Silmitasertib (CX-4945)

For research use only.

Catalog No.S2248

56 publications

Silmitasertib (CX-4945) Chemical Structure

Molecular Weight(MW): 349.77

Silmitasertib (CX-4945) is a potent and selective inhibitor of CK2 (casein kinase 2) with IC50 of 1 nM in a cell-free assay, less potent to Flt3, Pim1 and CDK1 (inactive in cell-based assay). Silmitasertib induces autophagy and promotes apoptosis. Phase 1/2.

Size Price Stock Quantity  
10mM (1mL in DMSO) USD 291 In stock
USD 127 In stock
USD 170 In stock
USD 320 In stock
USD 890 In stock
USD 1270 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Selleck's Silmitasertib (CX-4945) has been cited by 56 publications

Purity & Quality Control

Choose Selective Casein Kinase Inhibitors

Biological Activity

Description Silmitasertib (CX-4945) is a potent and selective inhibitor of CK2 (casein kinase 2) with IC50 of 1 nM in a cell-free assay, less potent to Flt3, Pim1 and CDK1 (inactive in cell-based assay). Silmitasertib induces autophagy and promotes apoptosis. Phase 1/2.
Features First clinical inhibitor of CK2.
Targets
CK2 [1]
(Cell-free assay)
1 nM
In vitro

