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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5 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.

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 M2H6Z2tqdmG|ZTDBd5NigQ>? MVqxM|UwOTBizszN NIjK[HIxNjViaB?= NFv5T25FVVOR MX3y[YR2[2W|IFPLNkBscW6jc3WgZYN1cX[rdImgZY5lKHCuYYTlcIV1KGGpZ4Ll[4F1cW:w NGLMOoEzPjN6MUSzOy=>
HDMEC MWTLbY5ie2ViQYPzZZk> NG\WNowxNjJ3L{CuOU8yKM7:TR?= NH;MOJUzPCCq NIT2[otFVVOR M1T2OJJm\HWlZYOgR2szKGurbnHz[UBi[3Srdnn0fUwhfleIIHX4dJJme3Orb36gZY5lKHOnY4LleIlwdg>? NHO4fY0zPjN6MUSzOy=>
HDMEC MYnGeY5kfGmxbjDBd5NigQ>? MoSxNE4zPS9yLkWvNUDPxE1? MVmyOEBp NUHxN|Z3TE2VTx?= NWWzdlRSemWmdXPld{BmgHC{ZYPzbY9vKG:oIG\DRW0uOSCkdYSgco91KEmFQV2tNS=> NGjCN3UzPjN6MUSzOy=>
HDMEC NVPyTY92TnWwY4Tpc44hSXO|YYm= NFPiSZQyKM7:TR?= MVqyOEBp NWTs[VlnTE2VTx?= NF3Z[Ipi\m[nY4TzJJN2[mOnbHz1cIFzKGyxY3HsbZpifGmxbjDv[kBPTkGWY{GgZY5lKHCqb4PwbI8ueDZ3 MlvuNlY{QDF2M{e=
A549  M{K1fWZ2dmO2aX;uJGF{e2G7 MlW3N{8yOMLizszN NVXGN2RlPDhiaB?= MnjUd5VxeHKnc4Pld{B1cGVibXnjdo9xcWyuYYKtbY5lfWOnZDDlfJBz\XO|aX;uJI9nKHBvRlHL NHPtUIIzPjNzOEiwNC=>
HDMEC Mn;jT4lv[XOnIFHzd4F6 NFy3dYUyNTVyIN88US=> MYW1JIg> Mn7wSG1UVw>? M4LmUIRm[3KnYYPld{BEUzJia3nuZZNmKGGldHn2bZR6KHerdHjveZQh[W[oZXP0bY5oKGOnbHygeoli[mmuaYT5 MkD2NlYyQDl3OE[=
HDMEC NF:zTJJHfW6ldHnvckBCe3OjeR?= MYG1NEDPxE1? NX;HWIZXOS93IHi= MYrEUXNQ M1rtRoRm[3KnYYPld{B1cGViboXjcIVieiC|aXfuZYwhd2ZicHjvd5Bpd3K7bHH0[YQheDZ3IHnuJHRPTi4QsT3zeIlufWyjdHXkJGhFVUWFwrC= MmrHNlYyQDl3OE[=
HEK293 MnvKT4lv[XOnIFHzd4F6 MkPMNE42yqEQvF2= NUj6[m1jOTVibXnu NVLPfpc{TE2VTx?= M2PvfZJm\HWlZYOgR2szKGurbnHz[UBi[3Srdnn0fS=> NGXjbVQzPTh6N{[yOi=>
Hela M4HpWGtqdmG|ZTDBd5NigQ>? MkPJNE42yqEQvF2= MmrTNVUhdWmw M1j0PWROW09? NXS1PFZ2emWmdXPld{BEUzJia3nuZZNmKGGldHn2bZR6 MYGyOVg5PzZ{Nh?=
LAMA84 MUjLbY5ie2ViQYPzZZk> MVywMlXDqM7:TR?= M1\NfFE2KG2rbh?= MYXEUXNQ MVPy[YR2[2W|IFPLNkBscW6jc3WgZYN1cX[rdIm= NXizSGVXOjV6OEe2NlY>
HEK293 MYTGeY5kfGmxbjDBd5NigQ>? MXuzJO69VQ>? MYi1JIg> M2i5Z2ROW09? NI[zVXVEUzJicHjvd5Bpd3K7bHH0[ZMh\UmIM3qgZZQhW2W{MUK3 NH3qTFEzPTh6N{[yOi=>
UM-SCC1 NUHIWHk4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPEUJcxNjFvM{Cg{txO M{\LbVEuPSCm M2HvdWlEPTB;ND6xJO69VQ>? NXLp[4pzOjV5OUiwOlE>
UM-SCC46 NYDKVpVIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LVe|AvOS1|MDFOwG0> M{jwT|EuPSCm M1W2cmlEPTB;Mz60JO69VQ>? M{\PZVI2Pzl6ME[x
UM-SCC1 M4jzeGZ2dmO2aX;uJGF{e2G7 MWSwMlUwPC9zMDFOwG0> MWS3NkBp NFXBfGJld3ewLYLl[5Vt[XSnczD0bIUh\XiycnXzd4lwdiCxZjDOSk3FwEJuIFLjcE1ZVCCjbnSgeZAuemWpdXzheIV{KHSqZTDlfJBz\XO|aX;uJI9nKHB3MzygdFIyNCCDUD2xJIFv\CCLTD24JINwdmOnboTyZZRqd25iZHXw[Y5l\W62bIm= MUKyOVc6QDB4MR?=
UM-SCC46 MY\GeY5kfGmxbjDBd5NigQ>? NEKxc|AxNjVxND:xNEDPxE1? NGLJVFE4OiCq Morl[I94di2{ZXf1cIF1\XNidHjlJIV5eHKnc4Ppc44hd2ZiTl[tyNhDNCCEY3ytXGwtKHB3MzygdFIyNCCDUD2xJIFv\CC3cD3y[Yd2dGG2ZYOgeIhmKGW6cILld5Nqd25iSVytPEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 MWKyOVc6QDB4MR?=
NU-DUL MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\jOU0zPSEQvF2= NEH0emw1QCCq MoDGbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> MlPWNlU4QDh{Nkm=
Oci Ly 3 NFXEd5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXi1MVI2KM7:TR?= NYLvXGV7PDhiaB?= MX7pcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 NHTGbYIzPTd6OEK2PS=>
Oci Ly 10 NFXNUpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXjOU0zPSEQvF2= Mlu5OFghcA>? NH6xNXVqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 MV2yOVc5QDJ4OR?=
Oci Ly 1 NWjmRXhlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{SwelUuOjVizszN MnHZOFghcA>? M1nrTYlvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> M1vhdVI2Pzh6Mk[5
Oci Ly 18 MonMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlH0OU0zPSEQvF2= MVu0PEBp MXfpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 M2nnTFI2Pzh6Mk[5
Oci Ly 19  M{HnSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHGxbIo2NTJ3IN88US=> NFyzV4M1QCCq NUXme45LcW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? NIfZfYszPTd6OEK2PS=>
Raji NGPzPZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnOV4FwPS1{NTFOwG0> NYXUV4c5PDhiaB?= MkPFbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> Ml7oNlU4QDh{Nkm=
H1299 NF7t[JpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DLSFEwPS9zMDFOwG0> MYe3NkBp NYnTXnpPcW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? MX[yOVc2ODNyOB?=
