Umbralisib hydrochloride (Synonyms: TGR-1202 hydrochloride; RP5264 hydrochloride) |
Catalog No.GC37854 |
Umbralisib(TGR-1202) 염산염은 경구 활성, 강력하고 선택적인 이중 PI3Kδ 및 카제인 키나제-1-ε(CK1ε) 억제제이며 EC50은 각각 22.2nM 및 6.0μM입니다. Umbralisib 염산염은 만성 림프구성 백혈병(CLL) T 세포에 독특한 면역 조절 효과를 나타냅니다. Umbralisib 염산염은 혈액암 연구에 사용할 수 있습니다.
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Cas No.: 1532533-78-0
Sample solution is provided at 25 µL, 10mM.
Umbralisib hydrochloride (TGR-1202 hydrochloride) is a novel PI3Kδ inhibitor, with IC50 and EC50 of 22.2 nM and 24.3 nM, respectively; Umbralisib hydrochloride (TGR-1202 hydrochloride) is also active against CK1ε, with an EC50 value of 6.0 μM. PI3Kδ|22.2 nM (IC50)
Umbralisib (RP5264) causes a half-maximal inhibition of human whole blood CD19 cell proliferation between 100-300 nM[1]. In human lymphoma and leukemia cell lines, Umbralisib (TGR-1202; 10 nM-100 μM) inhibits phosphorylated AKT at Ser473 in a concentration-dependent manner. Umbralisib and carfilzomib synergistically kill blood cancer cells through disrupting the 4E-BP1-eIF4F-c-Myc axis. Umbralisib and carfilzomib 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[2].
In a subcutaneous xenograft model of T-cell acute lymphoblastic leukemia (T-ALL) in NOD/SCID mice using the MOLT-4 cell line, Umbralisib (TGR-1202; 150 mg/kg, daily p.o.) significantly shrinks the tumors by day 25[2].
[1]. Swaroop Vakkalankaa, et al. Inhibition of PI3Kδ kinase by a selective, small molecule inhibitor suppresses B-cell proliferation and leukemic cell growth. [2]. Deng C, et al. Silencing c-Myc translation as a therapeutic strategy through targeting PI3Kδ and CK1ε in hematological malignancies. Blood. 2017 Jan 5;129(1):88-99
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