1. Protein Tyrosine Kinase/RTK
  2. SHP2
  3. SHP2-IN-46

SHP2-IN-46 是一种具有口服活性的 SHP2 抑制剂 (IC50 = 11.76 μM)。SHP2-IN-46 可抑制 SHP2 酶活性,介导抗肿瘤活性。SHP2-IN-46 在多种癌细胞中抑制细胞增殖。SHP2-IN-46 可用于肺腺癌、胰腺癌、肝母细胞瘤的相关研究。

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SHP2-IN-46

SHP2-IN-46 Chemical Structure

CAS No. : 3086360-36-0

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SHP2-IN-46 is an orally active SHP2 inhibitor (IC50 = 11.76 μM). SHP2-IN-46 inhibits SHP2 enzymatic activity and mediates anti-tumor activity. SHP2-IN-46 suppresses cell proliferation in various cancer cells. SHP2-IN-46 can be used in research related to lung adenocarcinoma, pancreatic cancer and hepatoblastoma[1].

体外研究
(In Vitro)

SHP2-IN-46 (Compound 27) (72 h) 可强效抑制 A549、MIA PaCa-2 和 HepG2 癌细胞的增殖,其 IC50 值分别为 0.24 μM、0.16 μM 和 0.09 μM,在非癌变 Vero 细胞中细胞毒性较低,其 IC50 值为 42.79 μM[1]
SHP2-IN-46 (0.5 μM, 24 h) 可诱导 HepG2 细胞发生 S 期细胞周期阻滞,从而抑制细胞增殖[1]
SHP2-IN-46 在人肝微粒体中表现出良好的代谢稳定性,T1/2 为 40.63 min,CLint 为 34.11 μL/min/mg protein[1]
SHP2-IN-46 (0.001-100 μM; 90 min ) 可抑制 SHP2 酶活性,其 IC50 值为 11.76 μM[1]

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

Cell Cycle Analysis[1]

Cell Line: HePG2 cells
Concentration: 0.5 μM
Incubation Time: 24 h
Result: Promoted the transition from G1 to S phase and subsequently induce S-phase arrest.
体内研究
(In Vivo)

SHP2-IN-46 (50-200 mg/kg; p.o.; single dose) 在 ICR 小鼠中最大耐受剂量可大于 200 mg/kg[1]

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

Animal Model: ICR mice (8 weeks old, 50% male/female)[1]
Dosage: 50 mg/kg; 100 mg/kg; 200 mg/kg
Administration: p.o.; single dose
Result: Had a maximum tolerated dose greater than 200 mg/kg in ICR mice.
分子量

309.37

Formula

C17H19N5O

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
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  • 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.

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产品名称:
SHP2-IN-46
目录号:
HY-181250
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