Umbralisib hydrochloride (Synonyms: TGR-1202 hydrochloride; RP5264 hydrochloride) |
| Catalog No.GC37854 |
El clorhidrato de umbralisib (TGR-1202) es un inhibidor dual oralmente activo, potente y selectivo de PI3Kδ y caseÍna quinasa-1-ε (CK1ε), con EC50 de 22,2 nM y 6,0 μM, respectivamente. El clorhidrato de umbralisib exhibe efectos inmunomoduladores Únicos en las células T de la leucemia linfocÍtica crÓnica (LLC). El clorhidrato de umbralisib se puede utilizar para la investigaciÓn de neoplasias malignas hematolÓgicas.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1532533-78-0
Sample solution is provided at 25 µL, 10mM.
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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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