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

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.

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Pifusertib

Pifusertib Chemical Structure

CAS No. : 1402602-94-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

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Pifusertib Related Antibodies

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Akt Akt1 Akt2 Akt3

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Description

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)

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].

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

Pifusertib Related Antibodies

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.
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].

MedChemExpress (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
Molecular Weight

424.49

Formula

C26H24N4O2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

C[C@@](C1)(O)C[C@]1(N)C2=CC=C(C3=C(N(COC4=CC=NC=C45)C5=N3)C6=CC=CC=C6)C=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (117.79 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3558 mL 11.7788 mL 23.5577 mL
5 mM 0.4712 mL 2.3558 mL 4.7115 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.81%

SDS (251 KB)

COA (250 KB) HNMR (223 KB) LCMS (95 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3558 mL 11.7788 mL 23.5577 mL 58.8942 mL
5 mM 0.4712 mL 2.3558 mL 4.7115 mL 11.7788 mL
10 mM 0.2356 mL 1.1779 mL 2.3558 mL 5.8894 mL
15 mM 0.1571 mL 0.7853 mL 1.5705 mL 3.9263 mL
20 mM 0.1178 mL 0.5889 mL 1.1779 mL 2.9447 mL
25 mM 0.0942 mL 0.4712 mL 0.9423 mL 2.3558 mL
30 mM 0.0785 mL 0.3926 mL 0.7853 mL 1.9631 mL
40 mM 0.0589 mL 0.2945 mL 0.5889 mL 1.4724 mL
50 mM 0.0471 mL 0.2356 mL 0.4712 mL 1.1779 mL
60 mM 0.0393 mL 0.1963 mL 0.3926 mL 0.9816 mL
80 mM 0.0294 mL 0.1472 mL 0.2945 mL 0.7362 mL
100 mM 0.0236 mL 0.1178 mL 0.2356 mL 0.5889 mL
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Pifusertib Related Classifications

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.

Keywords:

Pifusertib1402602-94-1TAS-117TAS117TAS 117AktApoptosisAutophagyPKBProtein kinase Ballostericoralanti-myelomaERstressproteasomeInhibitorinhibitorinhibit

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