Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Umbralisib (TGR 1202) is a PI3Kδ inhibitor.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 41.00 | |
2 mg | In stock | $ 59.00 | |
5 mg | In stock | $ 97.00 | |
10 mg | In stock | $ 178.00 | |
25 mg | In stock | $ 360.00 | |
50 mg | In stock | $ 473.00 | |
100 mg | In stock | $ 693.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 123.00 |
Description | Umbralisib (TGR 1202) is a PI3Kδ inhibitor. |
Targets&IC50 | PI3Kδ:22.2 nM |
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. |
Synonyms | TGR-1202, RP5264, TGR 1202, TGR1202 |
Molecular Weight | 571.55 |
Formula | C31H24F3N5O3 |
CAS No. | 1532533-67-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 91 mg/mL(159.2 mM)
You can also refer to dose conversion for different animals. More
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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.
Umbralisib 1532533-67-7 PI3K/Akt/mTOR signaling PI3K inhibit TGR-1202 RP5264 lymphocytic leukemia lymphoma RP-5264 CLL T cells Inhibitor haematological malignancies cancer orally active RP 5264 TGR 1202 TGR1202 Phosphoinositide 3-kinase Casein Kinase inhibitor