2. GPCR/G Protein MAPK/ERK Pathway Stem Cell/Wnt PI3K/Akt/mTOR Metabolic Enzyme/Protease Immunology/Inflammation NF-κB Apoptosis
  3. Ras ERK Akt Reactive Oxygen Species (ROS) Apoptosis Bcl-2 Family Caspase
  4. KRAS G12D-IN-37

KRAS G12D-IN-37 是一种 KRASG12D 抑制剂。KRAS G12D-IN-37 对 KRASG12D 突变肿瘤细胞具有抗增殖活性，而对正常细胞的细胞毒性极低。KRAS G12D-IN-37 通过与 His 95、Arg 68 和 Asp 12 残基形成氢键相互作用，稳定结合 KRASG12D，并抑制下游 ERK/AKT 信号通路。KRAS G12D-IN-37 可提升活性氧 (ROS) 水平、诱导细胞凋亡 (apoptosis) 并破坏线粒体膜电位。KRAS G12D-IN-37 可下调抗凋亡蛋白 Bcl-2 的水平，同时上调促凋亡蛋白 Bax 和 caspase 3 的水平。KRAS G12D-IN-37 可用于癌症相关研究，例如胃腺癌和结直肠癌。

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KRAS G12D-IN-37

KRAS G12D-IN-37 Chemical Structure

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KRAS G12D-IN-37 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

KRAS G12D-IN-37 is a KRASG12D inhibitor. KRAS G12D-IN-37 shows antiproliferative activity against KRASG12D mutant tumor cells and minimal cytotoxicity toward normal cells. KRAS G12D-IN-37 binds stably to KRASG12D via hydrogen bond interactions with residues His 95, Arg 68, and Asp 12, and inhibits downstream ERK/AKT signaling pathways. KRAS G12D-IN-37 elevates ROS levels, induces apoptosis, disrupts mitochondrial membrane potential. KRAS G12D-IN-37 downregulates the level of anti-apoptotic protein Bcl-2, and upregulates the levels of pro-apoptotic proteins Bax and caspase 3. KRAS G12D-IN-37 can be used for the research of cancer, such as gastric adenocarcinoma and colorectal cancer[1].

IC50 & Target[1]

KRas G12D

 

Bcl-2

 

Bax

 

Caspase 3

 

体外研究
(In Vitro)

KRAS G12D-IN-37 (Compound 16k) (72 h) 可强效抑制 KRASG12D 突变型 AGS 和 GP2D 细胞的增殖，其 IC50 值分别为 0.18 μM 和 0.21 μM，而对其他 KRAS 突变型细胞、KRAS 野生型细胞以及正常 HIEC 细胞的活性较低[1]。
KRAS G12D-IN-37 (0.31-2.5 μM; 24-72 h) 对 KRASG12D 突变型 AGS 和 GP2D 细胞表现出时间依赖性细胞毒性[1]。
KRAS G12D-IN-37 (0.0625-0.5 μM; 14 days) 可剂量依赖性地强效抑制 KRASG12D 突变型 AGS 和 GP2D 细胞的集落形成[1]。
KRAS G12D-IN-37 (0.625-2.5 μM; 6 h) 可在 KRASG12D 突变型 AGS 和 GP2D 细胞中抑制 KRAS 下游的 ERK/AKT 信号通路，并以剂量依赖方式降低 p-ERK 和 p-AKT 的水平[1]。
KRAS G12D-IN-37 (0.625-2.5 μM; 24 h) 可剂量依赖性地增强 KRASG12D 突变型 AGS 和 GP2D 细胞内的 ROS 积累，并破坏线粒体膜电位[1]。
KRAS G12D-IN-37 (0.625-5 μM; 24 h) 可剂量依赖性地诱导 KRASG12D 突变型 AGS 和 GP2D 细胞发生凋亡，呈剂量依赖性地改变促凋亡与抗凋亡蛋白的平衡，并提高 Caspase 3 活性[1]。
KRAS G12D-IN-37 (1 μM; 0, 5, 15, 30, 60 min) 在大鼠肝微粒体中表现出良好的代谢稳定性，半衰期为 289 min[1]。