CX-4945 is selective for CK2, as it only inhibits 7 of the 238 kinases by more than 90% at concentration of 0.5 μM, which is 500-fold greater than the IC50 of CK2. Although in cell-free systems CX-4945 inhibits FLT3, PIM1, and CDK1 with IC50 of 35 nM, 46 nM, and 56 nM, respectively, CX-4945 treatment at 10 μM is inactive against FLT3, PIM1, and CDK1 in cell-based functional assays. CX-4945 exhibits a broad spectrum of antiproliferative activity, and the breast cancer cell lines displays the widest range of sensitivity to CX-4945 with EC50 of 1.71-20.01 μM. The antiproliferative activity of CX-4945 correlates with CK2α mRNA and protein levels but not the CK2α' catalytic subunit, the regulatory CK2β subunit, and the PI3K/Akt or PTEN mutational status. CX-4945 inhibits PI3K/Akt signaling by directly blocking the phosphorylation of Akt at Serine 129 by CK2 rather than through activation of PTEN. CX-4945 treatment causes reduced phosphorylation of p21 (T145), increased levels of total p21 and p27, and induction of caspase 3/7 activity. CX-4945 treatment induces a G2/M cell-cycle arrest in BT-474 cells and a G1 arrest in BxPC-3 cells. CX-4945 inhibits HUVEC proliferation, migration, and tube formation with IC50 of 5.5 μM, 2 μM, and 4 μM, respectively. Under hypoxic conditions in BT-474 and BxPC-3 cells, CX-4945 treatment prevents downregulation of p53 and pVHL and reduces activation of HIF-1α transcription. [1] CX-4945 potently inhibits endogenous intracellular CK2 activity with IC50 of 0.1 μM in Jurkat cells. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
platelets NHrJfFVMcW6jc3WgRZN{[Xl? MVWxM|UwOTBizszN MkTnNE42KGh? MUPEUXNQ NGDadohz\WS3Y3XzJGNMOiCtaX7hd4Uh[WO2aY\peJkh[W6mIIDsZZRmdGW2IHHn[5Jm\2G2aX;u MV[yOlM5OTR|Nx?=
HDMEC MVzLbY5ie2ViQYPzZZk> M3;V[VAvOjVxMD61M|Eh|ryP Mlm3NlQhcA>? MkL0SG1UVw>? NE\jNY9z\WS3Y3XzJGNMOiCtaX7hd4Uh[WO2aY\peJktKH[ZRjDlfJBz\XO|aX;uJIFv\CC|ZXPy[ZRqd25? MkPhNlY{QDF2M{e=
HDMEC MnXhSpVv[3Srb36gRZN{[Xl? MWCwMlI2NzBwNT:xJO69VQ>? MVKyOEBp M2LpRWROW09? NF3T[oNz\WS3Y3XzJIV5eHKnc4Ppc44hd2ZiVlPBUU0yKGK3dDDuc5QhUUODTT2x M{XzeVI3OzhzNEO3
HDMEC M1XvXmZ2dmO2aX;uJGF{e2G7 M3LEZlEh|ryP MnviNlQhcA>? NH3MXXlFVVOR MYLh[oZm[3S|IIP1ZoNmdGy3bHHyJIxw[2GuaYrheIlwdiCxZjDOSmFV[zFiYX7kJJBpd3OyaH:tdFY2 MmXlNlY{QDF2M{e=
A549  NV;FN|Q6TnWwY4Tpc44hSXO|YYm= MWCzM|ExyqEQvF2= Mor4OFghcA>? MkPQd5VxeHKnc4Pld{B1cGVibXnjdo9xcWyuYYKtbY5lfWOnZDDlfJBz\XO|aX;uJI9nKHBvRlHL NY\qboVEOjZ|MUi4NFA>
HDMEC MWLLbY5ie2ViQYPzZZk> MY[xMVUxKM7:TR?= NEnWW|M2KGh? NFH6TFZFVVOR MkG0[IVkemWjc3XzJGNMOiCtaX7hd4Uh[WO2aY\peJkhf2m2aH;1eEBi\m[nY4Tpcoch[2WubDD2bYFjcWyrdIm= M2O1VlI3OTh7NUi2
HDMEC MYXGeY5kfGmxbjDBd5NigQ>? NX\tV2RWPTBizszN NH\OZpEyNzViaB?= M3fTbmROW09? NEjxbHNl\WO{ZXHz[ZMhfGinIH71Z4xm[XJic3nncoFtKG:oIIDoc5NxcG:{eXzheIVlKHB4NTDpckBVVkZvzsGtd5RqdXWuYYTl[EBJTE2HQ9Mg M2jqXVI3OTh7NUi2
