2. GPCR/G Protein MAPK/ERK Pathway Stem Cell/Wnt
  3. Ras ERK p38 MAPK
  4. KRAS G12C-IN-78

KRAS G12C-IN-77 是一种具有选择性的 KRASG12C 共价双态抑制剂，可以高亲和力与 GDP 结合 (非活性态) (IC50 = 7 nM) 和 GTP 结合 (IC50 = 4 nM) (活性态) 的 KRASG12C 结合。KRAS G12C-IN-77 可快速抑制 ERK1/2 磷酸化，诱导与内源性 KRASG12C 形成共价加合物，抑制 MAPK 通路基因的表达，并抑制 KRASG12C 突变细胞的增殖。KRAS G12C-IN-77 可用于 KRASG12C 突变实体瘤的相关研究，包括胰腺导管腺癌和非小细胞肺癌。

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KRAS G12C-IN-78

KRAS G12C-IN-78 Chemical Structure

CAS No. : 3023465-20-2

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KRAS G12C-IN-78 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 ERK 亚型特异性产品:

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ERK ERK1 ERK2 ERK5 ERK8

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p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

KRAS G12C-IN-78 is a selective SWII-binding KRASG12C dual inhibitor targeting both inactive and active states. KRAS G12C-IN-78 rapidly inhibits ERK1/2 phosphorylation, induces covalent adduct formation with endogenous KRASG12C, suppresses MAPK pathway gene expression, and inhibits cellular proliferation in KRASG12C mutant cells. KRAS G12C-IN-78 can be used for the research of KRASG12C mutant solid tumors, including pancreatic ductal adenocarcinoma and non-small cell lung cancer[1].

IC50 & Target[1]

KRas G12C

 

ERK1

 

ERK2

 

体外研究
(In Vitro)

KRAS G12C-IN-78 (Compound 6) (2 h) 可强效抑制 MIA PaCa-2 KRASG12C 突变细胞中的 ERK1/2 磷酸化，IC50 为 0.1 nM[1]。
KRAS G12C-IN-78 (5 days) 可强效抑制 MIA PaCa-2 KRASG12C 突变细胞的增殖，处理 5 天后的 IC50 为 0.1 nM[1]。
KRAS G12C-IN-78 对 G12C 突变细胞的 IC50 <10 nM，对非 G12C 突变细胞的 IC50 >1000 nM[1]。

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

KRAS G12C-IN-78 相关抗体:
分子量

729.75

Formula

C37H31F4N7O3S
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

KRAS G12C-IN-78 相关分类

  • 摩尔计算器

  • 稀释计算器

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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.

Keywords:

KRAS G12C-IN-783023465-20-2RasERKp38 MAPKExtracellular signal regulated kinasesBRAF1 RBDMAPK pathwayH1792cysteine residuesGDP nucleotide exchangeHEK293TKRAS G12C-RAF interactionsERK1/2KRAS G12CMIA PaCa-2Inhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-181965
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