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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
🥰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 Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 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]
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Batch Information
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Purity:99.56%
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Product Introduction
Bioactivity
Chemical Properties
| Description | Umbralisib (TGR 1202) is a PI3Kδ inhibitor. |
| Targets&IC50 | PI3Kγ:1400 nM (Kd), PI3Kδ:22.2 nM, PI3Kβ:>10000 nM (Kd), PI3Kα:>10000 nM (Kd), PI3Kδ:6.2 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. |
| Synonyms | TGR-1202, TGR1202, TGR 1202, RP5264 |
| 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. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Calculator
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 . A total of 10 animals were administered, and the formula you used is 5% 
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 DMSO (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.
(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 main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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
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