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Umbralisib

🥰Excellent
Catalog No. T4976Cas No. 1532533-67-7
Alias TGR-1202, TGR1202, TGR 1202, RP5264

Umbralisib (TGR 1202) is a PI3Kδ inhibitor.

Umbralisib
Other Forms of Umbralisib:

Umbralisib

🥰Excellent
Purity: 99.56%
Catalog No. T4976Alias TGR-1202, TGR1202, TGR 1202, RP5264Cas No. 1532533-67-7
Umbralisib (TGR 1202) is a PI3Kδ inhibitor.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$41In StockIn Stock
2 mg$59In StockIn Stock
5 mg$97In StockIn Stock
10 mg$178In StockIn Stock
25 mg$360In StockIn Stock
50 mg$473In StockIn Stock
100 mg$693In StockIn Stock
1 mL x 10 mM (in DMSO)$123In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.56%
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Product Introduction

Bioactivity
Description
Umbralisib (TGR 1202) is a PI3Kδ inhibitor.
Targets&IC50
PI3Kδ:22.2 nM, PI3Kγ:1400 nM (Kd), PI3Kα:>10000 nM (Kd), PI3Kδ:6.2 nM (Kd), PI3Kβ:>10000 nM (Kd)
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.
SynonymsTGR-1202, TGR1202, TGR 1202, RP5264
Chemical Properties
Molecular Weight571.55
FormulaC31H24F3N5O3
Cas No.1532533-67-7
SmilesCC(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
StoragePowder: -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 recommeded.
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
1mg5mg10mg50mg
1 mM1.7496 mL8.7481 mL17.4963 mL87.4814 mL
5 mM0.3499 mL1.7496 mL3.4993 mL17.4963 mL
10 mM0.1750 mL0.8748 mL1.7496 mL8.7481 mL
20 mM0.0875 mL0.4374 mL0.8748 mL4.3741 mL
50 mM0.0350 mL0.1750 mL0.3499 mL1.7496 mL
100 mM0.0175 mL0.0875 mL0.1750 mL0.8748 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:
TargetMol | Animal experimentsFor 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% Saline/PBS/ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | 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 DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2OTargetMol | reagent mix well and clarify
For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.
1 Enter information below:
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μL
2 Enter the in vivo formulation:
% DMSO
%
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% Saline/PBS/ddH2O

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

Keywords

UmbralisibRP-5264RP 5264PI3KδPI3KPhosphoinositide 3-kinaseorally activelymphomalymphocytic leukemiaInhibitorinhibithaematological malignanciesCLL T cellsCasein Kinasecancer
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