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  3. XL413 hydrochloride

XL413 hydrochloride 

Cat. No.: HY-15260A Purity: 99.72%
Handling Instructions

XL413 hydrochloride is a potent, selective and ATP competitive inhibitor of Cdc7, with an IC50 of 3.4 nM, and also shows potent effect with IC50s of 215, 42 nM on CK2, PIM1, respectively, and an EC50 of 118 nM on pMCM.

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

XL413 hydrochloride Chemical Structure

XL413 hydrochloride Chemical Structure

CAS No. : 2062200-97-7

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Customer Review

Based on 4 publication(s) in Google Scholar

Top Publications Citing Use of Products

    XL413 hydrochloride purchased from MCE. Usage Cited in: Am J Physiol Lung Cell Mol Physiol. 2018 Sep 1;315(3):L360-L370.

    Representative Western blot for Endo180 expression in U937 cells treated overnight with XL413.
    • Biological Activity

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    Description

    XL413 hydrochloride is a potent, selective and ATP competitive inhibitor of Cdc7, with an IC50 of 3.4 nM, and also shows potent effect with IC50s of 215, 42 nM on CK2, PIM1, respectively, and an EC50 of 118 nM on pMCM.

    IC50 & Target[1]

    Cdc7

    3.4 nM (IC50)

    PIM1

    42 nM (IC50)

    CK2

    215 nM (IC50)

    In Vitro

    XL413 inhibits the cell proliferation (IC50 = 2685 nM), decreases cell viability (IC50 = 2142 nM) and elicits the caspase 3/7 activity (EC50 = 2288 nM) in Colo-205 cells. XL413 also significantly inhibits the anchorage-independent growth of colo-205 in soft agar (IC50 = 715 nM)[1]. XL413 shows cytotoxic effects on tumors, with IC50 of 22.9 µM in HCC1954 cells and 1.1 µM in Colo-205 cells. XL413 induces apoptosis in the Colo-205 cells, but not in HCC1954 cells. XL413 is effective DDK inhibitors in vitro, with IC50 of 22.7 nM. XL413 is defective in inhibiting DDK-dependent Mcm2 phosphorylation in HCC1954 cells but is effective in Colo-205 cells[2].

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

    In Vivo

    XL413 (100 mg/kg, p.o.) shows excellent plasma exposures in mice and possesses good PK properties. XL413 (10, 30, or 100 mg/kg, p.o.) is well tolerated at all the doses, with no significant body weight loss[1].

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

    Molecular Weight

    326.18

    Formula

    C₁₄H₁₃Cl₂N₃O₂

    CAS No.

    2062200-97-7

    SMILES

    O=C1C(OC2=CC=C(Cl)C=C23)=C3N=C([[email protected]]4NCCC4)N1.[H]Cl

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    H2O : 10 mg/mL (30.66 mM; Need ultrasonic)

    DMSO : 3.4 mg/mL (10.42 mM; Need ultrasonic and warming)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.0658 mL 15.3290 mL 30.6579 mL
    5 mM 0.6132 mL 3.0658 mL 6.1316 mL
    10 mM 0.3066 mL 1.5329 mL 3.0658 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Kinase Assay
    [2]

    20 ng of purified human DDK is pre-incubated with increasing concentrations of each DDK inhibitor for 5 min. Then 10 µCi (γ)-32P ATP and 1.5 µM cold ATP are added in a buffer containing 50 mM Tris-HCl (pH 7.5), 10 mM MgCl2, and 1 mM DTT and incubated for 30 min at 30°C. The proteins are denatured in 1X Laemmli buffer at 100°C followed by SDS-PAGE and autoradiography on HyBlot CL film. Auto-phosphorylation of DDK is used as an indicator of its kinase activity. 32P-labeled bands are quantified using ImageJ and the IC50 values are calculated using GraphPad.

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

    Cell Assay
    [2]

    For assays in 96 well plates 2500 cells are plated per well. After 24 hours, cells are treated with small molecule inhibitors and incubated for 72 hours at 37°C. Subsequently the cells are lysed and the ATP content is measured as an indicator of metabolically active cells using the CellTiter-Glo assay. IC50 values are calculated using the GraphPad software. For assays in six well plates, 100,000 cells are plated per well. After 24 hours, cells are treated with small molecule inhibitors and incubated for varying time points. Cells are trypsinized and a suspension is made in 5 mL of phosphate buffered saline. 30 µL of this suspension is mixed with 30 µL of CellTiter-Glo reagent followed by a 10-minute incubation at room temperature. Luminescence is measured using EnVision 2104 Multilabel Reader and BioTek Synergy Neo Microplate Reader.

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

    References
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    Keywords:

    XL413XL 413XL-413CDKCyclin dependent kinaseInhibitorinhibitorinhibit

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    Product Name:
    XL413 hydrochloride
    Cat. No.:
    HY-15260A
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