TGR-1202 是一种PI3Kδ抑制剂，IC50=22.2 nM，EC50=24.3 nM。它同时可抑制CK1ε，EC50=6.0 μM。

TGR-1202 is a PI3Kδ inhibitor.

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 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.

1532533-67-7

C31H24F3N5O3

571.55

TGR1202;TGR-1202;TGR 1202;RP5264

DMSO:91 mg/mL(159.2 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years