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TGR-1202 hydrochloride

Chemical Structure : TGR-1202 hydrochloride

CAS No.: 1532533-78-0

TGR-1202 hydrochloride (RP5264 hydrochloride;TGR1202 hydrochloride;TGR 1202 hydrochloride;RP-5264 hydrochloride;RP 5264 hydrochloride)

Catalog No.: PC-42942Not For Human Use, Lab Use Only.

TGR-1202 (RP5264,TGR1202,Umbralisib) 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

TGR-1202 (RP5264,TGR1202,Umbralisib) hydrochloride 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.
TGR-1202 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.
TGR-1202 synergistically disrupts the 4E-BP1-eIF4F-c-Myc axis with carfilzomib, also potently inhibits 60% of the activity of CK1ε at 1uM.

Physicochemical Properties

M.Wt 608.0101
Formula C31H25ClF3N5O3
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

DMSO: 100 mM (60.8 mg/mL)

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)-, hydrochloride (1:1)

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.

4. Lampson BL, et al. Expert Opin Investig Drugs. 2017 Nov;26(11):1267-1279.

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