HEK293 MX\LbY5ie2ViQYPzZZk> MmD1NE42yqEQvF2= NVv4WHpMOTVibXnu NYi4ZZFCTE2VTx?= MmfkdoVlfWOnczDDT|Ihc2mwYYPlJIFkfGm4aYT5 M13PSVI2QDh5NkK2
Hela M{HUOWtqdmG|ZTDBd5NigQ>? M4TNXFAvPcLizszN MUmxOUBucW5? MVvEUXNQ Mk\PdoVlfWOnczDDT|Ihc2mwYYPlJIFkfGm4aYT5 NX62SXhEOjV6OEe2NlY>
LAMA84 NEfpcG5McW6jc3WgRZN{[Xl? NITDW5MxNjYEoN88US=> MlrUNVUhdWmw MljESG1UVw>? M2jyOZJm\HWlZYOgR2szKGurbnHz[UBi[3Srdnn0fS=> NVWwU4JWOjV6OEe2NlY>
HEK293 M1TBTmZ2dmO2aX;uJGF{e2G7 MVezJO69VQ>? NGPifFQ2KGh? NF3KW5pFVVOR Ml:4R2szKHCqb4PwbI9zgWyjdHXzJIVKTjOsIHH0JHNmejF{Nx?= MYWyOVg5PzZ{Nh?=
UM-SCC1 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHlfINEOC5zLUOwJO69VQ>? NHPscW0yNTViZB?= MV\JR|UxRTRwMTFOwG0> NFrQdpUzPTd7OEC2NS=>
UM-SCC46 MmfUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVOwMlEuOzBizszN MnHwNU02KGR? MkPWTWM2OD1|LkSg{txO NFTpNngzPTd7OEC2NS=>
UM-SCC1 NUD1PG5[TnWwY4Tpc44hSXO|YYm= NX\ERWZ6OC53L{SvNVAh|ryP M3HvNlczKGh? NX:yfVh2\G:5bj3y[Yd2dGG2ZYOgeIhmKGW6cILld5Nqd25ib3[gUmYuzLiELDDCZ4wuYExiYX7kJJVxNXKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCyNUOsJJAzOSxiQWCtNUBidmRiSVytPEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 NFL1PZQzPTd7OEC2NS=>
UM-SCC46 NV6yWpZnTnWwY4Tpc44hSXO|YYm= NEHqdWsxNjVxND:xNEDPxE1? M1rETFczKGh? NEn1S3hld3ewLYLl[5Vt[XSnczD0bIUh\XiycnXzd4lwdiCxZjDOSk3FwEJuIFLjcE1ZVCxicEWzMEBxOjFuIFHQMVEh[W6mIIXwMZJm\3WuYYTld{B1cGViZYjwdoV{e2mxbjDJUE05KGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> MYKyOVc6QDB4MR?=
NU-DUL MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTzV2lsPS1{NTFOwG0> MX60PEBp NEO0W4FqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NGPvSlYzPTd6OEK2PS=>
Oci Ly 3 M{\Cbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYfaeGMxPS1{NTFOwG0> NXnwUVRKPDhiaB?= MmT2bY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> NHq0cnIzPTd6OEK2PS=>
Oci Ly 10 MkX3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;sOU0zPSEQvF2= MmfPOFghcA>? NFW1cWRqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NXXXSIhJOjV5OEiyOlk>
Oci Ly 1 MoX3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrnNYFEPS1{NTFOwG0> NXHZXlVqPDhiaB?= NE\WclBqdmirYnn0d{Bk\WyuIHfyc5d1cCClb37j[Y51emG2aX;uJIRmeGWwZHXueIx6 NVfmSJhGOjV5OEiyOlk>
Oci Ly 18 NIPTUVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWi1MVI2KM7:TR?= MnnTOFghcA>? NV;uTm9EcW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? NFy1O5gzPTd6OEK2PS=>
Oci Ly 19  MlL6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1HpO|UuOjVizszN NGTWNJI1QCCq MmPXbY5pcWKrdIOgZ4VtdCCpcn;3eIgh[2:wY3XueJJifGmxbjDk[ZBmdmSnboTsfS=> NYPrUmwxOjV5OEiyOlk>
Raji NVW2[2ZuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3rOU0zPSEQvF2= NYP3WFVuPDhiaB?= M3vLT4lvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> NF7vTZozPTd6OEK2PS=>
H1299 NW\p[oxmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjwV28yNzVxMUCg{txO MYS3NkBp NX[zbY9HcW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? MVqyOVc2ODNyOB?=
