1. Cell Cycle/DNA Damage
  2. CDK
  3. XL413

XL413 是一种有效的,选择性的,ATP 竞争性的 Cdc7 抑制剂,IC50 值为 3.4 nM,同时对 CK2 和 PIM1 的 IC50 值分别为 215 和 42 nM,对 pMCM 的 EC50 值为 118 nM。

在相同的摩尔浓度下,化合物盐形式与游离形式有相同的生物活性,但盐形式 XL413 monohydrochloride 通常具有更好的水溶性和稳定性。

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XL413 Chemical Structure

XL413 Chemical Structure

CAS No. : 1169558-38-6

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XL413 的其他形式现货产品:

Other Forms of XL413:

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

    Representative Western blot for Endo180 expression in U937 cells treated overnight with XL413.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    XL413 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)

    体外研究
    (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.

    体内研究
    (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.

    分子量

    289.72

    Formula

    C14H12ClN3O2

    CAS 号
    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    Please store the product under the recommended conditions in the Certificate of Analysis.

    纯度 & 产品资料
    参考文献
    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.

    参考文献

    XL413 相关分类

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    • 稀释计算器

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    • 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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    产品名称:
    XL413
    目录号:
    HY-15260
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