2. GPCR/G Protein MAPK/ERK Pathway Stem Cell/Wnt Apoptosis
  3. Ras ERK Apoptosis
  4. KRASG12D-IN-7

KRASG12D-IN-7 是一种具有选择性的 KRASG12D 抑制剂。KRASG12D-IN-7 对 KRASG12D 在 GDP 和 GTP 结合状态下均显示出强结合活性，Kd 值分别为 1.12 nM 和 1.86 nM。KRASG12D-IN-7 抑制携带 KRASG12D 的 AsPC-1 细胞增殖，IC50 值为 10 nM，并抑制 MAPK 信号传导。KRASG12D-IN-7 在 AsPC-1 细胞中诱导 G0/G1 期阻滞和凋亡 (apoptosis)，并强烈抑制其集落形成。KRASG12D-IN-7 可用于研究携带 KRASG12D 突变的癌症，特别是胰腺导管腺癌 (PDAC)。

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KRASG12D-IN-7

KRASG12D-IN-7 Chemical Structure

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KRASG12D-IN-7 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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

KRASG12D-IN-7 is a selective KRASG12D inhibitor. KRASG12D-IN-7 displays strong binding activity for KRASG12D in both its GDP- and GTP- bound states, with Kd value of 1.12 nM and 1.86 nM, respectively. KRASG12D-IN-7 inhibits the proliferation of KRASG12D harboring AsPC-1 cells with an IC50 value of 10 nM and suppresses MAPK signaling. KRASG12D-IN-7 induces G0/G1 phase arrest and apoptosis in AsPC-1 cells, and strongly inhibits their colony formation. KRASG12D-IN-7 can be used for the study of cancers harboring KRASG12D mutation, particularly pancreatic ductal adenocarcinoma (PDAC)[1].

IC50 & Target[1]

KRas G12D

1.12 nM (Kd, GDP-bound states)

KRas G12D

1.86 nM (Kd, GTP-bound states)

体外研究
(In Vitro)

KRASG12D-IN-7 (Compound (R)-5a) (72 小时) 对携带 KRASG12D 突变的 AsPC-1 细胞 (IC50 = 10 nM)、GP2D 细胞 (IC50 = 2.7 nM)、AGS 细胞 (IC50 = 6.1 nM)、HPAF-II 细胞 (IC50 = 6.8 nM) 和 Ls513 细胞 (IC50 = 27.3 nM) 表现出强效且选择性的抗增殖活性，同时对其他 KRAS 突变体 (H358 G12C、G12S) 和 KRAS 野生型细胞系的抑制作用不显著 (IC50 > 1000 nM)[1]。
KRASG12D-IN-7 可结合 GDP 和 GTP 结合形式的 KRASG12D，选择性地抑制 GDP 结合状态的 KRASG12D 与 SOS1 的相互作用，并阻碍 GTP 结合状态的 KRASG12D 与 RAF1 的结合[1]。
KRASG12D-IN-7 (1-1000 nM，3 小时) 以剂量依赖方式降低 AsPC-1 细胞中 p-ERK 和 p-S6 的蛋白水平，有效抑制 KRAS 下游 MAPK 信号通路[1]。
KRASG12D-IN-7 (1-1000 nM，24-72 小时) 在 AsPC-1 细胞中诱导 G0/G1 期阻滞和凋亡[1]。
KRASG12D-IN-7 (5 nM，10 天) 强烈抑制 AsPC-1 细胞的集落形成[1]。

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

KRASG12D-IN-7 相关抗体:

Western Blot Analysis[1]

Cell Line: AsPC-1 cells
Concentration: 1, 10, 100, 1000 nM
Incubation Time: 3 h
Result: Reduced the protein levels of p-ERK and p-S6 in AsPC-1 cells.

Cell Cycle Analysis[1]

Cell Line: AsPC-1 cells
Concentration: 1, 10, 100, 1000 nM
Incubation Time: 24 h
Result: Increased G0/G1 phase cell proportion.
Downregulated CDK2/Cyclin D3 protein levels.

Apoptosis Analysis[1]

Cell Line: AsPC-1 cells
Concentration: 1, 10, 100, 1000 nM
Incubation Time: 72 h
Result: Induced apoptosis in AsPC-1 cells.
Increased Annexin V-positive cells.
Upregulated cPARP/cCasp-3 protein levels.
分子量

671.04

Formula

C31H32ClF2N7OSe
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

KRASG12D-IN-7 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:

KRASG12D-IN-7RasERKApoptosisExtracellular signal regulated kinasesKRASG12Dcancerpancreatic ductal adenocarcinomaMAPKInhibitorinhibitorinhibit

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