Calu-1  MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFr2bmIyNzVxMUCg{txO MnXQO|IhcA>? NVHST3lmcW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? M{HrSFI2PzVyM{C4
H358 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTINU82NzFyIN88US=> NXH0VYI{PzJiaB?= NXO1cZI{cW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>? M3HMTVI2PzVyM{C4
H1299 NYi2VoE6SXCxcITvd4l{KEG|c3H5 NYHlU4FDOTBizszN NYnPSJVsPzJiaB?= MX3pcoR2[2W|IHHwc5B1d3Orcx?= M1y3e|I2PzVyM{C4
Calu-1  NVP5OVVWSXCxcITvd4l{KEG|c3H5 M2OwTlExKM7:TR?= MmToO|IhcA>? MWfpcoR2[2W|IHHwc5B1d3Orcx?= NFrRfZgzPTd3MEOwPC=>
H358 NFnUbZJCeG:ydH;zbZMhSXO|YYm= NVS1[GlYOTBizszN MWe3NkBp NV7a[o1tcW6mdXPld{BieG:ydH;zbZM> NVrzN2hoOjV5NUCzNFg>
PC9/GR NIrnbINHfW6ldHnvckBCe3OjeR?= NIexSHg2KML3TR?= NX7WV4VZPDhiaB?= M3ywc4lv\HWlZYOgZZV1d3CqYXf5 MnvhNlU1QDZ2MEm=
PC9/ER NFTmeYRHfW6ldHnvckBCe3OjeR?= NX3RVY9ZPSEEtV2= NGXUdmM1QCCq NGrT[2NqdmS3Y3XzJIF2fG:yaHHnfS=> MVqyOVQ5PjRyOR?=
H28 M3TLZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPKOXVwOC5yMT2zNEDPxE1? NHfXWWE4OiCq NGjpZmhFVVOR MUfJR|UxRTdwMjFOwG0> MkTrNlU1OjJyOEG=
H2052 NU\jb|RDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{X6UlAvODFvM{Cg{txO MkLsO|IhcA>? NHrOOVNFVVOR M2jafGlEPTB;Mj6wJO69VQ>? M3KwTVI2PDJ{MEix
UM-SCC-1 MUTDcI9vd2enbnnjJGF{e2G7 M4nKe|AvPS13IN88US=> MVyxOEBl M2HKd2ROW09? Mn;axsBqdmirYnn0d{BkdG:wb3flcolkKHO3co\peoFtKGGwZDDzdIhmemViZn;ycYF1cW:w MYqyOVM4QTBzNh?=
UM-SCC-46 MUjDcI9vd2enbnnjJGF{e2G7 MmryNE42NTVizszN Mmn0NVQh\A>? M1PzT2ROW09? MlOyxsBqdmirYnn0d{BkdG:wb3flcolkKHO3co\peoFtKGGwZDDzdIhmemViZn;ycYF1cW:w MkPINlU{PzlyMU[=
U87-MG MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4Xu[FEwPS9zMDFOwG0> MkO1NlQwPDhxN{KgbC=> NIPEPYRFVVOR M322fYlvcGmkaYTzJINmdGxiZ4Lve5RpKGKxdHigZ49v[2WwdILheIlwdiCjbnSgeIlu\SCmZYDlcoRmdnSueR?= MWmyOVI1OTh7Nx?=
MDA-MB-231 MVTGeY5kfGmxbjDBd5NigQ>? MlXqNk82NzFyIN88US=> MV:0JIg> Moq3[IVkemWjc3XzJJRp\SClb37zeIl1fXSrdnWgdIhwe3Cqb4L5cIF1cW:wIH;mJIJwfGhiIICtV|UzQS2yNkWgZY5lKHBvU{GyPU1Cc3R? M{CxfFI2OTV|N{K1
MDA-MB-231 M37RPGZ2dmO2aX;uJGF{e2G7 NIP6XnUzNzVxMUCg{txO NF\qc3c1KGh? NVqxeJNqcW6qaXLpeJMhe2W{aX7lJFUzQSCyaH;zdIhwenmuYYTpc44h[W6mIITo[UBmgHC{ZYPzbY9vKG:oIFnMMVYtKEmOLUi= NFfE[G0zPTF3M{eyOS=>
ARPE-19 M3PmOmtqdmG|ZTDBd5NigQ>? M2DWTFUwOTBxMkCg{txO MonjNlQwPDhiaB?= MX\pcohq[mm2czDDT|Ihc2mwYYPlJIFkfGm4aYT5JIF1KGFiY3;uZ4VvfHKjdHnvckBw\iB3wrFOwG0> M1zpWFI1Pjh4MEiw
ARPE-19 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUOxNEDPxE1? MlTvNlQuQTZiaB?= NUT6OIdbTE2VTx?= MYLpcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 NFvZVpgzPDZ6NkC4NC=>
HCT116  NHroNoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnYRYgyOCEQvF2= MYmyOE06PiCq MUjEUXNQ MVrpcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 MXmyOFY5PjB6MB?=
