2. Cell Cycle/DNA Damage Stem Cell/Wnt Autophagy
  3. Casein Kinase Autophagy
  4. Silmitasertib

Silmitasertib  (Synonyms: CX-4945)

Cat. No.: HY-50855 Purity: 99.94%
COA Handling Instructions

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Silmitasertib (CX-4945) is an orally bioavailable, highly selective and potent CK2 inhibitor, with IC50 values of 1 nM against CK2α and CK2α'.

For research use only. We do not sell to patients.

Silmitasertib Chemical Structure

Silmitasertib Chemical Structure

CAS No. : 1009820-21-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 106 In-stock
Solution
10 mM * 1 mL in DMSO USD 106 In-stock
Solid
1 mg USD 38 In-stock
5 mg USD 96 In-stock
10 mg USD 156 In-stock
50 mg USD 420 In-stock
100 mg USD 660 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 39 publication(s) in Google Scholar

Other Forms of Silmitasertib:

Silmitasertib Related Antibodies

Top Publications Citing Use of Products

37 Publications Citing Use of MCE Silmitasertib

WB

    Silmitasertib purchased from MedChemExpress. Usage Cited in: Oncol Rep. 2017 Feb;37(2):1141-1147.  [Abstract]

    CX-4945 increases the expression of apoptosis markers. Western blot analysis reveals that CX-4945 treatment increases the expression of cleaved PARP or cleaved caspase-3. CX-4945 treatment decreases the expression of Bcl-2 or Bcl-xL. The experiment is performed in triplicate, producing similar results.

    Silmitasertib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 Aug 16;7(33):53191-53203.  [Abstract]

    MPNST cell lines show a decrease in CK2 activity in response to escalating CX-4945 concentrations (24 h) as measured by a western blot analysis using anti-CK2 substrate, and to undergo apoptosis as indicated by increased cleaved PARP.

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    CK1 CK2

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Silmitasertib (CX-4945) is an orally bioavailable, highly selective and potent CK2 inhibitor, with IC50 values of 1 nM against CK2α and CK2α'.

    IC50 & Target[1]

    CK2α

    1 nM (IC50)

    CK2α'

    1 nM (IC50)

    In Vitro

    Silmitasertib (CX-4945) causes cell-cycle arrest and selectively induces apoptosis in cancer cells relative to normal cells, attenuates PI3K/Akt signalingand, and the antiproliferative activity of Silmitasertib (CX-4945) is correlated with expression levels of the CK2α catalytic subunit, Attenuation of PI3K/Akt signaling[1]. Silmitasertib (CX-4945) with PS-341 treatment prevents leukemic cells from engaging a functional UPR in order to buffer the PS-341-mediated proteotoxic stress in ER lumen, and decreases pro-survival ER chaperon BIP/Grp78 expression[2]. Silmitasertib (CX-4945) induces cytotoxicity and apoptosis, and exerts anti-proliferative effects in hematological tumors by downregulating CK2 expression and suppressing activation of CK2-mediated PI3K/Akt/mTOR signaling pathways[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Silmitasertib Related Antibodies
    In Vivo

    Silmitasertib (CX-4945) (25 or 75 mg/kg, p.o.) is well tolerated and demonstrated robust antitumor activity with concomitant reductions of the mechanism-based biomarker phospho-p21 (T145) in murine xenograft models[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    349.77

    Formula

    C19H12ClN3O2
    CAS No.
    Appearance

    Solid

    Color

    Yellow to orange

    SMILES

    O=C(C1=CC=C2C3=C(C(NC4=CC=CC(Cl)=C4)=NC2=C1)C=CN=C3)O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 35 mg/mL (100.07 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    0.1 M NaOH : 33.33 mg/mL (95.29 mM; ultrasonic and adjust pH to 9 with NaOH)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.8590 mL 14.2951 mL 28.5902 mL
    5 mM 0.5718 mL 2.8590 mL 5.7180 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: 2.08 mg/mL (5.95 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.08 mg/mL (5.95 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.94%

    COA (246 KB) LCMS (98 KB) Elemental Analysis Report (105 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [1]

    Various cell lines are seeded at a density of 3,000 cells per well 24 hours prior to treatment, in appropriate media, and then treated with indicated concentrations of Silmitasertib (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.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Xenografts are initiated by subcutaneous injection of BxPC-3 cells into the right hind flank region of each mouse or BT-474 cells are injected into the mammary fat pad of mice implanted with estrogen pellets. When tumors reach a designated volume of 150-200 mm3, animals are randomized and divided into groups of 9 to 10 mice per group. Silmitasertib (CX-4945) is administered by oral gavage twice daily at 25 or 75 mg/kg for 31 and 35 consecutive days for the BT-474 and BxPC-3 models, respectively. Tumor volumes and body weights are measured twice weekly. The length and width of the tumor are measured with calipers and the volume calculated using the following formula: tumor volume=(length × width2)/2.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    0.1 M NaOH / DMSO 1 mM 2.8590 mL 14.2951 mL 28.5902 mL 71.4755 mL
    5 mM 0.5718 mL 2.8590 mL 5.7180 mL 14.2951 mL
    10 mM 0.2859 mL 1.4295 mL 2.8590 mL 7.1476 mL
    15 mM 0.1906 mL 0.9530 mL 1.9060 mL 4.7650 mL
    20 mM 0.1430 mL 0.7148 mL 1.4295 mL 3.5738 mL
    25 mM 0.1144 mL 0.5718 mL 1.1436 mL 2.8590 mL
    30 mM 0.0953 mL 0.4765 mL 0.9530 mL 2.3825 mL
    40 mM 0.0715 mL 0.3574 mL 0.7148 mL 1.7869 mL
    50 mM 0.0572 mL 0.2859 mL 0.5718 mL 1.4295 mL
    60 mM 0.0477 mL 0.2383 mL 0.4765 mL 1.1913 mL
    80 mM 0.0357 mL 0.1787 mL 0.3574 mL 0.8934 mL
    DMSO 100 mM 0.0286 mL 0.1430 mL 0.2859 mL 0.7148 mL
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    Silmitasertib Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Silmitasertib1009820-21-6CX-4945CX4945CX 4945Casein KinaseAutophagyInhibitorinhibitorinhibit

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