1. PI3K/Akt/mTOR Apoptosis Autophagy
  2. Akt Apoptosis Autophagy
  3. Pifusertib

Pifusertib  (Synonyms: TAS-117)

目录号: HY-19934
产品使用指南

Pifusertib (TAS-117) 是一种有效、选择性、具有口服活性的别构 Akt 抑制剂 (对 Akt1、2 和 3 的 IC50 分别为 4.8、1.6 和 44 nM)。Pifusertib 激发抗骨髓瘤活性并增强蛋白酶体抑制诱导的致命内质网应激。Pifusertib 诱导细胞凋亡 (apoptosis) 和自噬 (autophagy)。

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Pifusertib Chemical Structure

Pifusertib Chemical Structure

CAS No. : 1402602-94-1

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查看 Akt 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Pifusertib (TAS-117) is a potent, selective, orally active allosteric Akt inhibitor (with IC50s of 4.8, 1.6, and 44 nM for Akt1, 2, and 3, respectively). Pifusertib triggers anti-myeloma activities and enhances fatal endoplasmic reticulum (ER) stress induced by proteasome inhibition. Pifusertib induces apoptosis and autophagy[1].

IC50 & Target[1]

Akt1

4.8 nM (IC50)

Akt2

1.6 nM (IC50)

Akt3

44 nM (IC50)

体外研究
(In Vitro)

Pifusertib (1 μM; 6 hours) blocks basal phosphorylation of Akt and downstream p-FKHR/FKHRL1 in MM cells with high baseline p-Akt[1].
Pifusertib (0-10 μM; 72 hours) selectively inhibits Akt and induces cytotoxicity in MM cells with high baseline phosphorylation of Akt[1].
Pifusertib abrogates the cytoprotective effect of the bone marrow microenvironment associated with Akt inhibition in both MM cells and BMSCs. Pifusertib enhances Carfilzomib-induced cytotoxicity and fatal ER stress in MM cells. Pifusertib (0.5, 1 μM) triggers G0/G1 arrest followed by apoptosis, associated with induction of autophagy and endoplasmic reticulum stress response[1].
Pifusertib enhances bortezomib-induced cytotoxicity, associated with increased CHOP (a fatal ER-stress marker) and PARP cleavage and blockade of bortezomib-induced p-Akt, suggesting that Pifusertib augments Bortezomib-induced ER stress and apoptotic signaling[1].

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

Cell Viability Assay[1]

Cell Line: MM cell lines
Concentration: 0-10 μM
Incubation Time: 72 hours
Result: Induced significant growth inhibition in MM cell lines with high baseline p-Akt, but not in cell lines with low baseline p-Akt.

Western Blot Analysis[1]

Cell Line: MM cell lines
Concentration: 0-10 μM
Incubation Time: 72 hours
Result: Blocked basal phosphorylation of Akt and downstream p-FKHR/FKHRL1 in MM cells with high baseline p-Akt, but did not inhibit autophosphorylation of PDK1 which phosphorylates Akt at Thr308.
体内研究
(In Vivo)

Pifusertib (12-16 mg/kg; p.o.; daily for 5 days a week, 21 days) inhibits tumor growth in murine xenograft models of human MM[1].
Pifusertib enhances bortezomib-induced MM cytotoxicity in vivo[1].

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

Animal Model: SCID mice (xenograft models bearing MM.1S cells)[1]
Dosage: 12, 16 mg/kg
Administration: P.o.; daily for 5 days a week, 21 days
Result: Significantly reduced MM.1S tumor growth versus vehicle control.
Clinical Trial
分子量

424.49

Formula

C26H24N4O2

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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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:
Pifusertib
目录号:
HY-19934
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