Calu-1  MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LIPFEwPS9zMDFOwG0> M3jmV|czKGh? NWK4[XR3cW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? MmD6NlU4PTB|MEi=
H358 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPkNU82NzFyIN88US=> Ml35O|IhcA>? NF\xVXVqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NH[0XlMzPTd3MEOwPC=>
H1299 NIjlW|FCeG:ydH;zbZMhSXO|YYm= NEX6SWgyOCEQvF2= NFfNboo4OiCq M1vuSolv\HWlZYOgZZBweHSxc3nz MYSyOVc2ODNyOB?=
Calu-1  MUHBdI9xfG:|aYOgRZN{[Xl? NHnTN2MyOCEQvF2= NXTFNGwxPzJiaB?= MmTIbY5lfWOnczDhdI9xfG:|aYO= MkWyNlU4PTB|MEi=
H358 NYqwOoVPSXCxcITvd4l{KEG|c3H5 MmS3NVAh|ryP MVy3NkBp M{ezb4lv\HWlZYOgZZBweHSxc3nz M172ZVI2PzVyM{C4
PC9/GR NHHEOoVHfW6ldHnvckBCe3OjeR?= MmPWOUDDvU1? NUTvZ3o4PDhiaB?= M2P4fYlv\HWlZYOgZZV1d3CqYXf5 M{\oSVI2PDh4NEC5
PC9/ER NUPMOIJPTnWwY4Tpc44hSXO|YYm= NHH0PZI2KML3TR?= NXm5c5NHPDhiaB?= NGHYVoFqdmS3Y3XzJIF2fG:yaHHnfS=> NX\DT5l4OjV2OE[0NFk>
H28 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDlW4gxNjBzLUOwJO69VQ>? Ml7YO|IhcA>? MVvEUXNQ MnzGTWM2OD15LkKg{txO M3n0WVI2PDJ{MEix
H2052 M4\NUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3Zd2dpOC5yMT2zNEDPxE1? NVzlWWdkPzJiaB?= NUHnZYs1TE2VTx?= MUfJR|UxRTJwMDFOwG0> MYOyOVQzOjB6MR?=
UM-SCC-1 MorwR4xwdm:pZX7pZ{BCe3OjeR?= NHnGcW0xNjVvNTFOwG0> NWL3NYpJOTRiZB?= Mk\6SG1UVw>? Mn7WxsBqdmirYnn0d{BkdG:wb3flcolkKHO3co\peoFtKGGwZDDzdIhmemViZn;ycYF1cW:w NXvsfJUyOjV|N{mwNVY>
UM-SCC-46 MU\DcI9vd2enbnnjJGF{e2G7 MV[wMlUuPSEQvF2= NYLEdIJ7OTRiZB?= NHO0UY1FVVOR NIXZb3XDqGmwaHnibZR{KGOub37v[4VvcWNic4Xyeol3[WxiYX7kJJNxcGW{ZTDmc5Ju[XSrb36= NEe5OW4zPTN5OUCxOi=>
U87-MG MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrm[|gyNzVxMUCg{txO M{X3c|I1NzR6L{eyJIg> NWqwPVJTTE2VTx?= Ml76bY5pcWKrdIOgZ4VtdCCpcn;3eIgh[m:2aDDjc45k\W62cnH0bY9vKGGwZDD0bY1mKGSncHXu[IVvfGy7 MnX5NlUzPDF6OUe=
MDA-MB-231 MmrlSpVv[3Srb36gRZN{[Xl? NYrNeHN[Oi93L{GwJO69VQ>? M1rPS|QhcA>? M2f1PYRm[3KnYYPld{B1cGViY3;ud5RqfHW2aY\lJJBpd3OyaH;yfYxifGmxbjDv[kBjd3SqIDDwMXM2OjlvcE[1JIFv\CCyLWOxNlkuSWu2 NIDVbWszPTF3M{eyOS=>
MDA-MB-231 NIXn[G1HfW6ldHnvckBCe3OjeR?= MYOyM|UwOTBizszN NUC5NVk4PCCq NH;iUVFqdmirYnn0d{B{\XKrbnWgOVI6KHCqb4PwbI9zgWyjdHnvckBidmRidHjlJIV5eHKnc4Ppc44hd2ZiSVytOkwhUUxvOB?= MmfZNlUyPTN5MkW=
ARPE-19 MW\LbY5ie2ViQYPzZZk> M1\DNVUwOTBxMkCg{txO MV6yOE81QCCq NVzSOJFucW6qaXLpeJMhS0t{IHvpcoF{\SCjY4Tpeol1gSCjdDDhJINwdmOnboTyZZRqd25ib3[gOeKh|ryP NIf0Zo8zPDZ6NkC4NC=>
ARPE-19 NYXHS29OT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrHO3oyOCEQvF2= M3j3fFI1NTl4IHi= NWq4cpVuTE2VTx?= Ml:ybY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> M2PtN|I1Pjh4MEiw
HCT116  NGOyWVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmHFNVAh|ryP MmXkNlQuQTZiaB?= MnKzSG1UVw>? MkPxbY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> Ml\MNlQ3QDZyOEC=
ARPE-19 NXnyZXF3TnWwY4Tpc44hSXO|YYm= M3rrVVExKM7:TR?= MoXQOEBp NInrW41FVVOR MXTjZZV{\XNiRWKtd5Rz\XO|IILld5BwdnOnIH;2[ZIhfGinIICt[WlHOs7zIHLyZY5kcCxiYoX0JIRw\XNibn;0JIlv\HWlZTDDTG9RyqB? NWj5U2FWOjR4OE[wPFA>
HCT116  NYXCPWxTTnWwY4Tpc44hSXO|YYm= NWPvZoF[OTBizszN NXHvSVFjPCCq MWDEUXNQ NG\Lcnhk[XW|ZYOgSXIue3S{ZYPzJJJme3CxboPlJI93\XJidHjlJJAu\UmIMt8xJIJz[W6laDygZpV1KGSxZYOgco91KGmwZIXj[UBEUE:SwrC= MYeyOFY5PjB6MB?=
HCT116  MYrBdI9xfG:|aYOgRZN{[Xl? MonKNVAh|ryP MVSyOE81QCCq M4PTW2ROW09? NWC0UGFXcW6mdXPld{BieG:ydH;zbZM> M4jCXFI1Pjh4MEiw
Nalm6  NEf6S|BHfW6ldHnvckBCe3OjeR?= MW[xNE8zOCEQvF2= NEizTXIzPCCq M2\VVZJme3WudIOgbY4h\GWlcnXhd4VlKFCWRV6gdIhwe3Cqb4L5cIF1cW:wIHH0JJRp\SCFS{KgeIFz\2W2IILld4llfWViU{O4NEBidmRiY3;uZ49ucXSjboSg[I94dnKnZ4XsZZRqd25ib3[gVHRGViCycn;0[YlvKGW6cILld5Nqd25? MX[yOFU3OTd7Mh?=
SUP-B15 MoLMSpVv[3Srb36gRZN{[Xl? M2rHeFExNzJyIN88US=> MoD2NlQhcA>? NG[4[VBz\XO3bITzJIlvKGSnY4LlZZNm\CCSVFXOJJBpd3OyaH;yfYxifGmxbjDheEB1cGViQ1uyJJRiemendDDy[ZNq\HWnIGOzPFAh[W6mIHPvcoNwdWm2YX70JIRwf26{ZXf1cIF1cW:wIH;mJHBVTU5icILveIVqdiCneIDy[ZN{cW:w Mk[xNlQ2PjF5OUK=
Nalm6  Mmj6RZBweHSxc3nzJGF{e2G7 NWHIXYh3Pi9zMDFOwG0> MYC0PEBp MV3pcoR2[2W|IHHwc5B1d3Orcx?= M2jtXlI1PTZzN{my
SUP-B15 NUDjUWFUSXCxcITvd4l{KEG|c3H5 MXm2M|ExKM7:TR?= NGfKW|A1QCCq NE\WbGtqdmS3Y3XzJIFxd3C2b4Ppdy=> NYPBbnBUOjR3NkG3PVI>
C2C12 MVrGeY5kfGmxbjDBd5NigQ>? NVfreWFmOyEQvF2= NX71[FJDOTJxMkSvOFghcA>? MmnlbY5pcWKrdIOgeIhmKGW6cILld5Nqd25ib3[gc5N1\W:lbHHzeEBlcW[oZYLlcpRq[XSrb36gcYFzc2W{czDhcoQhSWu2IIDoc5NxcG:{eXzheIlwdg>? MmT0NlQzQTNyMUG=
Jurkat NV\nXWFKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGSxNHIyNTFyIN88US=> MliyOFghcA>? NGjWOWZKSzVyPUSuPUDPxE1? M2\2W|I1OjV|MEK0
