryP M4KzT|I2PDJ{MEix
UM-SCC-1 MlP4R4xwdm:pZX7pZ{BCe3OjeR?= M{nmclAvPS13IN88US=> NH;HZlkyPCCm M1[5W2ROW09? MmfuxsBqdmirYnn0d{BkdG:wb3flcolkKHO3co\peoFtKGGwZDDzdIhmemViZn;ycYF1cW:w M1jLWVI2Ozd7MEG2
UM-SCC-46 MVnDcI9vd2enbnnjJGF{e2G7 NYWwcW0{OC53LUWg{txO M4DsSFE1KGR? NWfTOYp5TE2VTx?= NHrqVmPDqGmwaHnibZR{KGOub37v[4VvcWNic4Xyeol3[WxiYX7kJJNxcGW{ZTDmc5Ju[XSrb36= M2HQOFI2Ozd7MEG2
U87-MG M1W0eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUOxM|UwOTBizszN MmPXNlQwPDhxN{KgbC=> NV35c4ZOTE2VTx?= MoTCbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[m:2aDDjc45k\W62cnH0bY9vKGGwZDD0bY1mKGSncHXu[IVvfGy7 M{LhSFI2OjRzOEm3
MDA-MB-231 MXnGeY5kfGmxbjDBd5NigQ>? MofENk82NzFyIN88US=> M16xfVQhcA>? MnX1[IVkemWjc3XzJJRp\SClb37zeIl1fXSrdnWgdIhwe3Cqb4L5cIF1cW:wIH;mJIJwfGhiIICtV|UzQS2yNkWgZY5lKHBvU{GyPU1Cc3R? MlXRNlUyPTN5MkW=
MDA-MB-231 M1jnVWZ2dmO2aX;uJGF{e2G7 M4rnXVIwPS9zMDFOwG0> MkeyOEBp MmLrbY5pcWKrdIOgd4VzcW6nIEWyPUBxcG:|cHjvdplt[XSrb36gZY5lKHSqZTDlfJBz\XO|aX;uJI9nKEmOLU[sJGlNNTh? MXSyOVE2Ozd{NR?=
ARPE-19 MYLLbY5ie2ViQYPzZZk> M{nVW|UwOTBxMkCg{txO M33OS|I1NzR6IHi= NILUd|RqdmirYnn0d{BEUzJia3nuZZNmKGGldHn2bZR6KGG2IHGgZ49v[2WwdILheIlwdiCxZjC1xsDPxE1? MUSyOFY5PjB6MB?=
ARPE-19 MnzrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWWxNEDPxE1? NVTZNWFlOjRvOU[gbC=> NX\lW5VITE2VTx?= MVHpcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 MlTUNlQ3QDZyOEC=
HCT116  NYLvOXJLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYixNEDPxE1? NGX6N5gzPC17NjDo M4\mSWROW09? M{PIfYlvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk> M{GwdlI1Pjh4MEiw
ARPE-19 NVL0Z3VwTnWwY4Tpc44hSXO|YYm= NWmwVoJIOTBizszN M3u1dFQhcA>? NETpXHVFVVOR NXvlRmlz[2G3c3XzJGVTNXO2cnXzd{Bz\XOyb37z[UBwfmW{IITo[UBxNWWLRkNOtUBjemGwY3isJIJ2fCCmb3XzJI5wfCCrbnT1Z4UhS0iRUNMg NXzhcFhKOjR4OE[wPFA>
HCT116  M2j5SWZ2dmO2aX;uJGF{e2G7 MX2xNEDPxE1? MYW0JIg> M17YbGROW09? MUfjZZV{\XNiRWKtd5Rz\XO|IILld5BwdnOnIH;2[ZIhfGinIICt[WlHOs7zIHLyZY5kcCxiYoX0JIRw\XNibn;0JIlv\HWlZTDDTG9RyqB? M{HSOVI1Pjh4MEiw
HCT116  M{nFRWFxd3C2b4Ppd{BCe3OjeR?= NYrybnhmOTBizszN MmDPNlQwPDhiaB?= M1vHXmROW09? MoK2bY5lfWOnczDhdI9xfG:|aYO= M3jTXlI1Pjh4MEiw
Nalm6  M{DVTGZ2dmO2aX;uJGF{e2G7 NVj5bG1zOTBxMkCg{txO MXmyOEBp NID5TYRz\XO3bITzJIlvKGSnY4LlZZNm\CCSVFXOJJBpd3OyaH;yfYxifGmxbjDheEB1cGViQ1uyJJRiemendDDy[ZNq\HWnIGOzPFAh[W6mIHPvcoNwdWm2YX70JIRwf26{ZXf1cIF1cW:wIH;mJHBVTU5icILveIVqdiCneIDy[ZN{cW:w MYGyOFU3OTd7Mh?=
SUP-B15 MUTGeY5kfGmxbjDBd5NigQ>? NISxZ2wyOC9{MDFOwG0> MoTtNlQhcA>? NV7OUI1MemW|dXz0d{BqdiCmZXPy[YF{\WRiUGTFUkBxcG:|cHjvdplt[XSrb36gZZQhfGinIFPLNkB1[XKpZYSgdoV{cWS3ZTDTN|gxKGGwZDDjc45kd22rdHHueEBld3ewcnXneYxifGmxbjDv[kBRXEWQIIDyc5RmcW5iZYjwdoV{e2mxbh?= NHPKcVEzPDV4MUe5Ni=>
