2. GPCR/G Protein MAPK/ERK Pathway Cell Cycle/DNA Damage PI3K/Akt/mTOR Metabolic Enzyme/Protease Immunology/Inflammation NF-κB Apoptosis
  3. Ras PERK Akt Reactive Oxygen Species (ROS) Apoptosis Mitochondrial Metabolism
  4. KD36

KD36 是一种选择性 KRAS-G12C 抑制剂，其 IC50 值为 0.92 μM。KD36 可抑制 ERK 和 AKT 的磷酸化，诱导活性氧 (ROS) 积累，降低线粒体膜电位，从而导致 KRAS-G12C 突变细胞凋亡 (apoptosis)。KD36 可用于非小细胞肺癌 (NSCLC) 的研究。

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KD36

KD36 Chemical Structure

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

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Customer Review

KD36 相关抗体

Top Publications Citing Use of Products

查看 Ras 亚型特异性产品:

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K-Ras H-Ras N-Ras Ras

查看 Akt 亚型特异性产品:

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Akt Akt1 Akt2 Akt3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

KD36 is a selective KRAS-G12C inhibitor with an IC50 value of 0.92 μM. KD36 can inhibit the phosphorylation of ERK and AKT, induce the accumulation of reactive oxygen species (ROS), reduce mitochondrial membrane potential, thereby leading to apoptosis of KRAS-G12C mutant cells. KD36 can be used in the research of non-small cell lung cancer (NSCLC)[1].

IC50 & Target[1]

KRas G12C

0.92 μM (IC50)

体外研究
(In Vitro)

KD36 (72 h) 在 KRAS-G12C 突变型 NCI-H23、NCI-H358 细胞中表现出强大的抗增殖活性， IC50 值分别为 0.42 和 0.65 μM[1]。
KD36 (0.5-4.0 μM; 24-48 h) 通过增加 NCI-H23 细胞内的 ROS 水平并降低线粒体膜电位，诱导线粒体依赖性凋亡[1]。
KD36 (0.5-8.0 μM; 8 h) 可显著抑制 NCI-H23 细胞中 KRAS 下游效应分子 ERK 和 AKT 的磷酸化 (p-ERK、p-AKT)，而对 KRAS 野生型 NCI-H2228 细胞无明显抑制作用[1]。
KD36 (0.1-1.0 μM, 14 days) 以剂量依赖性方式抑制 NCI-H23 和 NCI-H358 细胞的集落形成[1]。

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

KD36 相关抗体:

Western Blot Analysis[1]

Cell Line: NCI–H23, NCI–H2228
Concentration: 0.5 μM, 1.0 μM, 2.0 μM, 4.0 μM, 8.0 μM
Incubation Time: 8 h
Result: Significantly reduced the phosphorylation of ERK and AKT in NCI-H23 cells, with a 80% reduction in pERK and 70% reduction in pAKT at 4.0 μM.

Immunofluorescence[1]

Cell Line: NCI–H23 cells
Concentration: 0.5 μM, 1.0 μM, 2.0 μM, 4.0 μM
Incubation Time: 24 h, 48 h
Result: Increased the levels of JC-1 monmers and DCFH-DA fluorescence intensity.
体内研究
(In Vivo)

KD36 (30 mg/kg, i.p., once daily for 11 days) 在 NCI-H358 异种移植模型小鼠中显著抑制肿瘤生长，肿瘤生长抑制率 (TGI) 达 54.6[1]。

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

Animal Model: NCI-H358 xenograft mice models (male, 6 weeks)[1]
Dosage: 30 mg/kg
Administration: Intraperitoneally injection
Result: Reduced tumor weight and volume.
Showed tumor growth inhibition (TGI) rate of 54.6%.
Caused no obvious pathological damage to major organs (heart, liver, spleen, lung, kidney), and exhibited no systemic toxicity.
分子量

512.60

Formula

C29H32N6O3
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

KD36 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

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)
× = ×
C1   V1   C2   V2
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:

KD36KD 36KD-36RasPERKAktReactive Oxygen Species (ROS)ApoptosisMitochondrial MetabolismProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinasePKBProtein kinase BPyrimidineKRAS-G12CStructure-activity relationshipNSCLCInhibitorinhibitorinhibit

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