2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  3. HSP
  4. Onalespib lactate

Onalespib lactate  (Synonyms: AT13387 lactate)

目录号: HY-113916
产品使用指南

摩尔计算器

Onalespib lactate 是一种有效的穿过血脑屏障的 heat-shock-protein-90 (Hsp90) 抑制剂，Kd 值为 0.71 nM。Onalespib lactate 抑制细胞增殖、存活和迁移。Onalespib lactate 降低 EGFR、p-EGFR、AKT、P-AKT、ERK1/2、P-ERK1/2、S6、P-S6 蛋白的表达。Onalespib lactate 具有抗肿瘤活性。Onalespib 具有非小细胞肺癌 (NSCLC) 研究的潜力。

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Onalespib lactate Chemical Structure

Onalespib lactate Chemical Structure

CAS No. : 1019889-35-0

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Onalespib lactate 的其他形式现货产品:

Customer Review

Other Forms of Onalespib lactate:

Onalespib lactate 相关抗体

Top Publications Citing Use of Products

    Onalespib lactate purchased from MCE. Usage Cited in: Sci Rep. 2017 Mar 15;7(1):201.  [Abstract]

    For the caspase 3/7 assay, the HSP90 inhibitor-treated 5637 or SV-HUC cells are stained with Nexcelom ViaStain Caspase 3/7 reagent and Hoechst 33342. Caspase 3/7 positive cells are identified using the Celigo imaging cytometer, and the percentage of apoptotic caspase 3/7 positive cells is calculated with the Celigo software.

    查看 HSP 亚型特异性产品:

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    HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Onalespib lactate is a potent and cross the blood-brain barrier heat-shock-protein-90 (Hsp90) inhibitor with an Kd value of 0.71 nM. Onalespib lactate inhibits the proliferation, survival and migration. Onalespib lactate decreases the expression of EGFR, p-EGFR, AKT, P-AKT, ERK1/2, P-ERK1/2, S6, P-S6 protein. Onalespib lactate shows antitumor activity. Onalespib lactate has the potential for the research of non-small cell lung cancer (NSCLC)[1][2][3][4].

    IC50 & Target[4]

    HSP90

    0.71 nM (Kd)

    体外研究
    (In Vitro)

    Onalespib lactate (0-0.4 µM; 72 h, 48 h) 抑制神经胶质瘤细胞的增殖、存活和迁移[2]。
    Onalespib lactate (0-0.4 µM; 48 h) 以剂量依赖性方式降低 EGFR、p-EGFR、AKT、P-AKT、ERK1/2、P-ERK1/2、S6、P-S6 蛋白的表达[2]。

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

    Onalespib lactate 相关抗体:

    Cell Proliferation Assay[2]

    Cell Line: LN229, U251 and A172 cells
    Concentration: 0.1, 0.2, 0.4 µM
    Incubation Time: 72 h
    Result: Inhibited cell proliferation in a dose-dependent manner.

    Western Blot Analysis[2]

    Cell Line: LN229, U251 and A172 cells
    Concentration: 0.1, 0.2, 0.4 µM
    Incubation Time: 48 h
    Result: Decreased the expression of EGFR, p-EGFR, AKT, P-AKT, ERK1/2, P-ERK1/2, S6, P-S6 protein in a dose-dependent manner.
    体内研究
    (In Vivo)

    Onalespib lactate (30 mg/kg；i.v.；一次) 可穿过血脑屏障 (BBB) 并在 6 周龄 ICR 小鼠中引起 HSP90 的持续抑制[2]。
    Onalespib lactate (0.5 µM；移植后 5 至 10 天) 和 TMZ (HY-17364) (10 µM) 可减少斑马鱼胚胎中的肿瘤生长并延长存活期[2]。
    Onalespib lactate (5、10 mg/kg 用于 HCT116 异种移植物，20 mg/kg 用于 A431 异种移植物；i.p.；每天一次，持续 3 天) 在 HCT116 和 A431 异种移植物中显示出抗肿瘤活性[3]。

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

    Animal Model: Female nu/nu Balb/c mice (HCT116 and A431 xenografts)[3]
    Dosage: 5, 10 mg/kg for HCT116 xenografts, 20 mg/kg for A431 xenografts
    Administration: I.p.; on day 1, 2, and 3 days
    Result: Inhibited tumor growth and had a median survival of 9.5 days and the maximum survival was 14 days in HCT116 xenografts, reduced the tumor size significantly by 32% in A431 xenografts.
    Clinical Trial
    分子量

    499.60

    Formula

    C27H37N3O6
    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

    Onalespib lactate 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:

    Onalespib1019889-35-0AT13387AT 13387AT-13387HSPHeat shock proteinscross the blood-brain barrierantitumorproliferationmigrationLN229U251A172 cellsEGFRInhibitorinhibitorinhibit

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    目录号：
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