Nalm6  NWfFOWNHSXCxcITvd4l{KEG|c3H5 M3rwVFYwOTBizszN M3K4flQ5KGh? NWXR[VNZcW6mdXPld{BieG:ydH;zbZM> M4LMSFI1PTZzN{my
SUP-B15 MVPBdI9xfG:|aYOgRZN{[Xl? M3PYVFYwOTBizszN NYrLVI5{PDhiaB?= MXfpcoR2[2W|IHHwc5B1d3Orcx?= NHzBR5czPDV4MUe5Ni=>
C2C12 NW\rNJdETnWwY4Tpc44hSXO|YYm= MkHrN{DPxE1? MnroNVIwOjRxNEigbC=> MVHpcohq[mm2czD0bIUh\XiycnXzd4lwdiCxZjDvd5Rmd2OuYYP0JIRq\m[ncnXueIlifGmxbjDtZZJs\XK|IHHu[EBCc3RicHjvd5Bpd3K7bHH0bY9v M2H3clI1Ojl|MEGx
Jurkat NHToU3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\oPJdLOS1zMDFOwG0> NYjxdnZSPDhiaB?= MljFTWM2OD12Lkmg{txO MYSyOFI2OzB{NB?=
CEM-R MmmzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnkTowyOS1zMDFOwG0> MkTuOFghcA>? NXXTZnpbUUN3ME20JO69VQ>? MX2yOFI2OzB{NB?=
CEM-S NU\0c2V1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\6NU0yOCEQvF2= NWTxd3lrPDhiaB?= NWHtdJNUUUN3ME20MlYh|ryP NX;DZpZtOjR{NUOwNlQ>
MOLT-4 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDOV|cyNTFyIN88US=> NXP3UppxPDhiaB?= M4PQTGlEPTB;NT63JO69VQ>? NFP4ToozPDJ3M{CyOC=>
PF-382 Mn7yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUexMVExKM7:TR?= M3rKcFQ5KGh? MXLJR|UxRTRwNTFOwG0> NVfyUZV5OjR{NUOwNlQ>
ALL-SIL M3zJUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnyS2dCOS1zMDFOwG0> NWrGWYFpPDhiaB?= NYDQe3ZCUUN3ME21Mlch|ryP M4XzXlI1OjV|MEK0
HPB-ALL MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXGxMVExKM7:TR?= NVm2WolqPDhiaB?= MljnTWM2OD14LkGg{txO NWnKO4NEOjR{NUOwNlQ>
DND-41 NEDQN2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvYNU0yOCEQvF2= NXnvVnNZPDhiaB?= NGPsVGJKSzVyPUmg{txO M1njc|I1OjV|MEK0
ALL-SIL MkS3RZBweHSxc3nzJGF{e2G7 MVy1JO69VQ>? MYOyOE81QCCq NVrhOY15cW6mdXPld{BieG:ydH;zbZM> MkPTNlQzPTNyMkS=
DND-41 NYflbJY1SXCxcITvd4l{KEG|c3H5 NVjU[GlwPSEQvF2= MmfxNlQwPDhiaB?= M2jKbolv\HWlZYOgZZBweHSxc3nz NInN[JAzPDJ3M{CyOC=>
MOLT-4 NIDkUJBCeG:ydH;zbZMhSXO|YYm= M4TsRlUh|ryP NV\OeJpkOjRxNEigbC=> NV\tWWh7cW6mdXPld{BieG:ydH;zbZM> M1nFcVI1OjV|MEK0
U-266 MnLSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV[wMVQxKM7:TR?= NEi5e|Y1QCCq NF3SeVBKSzVyPUG5MlghyrWPwrC= M2DkUVI1ODh4NEm0
INA-6 MnK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYGwMVQxKM7:TR?= M1SzZlQ5KGh? NYnhUWVPUUN3ME2yMlQzKML3TR?= NV\NfZViOjRyOE[0PVQ>
Jeko-1 NY\DRXlFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXSwMVQxKM7:TR?= NYfN[pNpPDhiaB?= M13FTGlEPTB;Mj60JOK2VcLi MViyOFA5PjR7NB?=
Rec-1 M{PKRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUSwMVQxKM7:TR?= NIq5XpY1QCCq MnrNTWM2OD1zLkS2JOK2VcLi NEfi[pEzPDB6NkS5OC=>
A549 NWOwXm5QTnWwY4Tpc44hSXO|YYm= MVSxNEDPxE1? NELlPJkyOi9{ND:0PEBp NGjXVIVqdmirYnn0d{BVT0ZvzsKxMYlv\HWlZXSgcYloemG2aX;uJIFv\CCrbo\hd4lwdg>? MlHQNlQxOjN7M{i=
A549 MXHGeY5kfGmxbjDBd5NigQ>? NFizbJY{KM7:TR?= MlvwOFghcA>? MkS5bY5pcWKrdIOgWGdHNc7{MT3pcoR2[2WmIHHjeIl3[XSrb36gc4YhW22jZDDhcoQh\XiycnXzd4lwdiCxZjDTcoFqdCCjbnSgWJdqe3R? NXLjd4VzOjRyMkO5N|g>
S-LAMA84 M1\YVmZ2dmO2aX;uJGF{e2G7 NFqweI4{yqEQvF2= MWGyOEBp NXq2b4Q6TE2VTx?= M{m2[pJm\HWlZYOgR2szKGGldHn2bZR6 M4\EWFI1ODF{MUC5
R-LAMA84 M3r5bmZ2dmO2aX;uJGF{e2G7 MWizxsDPxE1? Ml;hNlQhcA>? Mnj4SG1UVw>? NH7sW2Fz\WS3Y3XzJGNMOiCjY4Tpeol1gQ>? NUfmUmo1OjRyMUKxNFk>
S-LAMA84 MnXES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvBNk42NTFyIN88US=> NVLj[GZ3PDhiaB?= MUPEUXNQ NFfqZ49qdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 M{[4dFI1ODF{MUC5
R-LAMA84 NYe3b4RLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGCwZ4UzNjVvMUCg{txO NFqzZlc1QCCq M1TjUWROW09? MVnpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 M2n0UlI1ODF{MUC5
A549 NVjWdFNMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlG3NE0{OCEQvF2= MkjnO|IhcA>? NXfqVFlQTE2VTx?= M3\4VmlEPTB;ND6xOUDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJINwdmOnboTyZZRqd25iZHXw[Y5l\W62bIm= MWKyN|Y2OTR2Mx?=
H1299 NUfMRVdrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXewMVMxKM7:TR?= MkO1O|IhcA>? M{W3fmROW09? MnTRTWM2OD1zLkiwJO69VSxiaX7obYJqfHNiY3XscEBoem:5dHigZ49v[2WwdILheIlwdiCmZYDlcoRmdnSueR?= MofZNlM3PTF2NEO=
A549 MV3GeY5kfGmxbjDBd5NigQ>? M2L0T|EwOTBizszN NVn5bnBLPDhiaB?= MXnEUXNQ Mm\icIVi\HNidH:gZUBld3OnLXTldIVv\GWwdDDk[YNz\WG|ZTDpckBPd3SlaDDy[ZBwenSncjDhZ5Rqfmm2eR?= MUWyN|Y2OTR2Mx?=
LNCap NH\Me|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\QNE0{OCEQvF2= Mm\NOEBl M3;CVGlEPTB;ND61PeKh|ryP M3S3R|IzQDN{M{G2
A431  MWDGeY5kfGmxbjDBd5NigQ>? M1;BfVExKM7:TR?= NXjrVYRxOzBibXnu NE\aTZRifHSnboXheIV{KFCLM1utRYt1NW2WT2Kgd4lodmGuaX7n MknHNlI{QDd7OEi=
H2170  MkTiSpVv[3Srb36gRZN{[Xl? MXyxNEDPxE1? NGHVeVA{OCCvaX6= Mn3hZZR1\W63YYTld{BRUTONLVHreE1uXE:UIIPp[45idGmwZx?= MWGyNlM5Pzl6OB?=
A431  M{HmeWZ2dmO2aX;uJGF{e2G7 NWPxR4ltOTBizszN NFixSoE1NTJ2IHi= M2DtW4VvcGGwY3XzJIFxd3C2b4Ppd{B4cXSqIHXycI91cW6rYh?= NU\Hc|JROjJ|OEe5PFg>
H2170  M{TINmZ2dmO2aX;uJGF{e2G7 MYqxNEDPxE1? NYr2SItjPC1{NDDo Mo[w[Y5p[W6lZYOgZZBweHSxc3nzJJdqfGhiZYLsc5Rqdmmk NEL4fJczOjN6N{m4PC=>

... 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 )

  • 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):
    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

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

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