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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

Umbralisib

🥰Excellent
Purity: 99.83%
Catalog No. T4976Alias TGR-1202, TGR1202, TGR 1202, RP5264Cas No. 1532533-67-7
Umbralisib (TGR 1202) is a PI3Kδ inhibitor.
Pack SizePriceAvailabilityQuantity
1 mg$41In Stock
2 mg$59In Stock
5 mg$97In Stock
10 mg$178In Stock
25 mg$360In Stock
50 mg$473In Stock
100 mg$693In Stock
1 mL x 10 mM (in DMSO)$123In Stock
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Purity:99.83%
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Product Introduction

Bioactivity
Description
Umbralisib (TGR 1202) is a PI3Kδ inhibitor.
Targets&IC50
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.
AliasTGR-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.
Solubility Information
DMSO: 91 mg/mL (159.2 mM)
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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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 μLddH2OTargetMol | reagent mix well and clarify
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