2. Protein Tyrosine Kinase/RTK
  3. SHP2
  4. SHP2-IN-13

SHP2-IN-13 是一种具有高选择性和口服活性的 SHP2 “tunnel site” 变构抑制剂，IC50 为 83.0 nM。SHP2-IN-13 可用于具有携带 RTK 致癌驱动因子的癌症和 SHP2-相关疾病研究的潜力。

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SHP2-IN-13 Chemical Structure

SHP2-IN-13 Chemical Structure

CAS No. : 2951854-02-5

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SHP2-IN-13 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SHP2-IN-13 is a highly selective and orally active SHP2 “tunnel site” allosteric inhibitor with an IC50 of 83.0 nM. SHP2-IN-13 has the potential for cancers bearing RTK oncogenic drivers and SHP2-related diseases research.

体外研究
(In Vitro)

SHP2-IN-13 (compound 129) 以剂量依赖性的方式有效抑制 pERK 信号通路, 在 NSCLC cells 和 NCI–H1975-OR 细胞中的 IC50值分别为0.59 μM 和 0.63±0.32 μM时，[1]。 Shp2-in-13 (0-30 μM; 24 h) 抑制 NCI-H1975 细胞 pERK 水平和受体酪氨酸激酶 (RTK) 驱动的癌细胞增殖。它还能抑制受体酪氨酸激酶 (RTK) 耐药 NSCLC 细胞中磷酸化 ERK (pERK) 水平[1]。

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

SHP2-IN-13 相关抗体:

Western Blot Analysis[1]

Cell Line: NSCLC cells or NCI–H1975-OR cells
Concentration: 0 μM, 0.01 μM, 0.04 μM, 0.1 μM, 0.4 μM, 1.1 μM, 3.3 μM, 10 μM, 30 μM
Incubation Time: 24 hours
Result: Inhibited p-ERK expression in a dose-dependent manner.
体内研究
(In Vivo)

在药代动力学实验中，SHP2-IN-13 (compound 129) (IV/PO;5mg/kg) 表现出清除率高，分布量大 (13.9 L/kg)，半衰期中等(T1/2=5.31 h) 的特性，它的口服生物利用度 (F =55.07±7.93%) 高于SHP099 (F =46%)，适合进一步用于体内抗肿瘤药效学的评价[1]。
SHP2-IN-13 (oral gavage; 20 mg/kg; daily) 显示出强的抗白血病的功效，并引起白血病负担的显著减少。此外，它几乎完全根除了人血液和脾脏样本中的 CD45+ 白血病细胞[1]。

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

Animal Model: Murine NSG xenograft model inoculated with FLT3-ITD mutated MV-4-11-luciferase (MV-4-11-Luc) AML cells[1]
Dosage: 20 mg/kg
Administration: Oral gavage; 20 mg/kg; daily
Result: Exhibited an anti-tumour efficacy in AML model.
分子量

327.38

Formula

C16H21N7O
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

SHP2-IN-13 相关分类

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  • 稀释计算器

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  • Do most proteins show cross-species activity?

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Keywords:

SHP2-IN-132951854-02-5SHP2Src homology phosphatase 2PTPN11sHP2Receptor tyrosine kinaseLead compoundRTKoncogenicdriverSHP2-relateddiseasesAMLCANCERInhibitorinhibitorinhibit

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