TGR-1202 hydrochloride |CAS:1532533-78-0 Probechem Biochemicals

Chemical Structure : TGR-1202 hydrochloride

CAS No.: 1532533-78-0

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

货号: 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.

规格	价格	库存
5 mg	￥980	In stock
10 mg	￥1580	In stock
50 mg	￥4880	In stock
100 mg	￥7580	In stock
200 mg		Get quote
1 g		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	608.0101
分子式	C31H25ClF3N5O3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
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)

参考文献

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.

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

生物&药学活性

物理化学性质&存储条件

参考文献

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

生物&药学活性

物理化学性质&存储条件

参考文献

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