ARPE-19 M3z2OGZ2dmO2aX;uJGF{e2G7 NH;OWWwyOCEQvF2= M4PYeFQhcA>? M3zGV2ROW09? MV;jZZV{\XNiRWKtd5Rz\XO|IILld5BwdnOnIH;2[ZIhfGinIICt[WlHOs7zIHLyZY5kcCxiYoX0JIRw\XNibn;0JIlv\HWlZTDDTG9RyqB? MmDmNlQ3QDZyOEC=
HCT116  M{L1cWZ2dmO2aX;uJGF{e2G7 NH\l[FEyOCEQvF2= NYLXcXpVPCCq MVjEUXNQ NHrwXZFk[XW|ZYOgSXIue3S{ZYPzJJJme3CxboPlJI93\XJidHjlJJAu\UmIMt8xJIJz[W6laDygZpV1KGSxZYOgco91KGmwZIXj[UBEUE:SwrC= M1;h[|I1Pjh4MEiw
HCT116  MoXQRZBweHSxc3nzJGF{e2G7 MkjiNVAh|ryP MWWyOE81QCCq NUnHWYRTTE2VTx?= NHTsNodqdmS3Y3XzJIFxd3C2b4Ppdy=> NVHJeIttOjR4OE[wPFA>
Nalm6  NVvJNHZ5TnWwY4Tpc44hSXO|YYm= NX7qN3JnOTBxMkCg{txO NX3h[YkxOjRiaB?= MnrTdoV{fWy2czDpckBl\WO{ZXHz[YQhWFSHTjDwbI9{eGixconsZZRqd25iYYSgeIhmKEONMjD0ZZJo\XRicnXzbYR2\SCVM{iwJIFv\CClb37jc41qfGGwdDDkc5dvemWpdXzheIlwdiCxZjDQWGVPKHC{b4TlbY4h\XiycnXzd4lwdg>? MlPjNlQ2PjF5OUK=
SUP-B15 MXPGeY5kfGmxbjDBd5NigQ>? NFnpbHQyOC9{MDFOwG0> MY[yOEBp M1\QRZJme3WudIOgbY4h\GWlcnXhd4VlKFCWRV6gdIhwe3Cqb4L5cIF1cW:wIHH0JJRp\SCFS{KgeIFz\2W2IILld4llfWViU{O4NEBidmRiY3;uZ49ucXSjboSg[I94dnKnZ4XsZZRqd25ib3[gVHRGViCycn;0[YlvKGW6cILld5Nqd25? M3PpZ|I1PTZzN{my
Nalm6  MlW0RZBweHSxc3nzJGF{e2G7 NVnHNZBFPi9zMDFOwG0> MknMOFghcA>? Mn7hbY5lfWOnczDhdI9xfG:|aYO= M{nGUVI1PTZzN{my
SUP-B15 MnXCRZBweHSxc3nzJGF{e2G7 M3fPRlYwOTBizszN MWe0PEBp M2rJUolv\HWlZYOgZZBweHSxc3nz MkXLNlQ2PjF5OUK=
C2C12 NYHHSI44TnWwY4Tpc44hSXO|YYm= M{PqeFMh|ryP MYGxNk8zPC92ODDo M4DGSIlvcGmkaYTzJJRp\SCneIDy[ZN{cW:wIH;mJI9{fGWxY3zhd5Qh\GmoZnXy[Y51cWG2aX;uJI1iemuncoOgZY5lKEGtdDDwbI9{eGixconsZZRqd25? NXLCWXpCOjR{OUOwNVE>
Jurkat NFXhPHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIWycFEyNTFyIN88US=> M4\5N|Q5KGh? MmPVTWM2OD12Lkmg{txO NXv1bVI2OjR{NUOwNlQ>
CEM-R NY\P[45YT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnizNU0yOCEQvF2= MmfoOFghcA>? NYC1Z3NQUUN3ME20JO69VQ>? MkP1NlQzPTNyMkS=
CEM-S MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLUUm4yNTFyIN88US=> MV:0PEBp MmX3TWM2OD12Lk[g{txO MY[yOFI2OzB{NB?=
MOLT-4 Ml2yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfTfWYyNTFyIN88US=> MWm0PEBp M4\mdmlEPTB;NT63JO69VQ>? NXy2N3FXOjR{NUOwNlQ>
PF-382 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\5T3d7OS1zMDFOwG0> MkjPOFghcA>? NHPT[VJKSzVyPUSuOUDPxE1? MmfENlQzPTNyMkS=
ALL-SIL Mk\6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFOzbY8yNTFyIN88US=> M1vmRVQ5KGh? M2TiVmlEPTB;NT63JO69VQ>? NGjMe3YzPDJ3M{CyOC=>
HPB-ALL M{W4NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfyZVEyNTFyIN88US=> MYe0PEBp MlXyTWM2OD14LkGg{txO Ml;WNlQzPTNyMkS=
DND-41 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXCUnEzOS1zMDFOwG0> MUi0PEBp MkPFTWM2OD17IN88US=> MnXoNlQzPTNyMkS=
ALL-SIL MVrBdI9xfG:|aYOgRZN{[Xl? NHLFWmM2KM7:TR?= M1XJUVI1NzR6IHi= M3GyO4lv\HWlZYOgZZBweHSxc3nz MYeyOFI2OzB{NB?=
DND-41 NVHISnhnSXCxcITvd4l{KEG|c3H5 M4jqWFUh|ryP NXvNfmx6OjRxNEigbC=> NUXKTYdYcW6mdXPld{BieG:ydH;zbZM> MlTGNlQzPTNyMkS=
MOLT-4 M1zhXWFxd3C2b4Ppd{BCe3OjeR?= MlftOUDPxE1? M1u5VFI1NzR6IHi= NFrq[XJqdmS3Y3XzJIFxd3C2b4Ppdy=> MVyyOFI2OzB{NB?=
