Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Umbralisib (TGR 1202) is a PI3Kδ inhibitor.
説明 | Umbralisib (TGR 1202) is a PI3Kδ inhibitor. |
ターゲット&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. |
別名 | TGR-1202, RP5264, TGR 1202, TGR1202 |
分子量 | 571.55 |
分子式 | 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. 詳細
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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