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Umbralisib

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Purity:99.83%

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COA HNMR HPLC

Umbralisib

Catalog No. T4976Cas No. 1532533-67-7

Umbralisib (TGR 1202) is a PI3Kδ inhibitor.

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

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Product Introduction

Bioactivity

Description	Umbralisib (TGR 1202) is a PI3Kδ inhibitor.
In vitro	TGR-1202 and carfilzomib synergistically kill blood cancer cells through disrupting the 4E-BP1-eIF4F-c-Myc axis. TGR-1202 and carfilzomib in combination synergistically and selectively silence the c-Myc and E2F transcription programs. TGR-1202 (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.
Alias	TGR-1202, RP5264, TGR 1202, TGR1202

Chemical Properties

Molecular Weight	571.55
Formula	C31H24F3N5O3
Cas No.	1532533-67-7

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 91 mg/mL(159.2 mM)

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 mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

Dose Conversion

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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