U-266 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPJWXkxNTRyIN88US=> Ml;rOFghcA>? NVPHeHBlUUN3ME2xPU45KML3TdMg MVSyOFA5PjR7NB?=
INA-6 NYizRWZxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHy0eosxNTRyIN88US=> MmixOFghcA>? NXO3TVVxUUN3ME2yMlQzKML3TR?= M1fLcFI1ODh4NEm0
Jeko-1 Mm\BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHT4PGQxNTRyIN88US=> MVK0PEBp M3LmUmlEPTB;Mj60JOK2VcLi NWHXPGhFOjRyOE[0PVQ>
Rec-1 M1;INGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljDNE01OCEQvF2= NGDzfZA1QCCq MofsTWM2OD1zLkS2JOK2VcLi MV2yOFA5PjR7NB?=
A549 M37aOGZ2dmO2aX;uJGF{e2G7 MorwNVAh|ryP MorKNVIwOjRxNEigbC=> NVn0UHhtcW6qaXLpeJMhXEeILd8yNU1qdmS3Y3XkJI1q\3KjdHnvckBidmRiaX72ZZNqd25? NGe5NXkzPDB{M{mzPC=>
A549 MWrGeY5kfGmxbjDBd5NigQ>? M4TzdVMh|ryP Mo\oOFghcA>? M3KzTIlvcGmkaYTzJHRITi4QskGtbY5lfWOnZDDhZ5RqfmG2aX;uJI9nKFOvYXSgZY5lKGW6cILld5Nqd25ib3[gV45icWxiYX7kJHR4cXO2 NF[1ZlkzPDB{M{mzPC=>
S-LAMA84 MVTGeY5kfGmxbjDBd5NigQ>? NIjye2I{yqEQvF2= MkjpNlQhcA>? MXzEUXNQ NY\lbmtVemWmdXPld{BEUzJiYXP0bZZqfHl? MlPZNlQxOTJzMEm=
R-LAMA84 Mn3YSpVv[3Srb36gRZN{[Xl? MoD2N:Kh|ryP NGDY[YIzPCCq M{i3NmROW09? NVvZblJEemWmdXPld{BEUzJiYXP0bZZqfHl? M4rPN|I1ODF{MUC5
S-LAMA84 NEfGW|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWSyMlUuOTBizszN Mkj4OFghcA>? MY\EUXNQ M{LpeYlvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk> NUK0dVJKOjRyMUKxNFk>
R-LAMA84 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPtNk42NTFyIN88US=> MWK0PEBp NXriUpVUTE2VTx?= MWrpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 NYXSTIhQOjRyMUKxNFk>
A549 NWLvOWNCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXNNE0{OCEQvF2= MXW3NkBp M4fFXmROW09? NEfsR|JKSzVyPUSuNVUh|ryPLDDpcohq[mm2czDj[YxtKGe{b4f0bEBkd26lZX70doF1cW:wIHTldIVv\GWwdHz5 M{nFU|I{PjVzNESz
H1299 M1nYPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{jkO|AuOzBizszN MkLDO|IhcA>? NIPPTpFFVVOR MoLOTWM2OD1zLkiwJO69VSxiaX7obYJqfHNiY3XscEBoem:5dHigZ49v[2WwdILheIlwdiCmZYDlcoRmdnSueR?= MoLKNlM3PTF2NEO=
A549 NHnkS45HfW6ldHnvckBCe3OjeR?= Mmi1NU8yOCEQvF2= NGfiUog1QCCq MlTHSG1UVw>? NWLWN28ydGWjZIOgeI8h[SCmb4PlMYRmeGWwZHXueEBl\WO{ZXHz[UBqdiCQb4TjbEBz\XCxcoTldkBi[3Srdnn0fS=> M1H2bFI{PjVzNESz
LNCap NE\uR4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLrNE0{OCEQvF2= MoDhOEBl MmfXTWM2OD12LkW5xsDPxE1? M2f1T|IzQDN{M{G2
A431  NYnB[XdSTnWwY4Tpc44hSXO|YYm= NWPaSW1jOTBizszN MnnlN|AhdWmw MkTDZZR1\W63YYTld{BRUTONLVHreE1uXE:UIIPp[45idGmwZx?= MWGyNlM5Pzl6OB?=
H2170  NWHDUHdnTnWwY4Tpc44hSXO|YYm= MkjZNVAh|ryP MVmzNEBucW5? MlPBZZR1\W63YYTld{BRUTONLVHreE1uXE:UIIPp[45idGmwZx?= MX2yNlM5Pzl6OB?=
A431  NYrwTHB6TnWwY4Tpc44hSXO|YYm= MorXNVAh|ryP Mn;0OE0zPCCq NFnaWGpmdmijbnPld{BieG:ydH;zbZMhf2m2aDDldoxwfGmwaXK= NX:2PGZlOjJ|OEe5PFg>
H2170  NUHEXplqTnWwY4Tpc44hSXO|YYm= Mmi1NVAh|ryP Mo\LOE0zPCCq MVTlcohidmOnczDhdI9xfG:|aYOge4l1cCCncnzveIlvcWJ? M3[0UFIzOzh5OUi4

