1. PI3K/Akt/mTOR
  2. PI3K
  3. PI3K-IN-6

PI3K-IN-6 (compound 20a) 是具有口服有效的、高度选择性的磷脂酰肌醇三激酶(PI3K) β/δ 的抑制剂,其对 PI3K β/δ 的 IC50 值分别为 7.8 nM 和 5.3 nM。PI3K-IN-6 (compound 20a) 可用于磷酸酶和紧张素同系物 (PTEN) 缺乏性肿瘤的研究。

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PI3K-IN-6 Chemical Structure

PI3K-IN-6 Chemical Structure

CAS No. : 1842380-77-1

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PI3K-IN-6 (compound 20a) is an oral active and highly selective phosphoinositide 3-kinase (PI3K) β/δ inhibitor, with IC50 values of 7.8 nM/5.3 nM for PI3K β/δ, respectively. PI3K-IN-6 (compound 20a) has potential top treat phosphatase and tensin homolog (PTEN) feficient tumors[1].

IC50 & Target

PI3Kβ

7.8 nM (IC50)

PI3Kδ

5.3 nM (IC50)

PI3Kα

850 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A498 GI50
80 nM
Compound: 20a
Growth inhibition of human A498 cells harboring PI3Kbeta mutant after 72 hrs by Celltiter-Glo reagent based assay
Growth inhibition of human A498 cells harboring PI3Kbeta mutant after 72 hrs by Celltiter-Glo reagent based assay
[PMID: 28106991]
LNCaP GI50
38 nM
Compound: 20a
Growth inhibition of PTEN-deficient human LNCAP cells after 72 hrs by Celltiter-Glo reagent based assay
Growth inhibition of PTEN-deficient human LNCAP cells after 72 hrs by Celltiter-Glo reagent based assay
[PMID: 28106991]
MDA-MB-415 GI50
12 nM
Compound: 20a
Growth inhibition of PTEN-deficient human MDA-MB-415 cells after 72 hrs by Celltiter-Glo reagent based assay
Growth inhibition of PTEN-deficient human MDA-MB-415 cells after 72 hrs by Celltiter-Glo reagent based assay
[PMID: 28106991]
PC-3 GI50
120 nM
Compound: 20a
Growth inhibition of PTEN-deficient human PC3 cells after 72 hrs by Celltiter-Glo reagent based assay
Growth inhibition of PTEN-deficient human PC3 cells after 72 hrs by Celltiter-Glo reagent based assay
[PMID: 28106991]
ZR-75-1 GI50
2 nM
Compound: 20a
Growth inhibition of PTEN-deficient human ZR-75-1 cells after 72 hrs by Celltiter-Glo reagent based assay
Growth inhibition of PTEN-deficient human ZR-75-1 cells after 72 hrs by Celltiter-Glo reagent based assay
[PMID: 28106991]
分子量

450.26

Formula

C17H14Cl2FN9O

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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Inquiry Information

产品名称:
PI3K-IN-6
目录号:
HY-101115
需求量: