Cat. No.: HY-19934

Pifusertib

(Synonyms: TAS-117)

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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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Pureté: 99.81%
CAS No.: 1402602-94-1
Formule: C₂₆H₂₄N₄O₂
Masse moléculaire:424.49

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Pifusertib Chemical Structure

CAS No.: 1402602-94-1

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Solvant et solubilité
- In Vitro
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

Akt1

4.8 nM (IC₅₀)

Akt2

1.6 nM (IC₅₀)

Akt3

44 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform Akt :

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.

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.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1402602-94-1
Appearance Solid
Masse moléculaire 424.49
Formule C₂₆H₂₄N₄O₂
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
Synonyms

TAS-117
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvant et solubilité

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3558 mL

11.7788 mL

23.5577 mL

5 mM

0.4712 mL

2.3558 mL

4.7115 mL

10 mM

0.2356 mL

1.1779 mL

2.3558 mL

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (275 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Mimura N, et al. Selective and potent Akt inhibition triggers anti-myeloma activities and enhances fatal endoplasmic reticulum stress induced by proteasome inhibition. Cancer Res. 2014;74(16):4458-4469. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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Highly Selective Inhibitors Library

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Multi-Target Compound Library

Bioactive Compound Library Max

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Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Voir tous les produits spécifiques à Isoform Akt

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Pifusertib Related Classifications

HY-19934 Related Classifications