CEM-R NUH5bld{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\xeY8yNTFyIN88US=> MkP6OFghcA>? NWrFcHRqUUN3ME20JO69VQ>? MVyyOFI2OzB{NB?=
CEM-S MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NULiTJhDOS1zMDFOwG0> NV;NeI9IPDhiaB?= M2XiZmlEPTB;ND62JO69VQ>? MX2yOFI2OzB{NB?=
MOLT-4 NHK0fZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXOxMVExKM7:TR?= MXu0PEBp MXXJR|UxRTVwNzFOwG0> MWSyOFI2OzB{NB?=
PF-382 NVnGdphIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVWxMVExKM7:TR?= MVS0PEBp NWe2WYdxUUN3ME20MlUh|ryP MoDTNlQzPTNyMkS=
ALL-SIL M2TuTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUSxMVExKM7:TR?= MmfyOFghcA>? MkTBTWM2OD13Lkeg{txO M{ix[FI1OjV|MEK0
HPB-ALL M{nRNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjXRWEyNTFyIN88US=> MXu0PEBp NYP0T2hjUUN3ME22MlEh|ryP MWiyOFI2OzB{NB?=
DND-41 NInqe4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfHXllFOS1zMDFOwG0> MonxOFghcA>? MmixTWM2OD17IN88US=> M1TQc|I1OjV|MEK0
ALL-SIL MljHRZBweHSxc3nzJGF{e2G7 MWe1JO69VQ>? NFvje4czPC92ODDo NVK2ZllncW6mdXPld{BieG:ydH;zbZM> MnW1NlQzPTNyMkS=
DND-41 M2LifmFxd3C2b4Ppd{BCe3OjeR?= NIn6doI2KM7:TR?= MXuyOE81QCCq NInNSYNqdmS3Y3XzJIFxd3C2b4Ppdy=> NIX5RmQzPDJ3M{CyOC=>
MOLT-4 MUnBdI9xfG:|aYOgRZN{[Xl? NWP2XnVnPSEQvF2= MYGyOE81QCCq M33oZ4lv\HWlZYOgZZBweHSxc3nz MU[yOFI2OzB{NB?=
U-266 M1u1Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mor0NE01OCEQvF2= MYe0PEBp MX7JR|UxRTF7LkigxtVOyqB? MmLDNlQxQDZ2OUS=
INA-6 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\TTW1yOC12MDFOwG0> NX\FRXU5PDhiaB?= NVr6TYVCUUN3ME2yMlQzKML3TR?= NX7vNIVJOjRyOE[0PVQ>
Jeko-1 M{nMdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXuwMVQxKM7:TR?= MmnMOFghcA>? M{nZUmlEPTB;Mj60JOK2VcLi MmLmNlQxQDZ2OUS=
Rec-1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYGwMVQxKM7:TR?= NGfZVYs1QCCq NIjHdZRKSzVyPUGuOFYhyrWPwrC= M4nzRlI1ODh4NEm0
A549 Mlq2SpVv[3Srb36gRZN{[Xl? MX2xNEDPxE1? MkXZNVIwOjRxNEigbC=> NWTtemh1cW6qaXLpeJMhXEeILd8yNU1qdmS3Y3XkJI1q\3KjdHnvckBidmRiaX72ZZNqd25? NVzXfZA{OjRyMkO5N|g>
A549 MlrhSpVv[3Srb36gRZN{[Xl? NHfkV5o{KM7:TR?= NFHyeVg1QCCq NXTJN3N3cW6qaXLpeJMhXEeILd8yNU1qdmS3Y3XkJIFkfGm4YYTpc44hd2ZiU33h[EBidmRiZYjwdoV{e2mxbjDv[kBUdmGrbDDhcoQhXHerc4S= MoLqNlQxOjN7M{i=
S-LAMA84 M{\MfGZ2dmO2aX;uJGF{e2G7 MYSzxsDPxE1? NXfwWVJHOjRiaB?= MnLvSG1UVw>? M{TwbJJm\HWlZYOgR2szKGGldHn2bZR6 MmDyNlQxOTJzMEm=
R-LAMA84 MULGeY5kfGmxbjDBd5NigQ>? MVyzxsDPxE1? MYOyOEBp NIn3VXZFVVOR NEPFe|Rz\WS3Y3XzJGNMOiCjY4Tpeol1gQ>? M{Xpd|I1ODF{MUC5
S-LAMA84 M2n5ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7ZNk42NTFyIN88US=> Mki2OFghcA>? NF;xfmhFVVOR NF;wfWhqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 Ml;oNlQxOTJzMEm=
R-LAMA84 NIrrW4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXnNk42NTFyIN88US=> NXK1VHFPPDhiaB?= MnX3SG1UVw>? M{DEVolvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> NXfXdYpjOjRyMUKxNFk>
A549 M1TTWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HKRVAuOzBizszN MUK3NkBp NV;CS49LTE2VTx?= NIfQUnhKSzVyPUSuNVUh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 MViyN|Y2OTR2Mx?=
H1299 NVPIOZRkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWPuOXhEOC1|MDFOwG0> MUe3NkBp M2jES2ROW09? NHrkW|lKSzVyPUGuPFAh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 MXOyN|Y2OTR2Mx?=
A549 NXfmXFBoTnWwY4Tpc44hSXO|YYm= M2PkOFEwOTBizszN M364clQ5KGh? NHz4TmNFVVOR NV7zVWV6dGWjZIOgeI8h[SCmb4PlMYRmeGWwZHXueEBl\WO{ZXHz[UBqdiCQb4TjbEBz\XCxcoTldkBi[3Srdnn0fS=> MVuyN|Y2OTR2Mx?=
LNCap NYDvbWVpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYK3RXJKOC1|MDFOwG0> MmGzOEBl MlizTWM2OD12LkW5xsDPxE1? MoHuNlI5OzJ|MU[=
A431  NVj5XpNpTnWwY4Tpc44hSXO|YYm= M4L0OFExKM7:TR?= NVXu[lNYOzBibXnu M1XqNIF1fGWwdXH0[ZMhWEl|Sz3Bb5QudVSRUjDzbYdv[Wyrbne= M{[3SFIzOzh5OUi4
H2170  MYTGeY5kfGmxbjDBd5NigQ>? NF22bo8yOCEQvF2= M{n0blMxKG2rbh?= NH\lRmlifHSnboXheIV{KFCLM1utRYt1NW2WT2Kgd4lodmGuaX7n MUeyNlM5Pzl6OB?=
A431  NHyxR|BHfW6ldHnvckBCe3OjeR?= MmrHNVAh|ryP NIXje2M1NTJ2IHi= MV3lcohidmOnczDhdI9xfG:|aYOge4l1cCCncnzveIlvcWJ? MUCyNlM5Pzl6OB?=
H2170  M{O4VWZ2dmO2aX;uJGF{e2G7 NFfjdJoyOCEQvF2= M1fJTFQuOjRiaB?= MXvlcohidmOnczDhdI9xfG:|aYOge4l1cCCncnzveIlvcWJ? NG\zVm4zOjN6N{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:
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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    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
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