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Umbralisib
CAS No. : 1532533-67-7
MCE 国际站：Umbralisib
产品活性：Umbralisib (TGR-1202) 是一种口服有效、选择性的 PI3Kδ 和 酪蛋白激酶-1-ε (CK1ε) 双抑制剂，其 EC50 分别为 22.2 nM 和 6.0 μM。Umbralisib 显示出对慢性淋巴细胞白血病 (CLL) T 细胞独特的免疫调节作用。Umbralisib 可用于血液系统恶性肿瘤的研究。
研究领域：PI3K/Akt/mTOR | Stem Cell/Wnt | Cell Cycle/DNA Damage
作用靶点：PI3K | Casein Kinase
In Vitro: Umbralisib causes a half-maximal inhibition of human whole blood CD19 cell proliferation between 100-300 nM.
Umbralisib (10 nM-100 μM) inhibits phosphorylated AKT at Ser473 in a concentration-dependent manner in human lymphoma and leukemia cell lines.
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: Umbralisib (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.
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