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  3. XL413 monohydrochloride

XL413 monohydrochloride  (Synonyms: BMS-863233 monohydrochloride)

目录号: HY-15260A 纯度: 99.72%
COA 产品使用指南

XL413 (BMS-863233) hydrochloride 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 CK2PIM1IC50 值分别为 215 和 42 nM,对 pMCM 的 EC50 值为 118 nM。

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XL413 monohydrochloride Chemical Structure

XL413 monohydrochloride Chemical Structure

CAS No. : 2062200-97-7

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥4880
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1 mg ¥604
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5 mg ¥1330
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10 mg ¥1860
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50 mg ¥5580
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Customer Review

Other Forms of XL413 monohydrochloride:

    XL413 monohydrochloride 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 (BMS-863233) 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)

    体外研究
    (In Vitro)

    XL413 (BMS-863233) hydrochloride 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 hydrochloride also significantly inhibits the anchorage-independent growth of colo-205 in soft agar (IC50=715 nM)[1].
    XL413 hydrochloride shows cytotoxic effects on tumors, with IC50 of 22.9 µM in HCC1954 cells and 1.1 µM in Colo-205 cells. XL413 hydrochloride 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 hydrochloride 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 (BMS-863233; 100 mg/kg, p.o.) hydrochloride shows excellent plasma exposures in mice and possesses good PK properties. XL413 (10, 30, or 100 mg/kg, p.o.) hydrochloride 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

    326.18

    Formula

    C14H13Cl2N3O2

    CAS 号
    性状

    固体

    颜色

    White to off-white

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

    溶解性数据
    细胞实验: 

    H2O 中的溶解度 : 10 mg/mL (30.66 mM; 超声助溶)

    DMSO 中的溶解度 : 3.4 mg/mL (10.42 mM; 超声加热助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 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
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    • 摩尔计算器

    • 稀释计算器

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

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    计算结果
    工作液所需浓度 : mg/mL
    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

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO / H2O 1 mM 3.0658 mL 15.3290 mL 30.6579 mL 76.6448 mL
    5 mM 0.6132 mL 3.0658 mL 6.1316 mL 15.3290 mL
    10 mM 0.3066 mL 1.5329 mL 3.0658 mL 7.6645 mL
    H2O 15 mM 0.2044 mL 1.0219 mL 2.0439 mL 5.1097 mL
    20 mM 0.1533 mL 0.7664 mL 1.5329 mL 3.8322 mL
    25 mM 0.1226 mL 0.6132 mL 1.2263 mL 3.0658 mL
    30 mM 0.1022 mL 0.5110 mL 1.0219 mL 2.5548 mL

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    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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    产品名称:
    XL413 monohydrochloride
    目录号:
    HY-15260A
    需求量: