1. Protein Tyrosine Kinase/RTK Metabolic Enzyme/Protease Cell Cycle/DNA Damage
  2. SHP2 Phosphatase CDK
  3. SHP2/CDK4-IN-1

SHP2/CDK4-IN-1 (compound 10) 是一种口服有效的 SHP2CDK4 双抑制剂,IC50 分别为 4.3 和 18.2 nM。SHP2/CDK4-IN-1 能有效诱导 G0/G1 阻滞,抑制 TNBC 细胞增殖。SHP2/CDK4-IN-1 在 EMT6 同基因小鼠模型中显示出显著的抗肿瘤作用。SHP2/CDK4-IN-1 可用于三阴性乳腺癌 (TNBC) 的研究。

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SHP2/CDK4-IN-1 Chemical Structure

SHP2/CDK4-IN-1 Chemical Structure

CAS No. : 2924036-87-1

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SHP2/CDK4-IN-1 (compound 10) is an orally active and potent SHP2 and CDK4 dual inhibitor, with IC50 values of 4.3 and 18.2 nM, respectively. SHP2/CDK4-IN-1 effectively induces G0/G1 arrest to prevent the proliferation of TNBC cell lines. SHP2/CDK4-IN-1 shows significant antitumor efficacy in the EMT6 syngeneic mouse model. SHP2/CDK4-IN-1 can be used for triple-negative breast cancer (TNBC) research[1].

IC50 & Target

CDK4

18.2 ± 1.3 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
EMT6 IC50
0.64 μM
Compound: 10
Antiproliferative activity against mouse EMT6 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against mouse EMT6 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
[PMID: 35447031]
MDA-MB-231 IC50
5.57 μM
Compound: 10
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
[PMID: 35447031]
MDA-MB-468 IC50
1.76 μM
Compound: 10
Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
[PMID: 35447031]
分子量

693.21

Formula

C33H35ClF2N10OS

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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  • 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/CDK4-IN-1
目录号:
HY-150609
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