CX-4945 (Silmitasertib)

Catalog No.S2248

CX-4945 (Silmitasertib) 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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CX-4945 (Silmitasertib) Chemical Structure

CX-4945 (Silmitasertib) Chemical Structure
Molecular Weight: 349.77

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Product Information

  • Compare Casein Kinase Inhibitors
    Compare Casein Kinase Products
  • Inhibition Profile
  • CX-4945 (Silmitasertib) Mechanism
  • Combination Therapy
    Combination Therapy

Product Description

Biological Activity

Description CX-4945 (Silmitasertib) 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.
Targets CK2 [1]
(Cell-free assay)
IC50 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
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A549NF\1PI1HfW6ldHnvckBCe3OjeR?=M1\qR|Mh|ryPM1zKcVQ5KGh?NVezUmc2cW6qaXLpeJMhXEeILd8yNU1qdmS3Y3XkJIFkfGm4YYTpc44hd2ZiU33h[EBidmRiZYjwdoV{e2mxbjDv[kBUdmGrbDDhcoQhXHerc4S=MVyyOFAzOzl|OB?=
S-LAMA84M136d2Z2dmO2aX;uJGF{e2G7MV2zxsDPxE1?M3\NPFI1KGh?MWXEUXNQNYHpXpVPemWmdXPld{BEUzJiYXP0bZZqfHl?M3GxOVI1ODF{MUC5
R-LAMA84MnTpSpVv[3Srb36gRZN{[Xl?MoPuN:Kh|ryPMnPSNlQhcA>?MoKwSG1UVw>?MX7y[YR2[2W|IFPLNkBi[3Srdnn0fS=>MVKyOFAyOjFyOR?=
S-LAMA84NWixbZVsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MkTLNk42NTFyIN88US=>MmW5OFghcA>?MW\EUXNQNYrNfok3cW6qaXLpeJMh[2WubDDndo94fGhiY3;uZ4VvfHKjdHnvckBl\XCnbnTlcpRtgQ>?MmToNlQxOTJzMEm=
R-LAMA84M4HEZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NGDTeFYzNjVvMUCg{txOM1T1N|Q5KGh?MmDGSG1UVw>?M{DHPYlvcGmkaYTzJINmdGxiZ4Lve5RpKGOxbnPlcpRz[XSrb36g[IVx\W6mZX70cJk>MVqyOFAyOjFyOR?=
A549NEnZdmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MXqwMVMxKM7:TR?=M2jISlczKGh?NUPtUJNzTE2VTx?=MlqyTWM2OD12LkG1JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHigZ49v[2WwdILheIlwdiCmZYDlcoRmdnSueR?=M2DOTVI{PjVzNESz
H1299NHXZO45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NWnJW5BJOC1|MDFOwG0>NWi3VIltPzJiaB?=M4Xk[WROW09?M{CzSGlEPTB;MT64NEDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJINwdmOnboTyZZRqd25iZHXw[Y5l\W62bIm=NWPOd3BbOjN4NUG0OFM>
A549NEP3bFBHfW6ldHnvckBCe3OjeR?=NGX1T20yNzFyIN88US=>NVXOOVdbPDhiaB?=MWPEUXNQNV;oS4Z1dGWjZIOgeI8h[SCmb4PlMYRmeGWwZHXueEBl\WO{ZXHz[UBqdiCQb4TjbEBz\XCxcoTldkBi[3Srdnn0fS=>M33xV|I{PjVzNESz
LNCapM4fMXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M2LrOFAuOzBizszNNW\jfZFuPCCmNYjvXWltUUN3ME20MlU6yqEQvF2=MV[yNlg{OjNzNh?=
A431 NHnI[49HfW6ldHnvckBCe3OjeR?=M{fCZVExKM7:TR?=NHi5VZg{OCCvaX6=NXrYW|l1[XS2ZX71ZZRmeyCSSUPLMWFsfC2vVF;SJJNq\26jbHnu[y=>NHHxdGEzOjN6N{m4PC=>
H2170 NYHIO2E5TnWwY4Tpc44hSXO|YYm=MmXLNVAh|ryPMVqzNEBucW5?MkTtZZR1\W63YYTld{BRUTONLVHreE1uXE:UIIPp[45idGmwZx?=M1\wfFIzOzh5OUi4
A431 NHq5PYFHfW6ldHnvckBCe3OjeR?=MY[xNEDPxE1?M3Pjc|QuOjRiaB?=M3naOYVvcGGwY3XzJIFxd3C2b4Ppd{B4cXSqIHXycI91cW6rYh?=MlPCNlI{QDd7OEi=
H2170 MmjOSpVv[3Srb36gRZN{[Xl?NH3teXcyOCEQvF2=MXS0MVI1KGh?Mmj5[Y5p[W6lZYOgZZBweHSxc3nzJJdqfGhiZYLsc5RqdmmkNULvbZJYOjJ|OEe5PFg>

