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Umbralisib (TGR 1202) is a PI3Kδ inhibitor.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
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 |
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. |
Alias | 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 | Powder: -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
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