1. GPCR/G Protein MAPK/ERK Pathway
  2. Ras
  3. TH-Z827

TH-Z827 是一种突变型选择性 KRAS(G12D) 抑制剂,IC50 为 2.4 μM。TH-Z827 不结合 KRAS(WT) 或 KRAS(G12C)。TH-Z827 阻断 KRAS(G12D)-CRAF 相互作用,IC50 值为 42 μM。

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TH-Z827 Chemical Structure

TH-Z827 Chemical Structure

CAS No. : 2847881-81-4

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  • 生物活性

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  • 参考文献

生物活性

TH-Z827 is a mutant selective KRAS(G12D) inhibitor with an IC50 of 2.4 μM. TH-Z827 does not bind KRAS(WT) or KRAS(G12C). TH-Z827 blocked the KRAS(G12D)-CRAF interaction with an IC50 value of 42 μM[1].

IC50 & Target[1]

KRAS(G12D)

2.4 μM (IC50)

体外研究
(In Vitro)

在带有 KRAS G12D 突变的两种胰腺癌细胞系(PANC-1 和 Panc 04.03)中,TH-Z827 具有抗增殖作用,IC50 值分别为 4.4 和 4.7 μM。TH-Z827 处理还可降低 PANC-1 和 Panc 04.03 细胞中 pERK 和 pAKT 的水平,证实 TH-Z827 可以阻止 MAPK 和 PI3K/mTOR 信号传导的激活[1]

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

体内研究
(In Vivo)

BALB/c 裸鼠皮下接种 Panc 04.03 细胞,C57BL/6 小鼠皮下接种 KPC 细胞。在裸鼠模型中,TH-Z827(10-30mg/kg)显着减少肿瘤体积,并且以剂量依赖性方式减少肿瘤体积。然而,腹腔内给药 30mg/kg TH-Z827 会导致观察到的体重减轻,再次表明潜在的脱靶效应[1]

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

分子量

498.66

Formula

C30H38N6O

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

TH-Z827 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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质量   浓度   体积   分子量 *
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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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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.

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产品名称:
TH-Z827
目录号:
HY-153663
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