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

CX-4945 (Synonyms: Silmitasertib)

Cat. No.: HY-50855 Purity: 98.08%
Data Sheet SDS Handling Instructions

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.
CX-4945 Chemical Structure

CX-4945 Chemical Structure

CAS No. : 1009820-21-6

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $88 In-stock
5 mg $80 In-stock
10 mg $130 In-stock
50 mg $350 In-stock
100 mg $550 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Other Forms of CX-4945:

    CX-4945 purchased from MCE. Usage Cited in: Oncol Rep. 2017 Feb;37(2):1141-1147.

    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.

    CX-4945 purchased from MCE. Usage Cited in: Science. 2017 Dec 1;358(6367). pii: eaan4368.

    Kinobead western Blot readout for selected inhibitor:protein combinations.

    CX-4945 purchased from MCE. Usage Cited in: Science. 2017 Dec 1;358(6367). pii: eaan4368.

    Immunoblot analysis in MV-4-11 cells and MOLM-13, FLT3-WT and FLT3-ITD transfected HEK293 cells, and Ba/F3 FLT3-ITD cells revealed FLT3 target engagement for Golvatinib and Cabozantinib.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

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

    IC50 & Target

    IC50: 1 nM (CK2α), 1 nM (CK2α')

    In Vitro

    CX-4945 causes cell-cycle arrest and selectively induced apoptosis in cancer cells relative to normal cells, attenuates PI3K/Akt signalingand, and the antiproliferative activity of CX-4945 is correlated with expression levels of the CK2α catalytic subunit, Attenuation of PI3K/Akt signaling[1]. CX-4945 with bortezomib treatment prevents leukemic cells from engaging a functional UPR in order to buffer the bortezomib-mediated proteotoxic stress in ER lumen, and decreases pro-survival ER chaperon BIP/Grp78 expression[2]. 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].

    In Vivo

    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]

    Clinical Trial
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    References
    Preparing Stock Solutions
    Concentration Volume 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.
    Kinase Assay
    [1]

    The percent inhibition of each kinase is estimated using 0.5 μM CX-4945 at ATP concentrations equivalent to the Km value for ATP for each respective human recombinant kinase. The determination of IC50 values is done at ATP concentrations equivalent to the Km for ATP for each kinase using 9 concentrations of CX-4945 over a range of 0.0001 to 1 μM. The Ki value (inhibition constant) for CX-4945 against recombinant CK2 is determined by graphing the IC50 values of CX-4945 determined in the presence of various concentrations of ATP against the concentration of ATP. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [1]

    CX-4945 is dissolved in DMSO at a concentration of 5 mM.

    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 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. 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
    Molecular Weight

    349.77

    Formula

    C₁₉H₁₂ClN₃O₂

    CAS No.

    1009820-21-6

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 35 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Purity: 98.08%

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    Product Name:
    CX-4945
    Cat. No.:
    HY-50855
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