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

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

743.75

C₃₈H₃₂F₃N₅O₆S

1532533-72-4

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