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PROTAC-O4I2

Name: PROTAC-O4I2
Brand: TargetMol
SKU: T74186
Price: 54 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T74186Cas No. 2785323-62-6

PROTAC-O4I2, a PROTAC ligand targeting splicing factor 3B1 (SF3B1), induced FLAG-SF3B1 degradation in K562 cells with an IC50 value of 0.244 μM. PROTAC-O4I2 induced apoptosis in K562 WT cells.

PROTAC-O4I2

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Purity: 97.45%

Catalog No. T74186Cas No. 2785323-62-6

PROTAC-O4I2, a PROTAC ligand targeting splicing factor 3B1 (SF3B1), induced FLAG-SF3B1 degradation in K562 cells with an IC50 value of 0.244 μM. PROTAC-O4I2 induced apoptosis in K562 WT cells.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$54	In Stock	In Stock
5 mg	$128	In Stock	In Stock
10 mg	$198	In Stock	In Stock
25 mg	$455	In Stock	In Stock
50 mg	$788	In Stock	In Stock
100 mg	$1,280	In Stock	In Stock
500 mg	$2,580	-	In Stock
1 mL x 10 mM (in DMSO)	$143	In Stock	In Stock

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

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:97.45%

Appearance:Solid

Color:Yellow

Resource Download

COA HNMR LCMS

Product Introduction

Bioactivity

Description	PROTAC-O4I2, a PROTAC ligand targeting splicing factor 3B1 (SF3B1), induced FLAG-SF3B1 degradation in K562 cells with an IC50 value of 0.244 μM. PROTAC-O4I2 induced apoptosis in K562 WT cells.
In vitro	PROTAC-O4I2 introduces thalidomide into the ubiquitin E3 ligase cereblon (CRBN), thereby selectively degrading SF3B1 and inhibiting tumor growth in cells.[1] PROTAC-O4I2 degrades and inhibits SF3B1 in K562 cells. PROTAC-O4I2 has anti-proliferative effects on SF3B1 WT, SF3B1 OE, and SF3B1 K700E cells with IC50 of 228, 63, and 90 nM, respectively.[1] PROTAC-O4I2 induces FLAG-SF3B1 degradation in a concentration-dependent manner, with a half-maximal inhibitory concentration (IC50) value of 0.244 μM in K562 cells.[1]
In vivo	Flies were fed on a round filter paper loaded with PROTAC-O4I2 (10 μM) in a 5% sucrose solution, maintained at 18℃, and flipped into a freshly prepared vial every 2 days. PROTAC-O4I2 significantly improves Drosophila survival in a Drosophila intestinal tumor model by interfering with tumor maintenance and proliferation.[1]

Chemical Properties

Molecular Weight	609.1
Formula	C₂₉H₂₉ClN₆O₅S
Cas No.	2785323-62-6
Smiles	O=C1C=2C(C(=O)N1C3C(=O)NC(=O)CC3)=CC=CC2NCCCCCCNC(=O)C=4N=C(NC5=CC=C(Cl)C=C5)SC4

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 200 mg/mL (328.35 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (8.21 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.6418 mL	8.2088 mL	16.4177 mL	82.0883 mL
5 mM	0.3284 mL	1.6418 mL	3.2835 mL	16.4177 mL
10 mM	0.1642 mL	0.8209 mL	1.6418 mL	8.2088 mL
20 mM	0.0821 mL	0.4104 mL	0.8209 mL	4.1044 mL
50 mM	0.0328 mL	0.1642 mL	0.3284 mL	1.6418 mL
100 mM	0.0164 mL	0.0821 mL	0.1642 mL	0.8209 mL

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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.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc