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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-PI3K-Umbralisib
Umbralisib

Chemical Structure : Umbralisib

CAS No.: 1532533-67-7

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Umbralisib (RP 5264;TGR1202;TGR-1202)

货号: 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.

规格 价格 库存 数量
10 mg ￥1280 In stock
25 mg ￥1980 In stock
50 mg ￥3280 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 571.5492
分子式 C31H24F3N5O3
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

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)-

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.

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