... 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]
Features First clinical inhibitor of CK2.

Protocol(Only for Reference)

Kinase Assay: [2]

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 Assay: [1]

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.

Animal Study: [1]

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

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Siddiqui-Jain A, et al. Cancer Res, 2010, 70(24), 10288-10298.

[2] Pierre F, et al. J Med Chem, 2011, 54(2), 635-654.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-06-18)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02128282 Recruiting Cholangiocarcinoma Senhwa Biosciences, Inc. June 2014 Phase 1|Phase 2
NCT01199718 Recruiting Multiple Myeloma Cylene Pharmaceuticals September 2010 Phase 1
NCT00891280 Recruiting Advanced Solid Tumors|Breast Cancer|Inflammatory Breast Cancer|Castlemans Disease|Multiple Myeloma Cylene Pharmaceuticals February 2009 Phase 1

Chemical Information

Download CX-4945 (Silmitasertib) SDF
Molecular Weight (MW) 349.77
Formula

C19H12ClN3O2

CAS No. 1009820-21-6
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 16 mg/mL (45.74 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo
* <1 mg/ml means slightly soluble or insoluble.
* 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 Name 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid

Customer Product Validation(4)


Click to enlarge
Rating
Source Nat Commun 2014 5, 3393. CX-4945 (Silmitasertib) purchased from Selleck
Method Western blot
Cell Lines HUT102 and KK1 cells
Concentrations 1 uM
Incubation Time 24 h
Results CX-4945 decreasedPTEN-Ser370, a bona fide CK2 substrate<SUP>26</SUP>, and AKT-Ser473 phosphorylation.

Click to enlarge
Rating
Source Oncotarget, 2015, 51: S659-S660. CX-4945 (Silmitasertib) purchased from Selleck
Method Immunofluorescence Analysis
Cell Lines RS4;11cells
Concentrations 5 µM
Incubation Time 22 h
Results In RS4;11 samples combined treatment induces Ser536 p-NF-κB nuclear translocation (see white arrows).

Click to enlarge
Rating
Source Cell Signal 2014 26(7), 1567-75. CX-4945 (Silmitasertib) purchased from Selleck
Method Protein kinase CK2 assay
Cell Lines ARPE-19 cells
Concentrations 5, 10, 20 uM
Incubation Time 24, 49 h
Results CX-4945 efficiently inhibits CK2 kinase activity in ARPE-19 cells.

Click to enlarge
Rating
Source Cell Signal 2014 26(7), 1567-75. CX-4945 (Silmitasertib) purchased from Selleck
Method Western blot
Cell Lines HCT116 cells
Concentrations 10 uM
Incubation Time 24, 48 h
Results CX-4945 induces apoptosis in HCT116 cells.

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.

Tel: +1-832-582-8158 Ext:3

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1  Questions/Answers

Is CX-4945 taken up and effective in yeast cells?

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Currently, no publication reports test of CX-4945 on yeast cells. However, the co-crystal structure of CX-4945 with human CK2 alpha subunit is available. You can check to see if the domains that interact with CX-4945 are conserved between human and yeast. If yes, you may see an effect in yeast cells.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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