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

Chemical Structure : Parsaclisib

CAS No.: 1426698-88-5

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Parsaclisib (INCB050465, IBI-376)

货号: PC-60527Not For Human Use, Lab Use Only.

Parsaclisib (INCB050465) is a potent and highly selective PI3Kδ inhibitor with IC50 of < 1 nM (SPA).

规格 价格 库存 数量
2 mg ￥1480 In stock
5 mg ￥2580 In stock
10 mg ￥4280 In stock
25 mg ￥7280 In stock
50 mg Get quote
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

Parsaclisib (INCB050465) is a potent and highly selective PI3Kδ inhibitor with IC50 of < 1 nM (SPA).
Parsaclisib (INCB050465) displayed cellular activity in SU-DHL-6 viability (IC50=1.6 nM) and Pfeiffer proliferation (IC50=2.5 nM).
Parsaclisib (INCB050465) is very selective over the other PI3K isoforms (PI3Kα/β/γ FB IC50 vuales >10,000 nM), exhibits selectivity over a panel of 197 kinases and is very potent in the RAMOS cellular and human whole blood basophil assays.
Parsaclisib (INCB050465) dosed orally twice daily significantly inhibited Pfeiffer xenograft tumor growth at 1 mg/kg, with profound inhibition of the phosphorylation of AKT at Ser473, a marker of PI3Kδ activity, observed in mice models.|
Parsaclisib (INCB050465) directly blocks PI3K signaling-mediated cell proliferation in B-cell lines in vitro and in vivo and indirectly controls tumor growth by lessening immunosuppression through regulatory T-cell inhibition in a syngeneic lymphoma model.

物理化学性质&存储条件

分子量 432.88
分子式 C20H22ClFN6O2
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

>200 mM in DMSO (>86 mg/mL)
Chemical Name/SMILES

(4R)-4-{3-[(1S)-1-(4-amino-3-methyl-1H-pyrazolo[3,4- d]pyrimidin-1-yl)ethyl]-5-chloro-2-ethoxy- 6-fluorophenyl}pyrrolidin-2-one

参考文献

1. Shin N, et al. J Pharmacol Exp Ther. 2020 Jul;374(1):211-222.
2. Forero-Torres A, et al. Blood. 2019 Apr 18;133(16):1742-1752.
3. Yue EW, et al. ACS Med Chem Lett. 2019 Oct 17;10(11):1554-1560.

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