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

KRAS G12D-IN-37 相关抗体:

Cell Proliferation Assay[1]

Cell Line: KRAS G12D-mutant AGS and GP2D cells
Concentration: 0.0625, 0.125, 0.25, 0.5 μM
Incubation Time: 14 days (medium changes every 72 h)
Result: Dose-dependently inhibited colony formation of AGS and GP2D cells.
Almost entirely suppressed AGS cell colony formation at 0.25 μM; almost entirely suppressed GP2D cell colony formation at 0.5 μM.
Showed superior colony formation inhibition efficacy compared to MRTX 1133 (HY-134813).

Western Blot Analysis[1]

Cell Line: KRAS G12D-mutant AGS and GP2D cells
Concentration: 0.625, 1.25, 2.5 μM
Incubation Time: 6 h
Result: Decreased the phosphorylation of ERK and AKT in AGS and GP2D cells.
Reduced p-AKT levels by 90% and p-ERK levels by 70% in GP2D cells at 2.5 μM; the effect on p-AKT/AKT was comparable to that of MRTX 1133.
Caused p-ERK levels to rebound at 1.25 μM in GP2D cells, potentially due to negative feedback in RAS signaling.

Apoptosis Analysis[1]

Cell Line: KRAS G12D-mutant AGS and GP2D cells
Concentration: 0.625, 1.25, 2.5 μM
Incubation Time: 24 h
Result: Induced apoptosis in AGS and GP2D cells in a dose-dependent manner.
Induced apoptosis in 80% of AGS cells at 5 μM; induced apoptosis in a high proportion of GP2D cells at 2.5 μM.
Induced higher apoptosis rates than MRTX 1133, with most apoptotic events occurring in the early stage.

Western Blot Analysis[1]

Cell Line: KRAS G12D-mutant AGS and GP2D cells
Concentration: 0.625, 1.25, 2.5 μM
Incubation Time: 24 h
Result: Dose-dependently upregulated the levels of pro-apoptotic proteins Bax and Caspase 3, and downregulated the level of anti-apoptotic protein Bcl-2 in AGS and GP2D cells.
Dose-dependently increased Caspase 3 activity in both cell lines.
体内研究
(In Vivo)

KRAS G12D-IN-37 (Compound 16k) (500-1500 mg/kg；口服；单次给药) 在昆明小鼠中表现出良好的体内安全性特征，其 LD50 约为 1270 mg/kg[1]。

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

Animal Model: Healthy Kunming mice (equally divided by sex)[1]
Dosage: 1500 mg/kg; 1200 mg/kg; 1000 mg/kg; 500 mg/kg
Administration: p.o.; single dose
Result: Caused death of all mice at 1500 mg/kg.
Led to death of 2 of 6 mice at 1200 mg/kg, with a calculated median lethal dose (LD50) of approximately 1270 mg/kg.
Showed no notable weight loss or physical abnormalities in mice treated with 500 mg/kg or 1000 mg/kg over 14 days.
Revealed no significant morphological changes or cellular abnormalities in heart, liver, spleen, lungs, and kidneys of mice treated with 1000 mg/kg.
分子量

557.61

Formula

C29H34F3N5O3
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

KRAS G12D-IN-37 相关分类

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  • 稀释计算器

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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.

Keywords:

KRAS G12D-IN-37RasERKAktReactive Oxygen Species (ROS)ApoptosisBcl-2 FamilyCaspaseExtracellular signal regulated kinasesPKBProtein kinase BAGS cellsERK/AKT signaling pathwaysapoptosisHIEC cellsKunming micegastric adenocarcinomaKRAS G12Dreactive oxygen speciesGP2D cellscolorectal cancerInhibitorinhibitorinhibit

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