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Chemical Structure : TGR-1202 hydrochloride
CAS No.: 1532533-78-0
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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $98 | In stock | |
| 10 mg | $158 | In stock | |
| 50 mg | $488 | In stock | |
| 100 mg | $758 | In stock | |
| 200 mg | Get quote | ||
| 1 g | Get quote |
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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.
| M.Wt | 608.0101 | |
| Formula | C31H25ClF3N5O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
DMSO: 100 mM (60.8 mg/mL) |
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| 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) |
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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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