PROTAC PI3K/110β degrader-2

Name: PROTAC PI3K/110β degrader-2
Brand: TargetMol
SKU: T210810
Rating: 4.5 (1 reviews)

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Catalog No. T210810Cas No. 3070438-79-5

PROTACPI3K/110β degrader-2 is a selective PI3K/p110β PROTAC degrader. It effectively degrades the 110β protein and inhibits the expression of P-glycoprotein. Additionally, it increases reactive oxygen species (ROS) levels. PROTACPI3K/110β degrader-2 exerts antitumor effects by activating the endoplasmic reticulum stress (ERS) mediated mitochondrial apoptosis pathway and inhibiting the AKT/Bcl-2 signaling pathway. This compound is applicable in cancer research.

PROTAC PI3K/110β degrader-2

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Catalog No. T210810Cas No. 3070438-79-5

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
10 mg	Inquiry	Inquiry	Inquiry
50 mg	Inquiry	Inquiry	Inquiry

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Product Introduction

Bioactivity

Description	PROTACPI3K/110β degrader-2 is a selective PI3K/p110β PROTAC degrader. It effectively degrades the 110β protein and inhibits the expression of P-glycoprotein. Additionally, it increases reactive oxygen species (ROS) levels. PROTACPI3K/110β degrader-2 exerts antitumor effects by activating the endoplasmic reticulum stress (ERS) mediated mitochondrial apoptosis pathway and inhibiting the AKT/Bcl-2 signaling pathway. This compound is applicable in cancer research.
In vitro	PROTAC PI3K/110β degrader-2 (Compound J-6) exhibits significant antitumor activity in A549 (IC50 = 58.2 μM), A549/DDP (IC50 = 39.23 μM), MCF-7 (IC50 = 53.99 μM), and MCF-7/ADM (IC50 = 38.73 μM) cell lines. This compound selectively degrades the 110β protein in MCF-7/ADM and A549/DDP cells in a time and concentration-dependent manner (0-50 μM, 0-48 hours). Furthermore, at concentrations of 0-25 μM for 24 hours, it markedly increases ROS levels, reduces mitochondrial membrane potential, and triggers ERS-mediated apoptosis in the same cell lines. Additionally, it inhibits Na+/K+-ATPase activity and decreases P-glycoprotein expression in MCF-7/ADM and A549/DDP cells.
In vivo	Compound J-6, known as PROTAC PI3K/110β degrader-2, administered at a dosage of 50 mg/kg via intraperitoneal injection every other day for a total of 7 treatments, effectively inhibits tumor growth by degrading the 110β protein in female MCF-7/ADM tumor BALB/c mice.

Chemical Properties

Molecular Weight	948.18
Formula	C₅₁H₆₅N₉O₇S
Cas No.	3070438-79-5
Smiles	C(NC1=C(C(NCCCCCCC(N[C@H](C(=O)N2[C@H](C(NCC3=CC=C(C=C3)C=4SC=NC4C)=O)C[C@@H](O)C2)C(C)(C)C)=O)=O)C=CC=C1)(C)C=5C=6N(C(=O)C=C(N6)N7CCOCC7)C=C(C)C5

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

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