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Umbralisib

Name: Umbralisib
Brand: TargetMol
SKU: T4976
Price: 41 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T4976Cas No. 1532533-67-7

Alias TGR-1202, TGR1202, TGR 1202, RP5264

Umbralisib (TGR 1202) is a PI3Kδ inhibitor.

Umbralisib

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Purity: 99.56%

Catalog No. T4976Alias TGR-1202, TGR1202, TGR 1202, RP5264Cas No. 1532533-67-7

Umbralisib (TGR 1202) is a PI3Kδ inhibitor.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$41	In Stock	In Stock
2 mg	$59	In Stock	In Stock
5 mg	$97	In Stock	In Stock
10 mg	$178	In Stock	In Stock
25 mg	$360	In Stock	In Stock
50 mg	$473	In Stock	In Stock
100 mg	$693	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$123	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:99.56%

Appearance:Solid

Color:White

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COA HPLC HNMR LCMS

Product Introduction

Bioactivity

Description	Umbralisib (TGR 1202) is a PI3Kδ inhibitor.
Targets&IC50	PI3Kα:>10000 nM (Kd), PI3Kβ:>10000 nM (Kd), PI3Kγ:1400 nM (Kd), PI3Kδ:6.2 nM (Kd), PI3Kδ:22.2 nM
In vitro	Umbralisib and carfilzomib synergistically kill blood cancer cells through disrupting the 4E-BP1-eIF4F-c-Myc axis. Umbralisib and carfilzomib in combination synergistically and selectively silence the c-Myc and E2F transcription programs. Umbralisib (15-50 μM) potently represses the expression of c-Myc in the DLBCL cell line LY7, and is uniquely characterized with structural features suitable for targeting CK1ε in lymphoma cells.
In vivo	In a subcutaneous xenograft model of T-cell acute lymphoblastic leukemia (T-ALL) in NOD/SCID mice using the MOLT-4 cell line, TGR-1202 (150 mg/kg, daily p.o.) significantly shrinks the tumors by day 25.
Synonyms	TGR-1202, TGR1202, TGR 1202, RP5264

Chemical Properties

Molecular Weight	571.55
Formula	C₃₁H₂₄F₃N₅O₃
Cas No.	1532533-67-7
Smiles	CC(C)Oc1ccc(cc1F)-c1nn([C@@H](C)c2oc3ccc(F)cc3c(=O)c2-c2cccc(F)c2)c2ncnc(N)c12
Relative Density.	1.43 g/cm3 (Predicted)

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.

Solubility Information

DMSO: 91 mg/mL (159.22 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+90% Corn Oil: 3.3 mg/mL (5.77 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	1.7496 mL	8.7481 mL	17.4963 mL	87.4814 mL
5 mM	0.3499 mL	1.7496 mL	3.4993 mL	17.4963 mL
10 mM	0.1750 mL	0.8748 mL	1.7496 mL	8.7481 mL
20 mM	0.0875 mL	0.4374 mL	0.8748 mL	4.3741 mL
50 mM	0.0350 mL	0.1750 mL	0.3499 mL	1.7496 mL
100 mM	0.0175 mL	0.0875 mL	0.1750 mL	0.8748 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