... Click to View More Cell Line Experimental Data

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

PubMed: 30683840     


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

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

PubMed: 25798061     


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

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

PubMed: 24023938     


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

30683840 25798061 24023938
Immunofluorescence
β-catenin; 

PubMed: 24023938     


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

E-cadherin / Vimentin; 

PubMed: 24023938     


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

24023938
Growth inhibition assay
Cell viability; 

PubMed: 30316146     


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

30316146
In vivo Oral administration of CX-4945 at 25 mg/kg or 75 mg/kg twice daily displays potent antitumor activity in the BT-474 model, with TGI of 88% and 97%, respectively, and 2 of 9 animals in each group showing more than 50% reduction in tumor size compared with the initial tumor volume. In the BxPC-3 model, CX-4945 treatment at 75 mg/kg twice daily shows 93% TGI with 3 animals having no evidence of tumor remaining at the end of the treatment period. [1] In PC3 xenograft model, administration of CX-4945 at 25 mg/kg, 50 mg/kg, or 75 mg/kg causes tumor growth inhibition with TGI of 19%, 40%, and 86%, respectively. [2]

Protocol

Kinase Assay:[2]
- Collapse

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]
- Collapse
  • 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]
- Collapse
  • Animal Models: Female immunocompromised mice CrTac:Ncr-Foxn1nu injected with BxPC-3 or BT-474 cells
  • Dosages: 25 or 75 mg/kg
  • Administration: Oral gavage twice daily
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 16 mg/mL (45.74 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1% CMC Na
For best results, use promptly after mixing.
30mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 349.77
Formula

C19H12ClN3O2

CAS No. 1009820-21-6
Storage powder
in solvent
Synonyms N/A
Smiles C1=CC(=CC(=C1)Cl)NC2=NC3=C(C=CC(=C3)C(=O)O)C4=C2C=CN=C4

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*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
    V1
    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

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.

Tags: buy Silmitasertib (CX-4945) | Silmitasertib (CX-4945) supplier | purchase Silmitasertib (CX-4945) | Silmitasertib (CX-4945) cost | Silmitasertib (CX-4945) manufacturer | order Silmitasertib (CX-4945) | Silmitasertib (CX-4945) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID