1. GPCR/G Protein MAPK/ERK Pathway Apoptosis
  2. Ras Apoptosis
  3. TH-Z835

TH-Z835 是一种突变型选择性 KRAS (G12D) 抑制剂,IC50 为 1.6 μM。TH-Z835 抑制 mantGMPPNP/GPPNP 交换和 GPPNP/mantGMPPNP 交换。

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TH-Z835 Chemical Structure

TH-Z835 Chemical Structure

CAS No. : 2766209-50-9

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生物活性

TH-Z835 is a mutant selective KRAS (G12D) inhibitor with an IC50 of 1.6 μM. TH-Z835 inhibits both mantGMPPNP/GPPNP exchange and GPPNP/mantGMPPNP exchange[1].

IC50 & Target[1]

KRAS(G12D)

1.6 μM (IC50)

体外研究
(In Vitro)

TH-Z835 降低 PANC-1 细胞中的 pERK 水平,IC50 值小于 2.5 μM[1]
TH-Z835 在其他非 G12D 突变癌细胞系(包括 4T1 (KRAS(WT))、MIA PaCa-2 (KRAS(G12C))、CFPAC-1 (KRAS(G12V)) 和 HCT116 (KRAS(G13D)) 细胞中具有抗增殖作用,降低 pERK 和 pAKT 水平并诱导细胞凋亡,表明存在脱靶效应[1]

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

体内研究
(In Vivo)

TH-Z835(10mg/kg;腹膜内注射)可减少 C57BL/6 小鼠模型中的肿瘤体积。TH-Z835 在体内诱导细胞凋亡并抑制 MAPK 信号传导[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
性状

固体

颜色

Off-white to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料
参考文献
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  • 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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TH-Z835
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HY-146243
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