2. Cell Cycle/DNA Damage Epigenetics Autophagy Apoptosis
  3. Aurora Kinase Autophagy Apoptosis
  4. Alisertib sodium

Alisertib sodium  (Synonyms: MLN 8237 sodium)

目录号: HY-10971A
产品使用指南

摩尔计算器

Aliertib (MLN 8237) sodium 是一种口服活性和选择性的 Aurora A 激酶抑制剂 (IC50=1.2 nM)，与Aurora A 激酶结合，导致有丝分裂纺锤体异常、有丝分裂累积。Aliertib sodium 通过靶向白血病细胞中的 AKT/mTOR/AMPK/p38 途径诱导其凋亡和自噬。具有抗肿瘤活性。

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Alisertib sodium Chemical Structure

Alisertib sodium Chemical Structure

CAS No. : 1028486-06-7

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Alisertib sodium 的其他形式现货产品:

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Alisertib sodium 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 45 篇科研文献

IF
IHC
WB

    Alisertib sodium purchased from MCE. Usage Cited in: FASEB J. 2018 May;32(5):2735-2746.  [Abstract]

    Representative immunofluorescence (IF) image and graph with frequency of ciliated WT or Pkd12/2 murine renal epithelial cells at 2 h after treatment with vehicle (V), Ganetespib (G), or Alisertib (A) to inhibit AURKA, or (C) combination of Alisertib and Ganetespib. On IF, acetylated a-tubulin (red); g-tubulin (green); DAPI (blue).

    Alisertib sodium purchased from MCE. Usage Cited in: College of Medicine. Drexel University. 2016 Nov.

    Alisertib and combination treatment suppress proliferation in BT474 orthotopic tumors as shown by decrease in Ki-67, which is statistically significantly different between vehicle and combination treatment, FRAX1036 and Alisertib, and FRAX1036 and combination treatment.

    Alisertib sodium purchased from MCE. Usage Cited in: College of Medicine. Drexel University. 2016 Nov.

    Alisertib enhances FRAX1036 inhibitory effect on PAK1 phosphorylation in BT474 xenograft model.

    查看 Aurora Kinase 亚型特异性产品:

    查看所有亚型
    Aurora Kinase Aurora A Aurora B Aurora C

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Alisertib (MLN 8237) sodium is an orally active and selective Aurora A kinase inhibitor (IC50=1.2 nM), which binds to Aurora A kinase resulting in mitotic spindle abnormalities, mitotic accumulation. Alisertib sodium induces apoptosis and autophagy through targeting the AKT/mTOR/AMPK/p38 pathway in leukemic cells. Antitumor activity[1][2][3].

    IC50 & Target[3]

    Aurora A

    12.5 nM (IC50)

    Aurora B

    396.5 nM (IC50)

    体外研究
    (In Vitro)

    Alisertib (MLN 8237) leads the MM cells to mitotic spindle abnormalities, mitotic accumulation, as well as inhibition of cell proliferation through apoptosis and senescence. Alisertib up-regulates p53 and tumor suppressor genes p21 and p27[1].
    The decreased activity of Alisertib (MLN 8237) for the T217D/W277E Aurora A/TPX2 complex may reflect the increased affinity for ATP induced by cofactor binding to Aurora A[2].
    Alisertib (MLN 8237) inhibits cell proliferation with IC50s ranging from 15 to 469 nM in different tumer cell lines[4].

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

    Alisertib sodium 相关抗体:
    体内研究
    (In Vivo)

    Alisertib (MLN 8237) (30 mg/kg, p.o.) significantly reduces tumor burden and increases overall survival in xenograft-murine model of human-MM[1].
    Alisertib (3-30 mg/kg; P.o.; once daily for 3 weeks) causes tumor growth inhibition in solid tumor xenograft models[4].

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

    Animal Model: Nude mice bearing HCT-116 colon tumor xenograft[4]
    Dosage: 3, 10, or 30 mg/kg
    Administration: P.o.; once daily for 3 weeks
    Result: Resulted in a dose-dependent TGI (tumor growth inhibition) of 43.3%, 84.2%, and 94.7% for the 3, 10, and 30 mg/kg groups,respectively.
    Clinical Trial
    分子量

    540.91

    Formula

    C27H19ClFN4NaO4
    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

    Alisertib sodium 相关分类

    • 摩尔计算器

    • 稀释计算器

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    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.

    Keywords:

    Alisertib1028486-06-7MLN 8237MLN8237MLN-8237Aurora KinaseAutophagyApoptosiscytotoxicitycell-cyclearrestmultiplemyelomamitoticspindlecancerInhibitorinhibitorinhibit

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