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CFI-400945 fumarate,1616420-30-4

产品信息

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    YZ剂描述：

    产品名称：CFI-400945 fumarate

    产品别名：见爱必信官网

    英文别名：CFI-400945 fumarate

    靶点：PLK

    CAS：1616420-30-4

    纯度：98%

    外观：见爱必信官网

    保存方法：store at -20℃ for one year（Powder）

    描述：CFI-400945 fumarate is a potent, selective and orally bioavailable PLK4 inhibitor with a Ki and an IC50 of 0.26 nM and 2.8 nM, respectively.

    溶解性：

    In Vitro: 

    DMSO : 50 mg/mL (76.84 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    ConcentrationSolventMass1 mg5 mg10 mg
    1 mM1.5368 mL7.6838 mL15.3676 mL
    5 mM0.3074 mL1.5368 mL3.0735 mL
    10 mM0.1537 mL0.7684 mL1.5368 mL
    *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，并请注意储备液的保存方式和期限。
    In Vivo:

    请根据您的实验动物和给YF式选择适当的溶解方案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的工作
    液，建议您现用现配，当天使用；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分比是指该溶剂在您配制终溶液中的体积占比)：

    • 1.

      请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (3.84 mM); Clear solution

    • 2.

      请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (3.84 mM); Clear solution

    • 3.

      请依序添加每种溶剂： 10% DMSO    90% corn oil

      Solubility: 2.5 mg/mL (3.84 mM); Clear solution; Need warming

    *

    体外研究：

    CFI-400945 (compound 48) shows potent inhibitory activities against a panel of kinases, including PLK4, TRKA, TRKB, AURKA, AURKB/INCENP, and TIE2/TEK, with IC50s of 2.8, 6, 9, 140, 98, 22 nM, and EC50s of 12, 84, 88, 510, 102, 117 nM, respectively. CFI-400945 exhibits growth inhibition effects on breast, lung, ovarian and colon cancer cells. The IC50s (in μM) are as follows: SKBr-3 (5.3), Cal-51 (0.26), BT-20 (0.058), A549 (0.005), OVCAR-3 (0.018), SW620 (0.38), Colo-205 (0.017), and HCT116+/+ (0.004) . CFI-400945 inhibits autophosphorylation of PLK4 at serine 305 with an EC50 value of 12.3 nM in cells overexpressing PLK4. Cancer cells treated with CFI-400945 exhibit effects consistent with PLK4 kinase inhibition, including dysregulated centriole duplication, mitotic defects, and cell death.

    体内研究：CFI-400945 (compound 48) shows potent inhibitory activities against a panel of kinases, including PLK4, TRKA, TRKB, AURKA, AURKB/INCENP, and TIE2/TEK, with IC50s of 2.8, 6, 9, 140, 98, 22 nM, and EC50s of 12, 84, 88, 510, 102, 117 nM, respectively. CFI-400945 exhibits growth inhibition effects on breast, lung, ovarian and colon cancer cells. The IC50s (in μM) are as follows: SKBr-3 (5.3), Cal-51 (0.26), BT-20 (0.058), A549 (0.005), OVCAR-3 (0.018), SW620 (0.38), Colo-205 (0.017), and HCT116+/+ (0.004) . CFI-400945 inhibits autophosphorylation of PLK4 at serine 305 with an EC50 value of 12.3 nM in cells overexpressing PLK4. Cancer cells treated with CFI-400945 exhibit effects consistent with PLK4 kinase inhibition, including dysregulated centriole duplication, mitotic defects, and cell death.

    产品信息订购：

      产品货号   产品名称   规格 价格 大包装及货期
      abs821017   CFI-400945 fumarate   5mg  1320   立即咨询

    产品更多信息请进入爱必信网站咨询

    温馨提示：不可用于临床ZL。
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