Umbralisib (Synonyms: RP 5264, Umbralisib) |
| Katalog-Nr.GC19355 |
Umbralisib (TGR-1202) ist ein oral aktiver, potenter und selektiver dualer PI3Kδ- und Caseinkinase-1-ε (CK1ε)-Inhibitor mit EC50 von 22,2 nM bzw. 6,0 μM. Umbralisib zeigt einzigartige immunmodulatorische Wirkungen auf T-Zellen der chronischen lymphatischen LeukÄmie (CLL). Umbralisib kann fÜr die Erforschung hÄmatologischer Malignome verwendet werden.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1532533-67-7
Sample solution is provided at 25 µL, 10mM.
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TGR-1202 is a PI3Kδ inhibitor, with IC50 and EC50 of 22.2 nM and 24.3 nM, respectively.
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, TGR-1202 (10 nM-100 uM) inhibits phosphorylated AKT at Ser473 in a concentration-dependent manner. TGR-1202 and carfilzomib synergistically kill blood cancer cells through disrupting the 4E-BP1-eIF4F-c-Myc axis. TGR-1202 and carfilzomib in combination synergistically and selectively silence the c-Myc and E2F transcription programs. TGR-1202 (15-50 uM) 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, TGR-1202 (150 mg/kg, daily p.o.) significantly shrinks the tumors by day 25[2].
References:
[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
Average Rating: 5 (Based on Reviews and 33 reference(s) in Google Scholar.)
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