Umbralisib (TGR-1202) sulfate is an orally active, potent and selective dualPI3Kδand casein kinase-1-ε (CK1ε) inhibitor, withEC₅₀of 22.2 nM and 6.0 μM, respectively. Umbralisib sulfate exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib sulfate can be used for haematological malignancies reseach^[1][2][3][4].

Umbralisib sulfate causes a half-maximal inhibition of human whole blood CD19 cell proliferation between 100-300 nM^[3].
In human lymphoma and leukemia cell lines, Umbralisib sulfate (10 nM-100 μM) inhibits phosphorylated AKT at Ser473 in a concentration-dependent manner^[4].
Umbralisib sulfate (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^[4].

Umbralisib sulfate (150 mg/kg, daily p.o.) significantly shrinks the tumors by day 25 in a subcutaneous xenograft model of T-cell acute lymphoblastic leukemia (T-ALL) in NOD/SCID mice using the MOLT-4 cell line^[4].

669.63

C₃₁H₂₆F₃N₅O₇S

1532533-75-7

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