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

Silmitasertib  (Synonyms: CX-4945)

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

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

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Solid + Solvent
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
5 mg USD 96 In-stock
10 mg USD 156 In-stock
50 mg USD 420 In-stock
100 mg USD 660 In-stock
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500 mg   Get quote  

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Customer Review

Based on 31 publication(s) in Google Scholar

Other Forms of Silmitasertib:

Top Publications Citing Use of Products

29 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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    • Biological Activity

    • Protocol

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    • 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.

    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)

    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
    10 mM 0.2859 mL 1.4295 mL 2.8590 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 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

    *All of the co-solvents are available by MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.94%

    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
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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.

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    Product Name:
    Silmitasertib
    Cat. No.:
    HY-50855
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