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Umbralisib

Chemical Structure : Umbralisib

CAS No.: 1532533-67-7

Umbralisib (RP 5264;TGR1202;TGR-1202)

Catalog No.: PC-42941Not For Human Use, Lab Use Only.

Umbralisib (RP5264,TGR1202, TGR-1202) is a potent, selective, orally available PI3Kδ inhibitor with IC50 of 22 nM, 50-fold selectivity over PI3Kα/β and >10,000 fold over PI3Kγ.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Umbralisib (RP5264, TGR1202, TGR-1202) is a potent, selective, orally available PI3Kδ inhibitor with IC50 of 22 nM, 50-fold selectivity over PI3Kα/β and >10,000 fold over PI3Kγ.
TGR1202 enhances Brentuximab Vedotin-induced Hodgkin lymphoma cell death via mitotic arrest, demonstrates highly synergistic effect with the proteasome inhibitor carfilzomib in lymphoma, leukemia, and myeloma cell lines and primary lymphoma and leukemia cells
TGR1202 synergistically disrupts the 4E-BP1-eIF4F-c-Myc axis with carfilzomib, also potently inhibits 60% of the activity of CK1ε at 1 uM.

Physicochemical Properties

M.Wt 571.5492
Formula C31H24F3N5O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4H-1-Benzopyran-4-one, 2-[(1S)-1-[4-amino-3-[3-fluoro-4-(1-methylethoxy)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-1-yl]ethyl]-6-fluoro-3-(3-fluorophenyl)-

References

1. Locatelli SL, et al. Leukemia. 2016 Dec;30(12):2402-2405.

2. Deng C, et al. Blood. 2017 Jan 5;129(1):88-99.

3. Burris HA 3rd, et al. Lancet Oncol. 2018 Feb 20. pii: S1470-2045(18)30082-2.

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