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Umbralisib

CAS No. : 1532533-67-7

MCE 站：Umbralisib

产品活性：Umbralisib (TGR-1202) 是 PI3Kδ 抑制剂，IC₅₀ 和 EC₅₀ 值分别为 22.2 nM 和 24.3 nM；Umbralisib (TGR-1202) 同时可抑制 CK1ε，EC₅₀ 值为 6.0 μM。

研究领域：PI3K/Akt/mTOR

作用靶点：PI3K

In Vitro: Umbralisib (RP5264) causes a half-maximal inhibition of human whole blood CD19 cell proliferation between 100-300 nM. In human lymphoma and leukemia cell lines, Umbralisib (RP5264; 10 nM-100 μM) inhibits phosphorylated AKT at Ser473 in a concentration-dependent manner. Umbralisib and PR-171 synergistically kill blood cancer cells through disrupting the 4E-BP1-eIF4F-c-Myc axis. Umbralisib and PR-171 in combination synergistically and selectively silence the c-Myc and E2F transcription programs. Umbralisib (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, Umbralisib (RP5264; 150 mg/kg, daily p.o.) significantly shrinks the tumors by day 25.

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