2. Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR
  3. Ack1 Akt
  4. Ack1 inhibitor 1

Ack1 inhibitor 1 是一种有效的，选择性的，具有口服活性的ACK1激酶抑制剂，其 IC50 值为 2.1 nM。Ack1 inhibitor 1 抑制 ACK1 的磷酸化和下游 AKT 的激活。Ack1 inhibitor 1 具有抗肿瘤活性。

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Ack1 inhibitor 1 Chemical Structure

Ack1 inhibitor 1 Chemical Structure

CAS No. : 2924415-92-7

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Ack1 inhibitor 1 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Ack1 inhibitor 1 is a potent, selective, and orally active inhibitor of ACK1 kinase with an IC50 value of 2.1 nM. Ack1 inhibitor 1 inhibits the phosphorylation of ACK1 and activation of downstream AKT. Ack1 inhibitor 1 has anti-tumor activity[1].

体外研究
(In Vitro)

Ack1 inhibitor 1 (Compound 10zi) 在 67R 和 H1975 细胞中抑制细胞生长的 IC50 分别为 3.71 μM 和 4.18 μM[1]。
Ack1 inhibitor 1 (0 nM-5000 nM, 72 h) 在 67R 细胞中单独或与 ASK120067 联合均可增强抗肿瘤作用[1]。
Ack1 inhibitor 1 (1 μM and 5 μM, 6 h) 呈剂量依赖性抑制 67R 细胞中 ACK1 和 AKT 的磷酸化[1]。

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

Ack1 inhibitor 1 相关抗体:

Cell Viability Assay[1]

Cell Line: 67R cells (ASK120067-resistant cells obtained from parental H1975 cells by a dose escalation method).
Concentration: 0-5000 nM (combined with ASK120067)
Incubation Time: 72 h
Result: Caused strong synergistic anti-growth effects on 67R cells with high synergy scores of 10.83, respectively

Western Blot Analysis[1]

Cell Line: 67R cells
Concentration: 1 μM and 5 μM
Incubation Time: 6 h (stimulated with or without EGF for 30 min)
Result: Caused moderate down-regulation of p-ACK1 and p-AKT at 1 μM.
Exhibited better potency against p-AKT, while it was unable to completely inhibit p-ACK1 at 5 μM.
体内研究
(In Vivo)

Ack1 inhibitor 1 (Compound 10zi) (10 mg/kg; 口服; 单次剂量) 在SD大鼠中 AUC 值为 1920.56 h•ng/mL, Cmax 值为 119.52 μg/L，生物利用度为 19.80%

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

727.77

Formula

C39H40F3N7O4
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.
溶解性数据

  • 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

动物实验：

以下溶解方案源自文献，仅供参考，建议您先取少量样品进行尝试。

  • 方案 一

    Ack1 inhibitor 1 dissolve in 5% DMSO + 10% Solutol + 85% (10% HP-β-CD in Saline)[1]

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

只
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

Ack1 inhibitor 1 相关分类

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:

Ack1 inhibitor 12924415-92-7Ack1AktActivated Cdc42 kinase 1TNK2PKBProtein kinase Borally activeantitumorH1975 cells67R cellsInhibitorinhibitorinhibit

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