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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-PI3K-IOA-244
IOA-244

Chemical Structure : IOA-244

CAS No.: 1305267-37-1

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IOA-244 (Roginolisib, MSC2360844, IOA244)

货号: PC-20591Not For Human Use, Lab Use Only.

IOA-244 (Roginolisib, MSC2360844) is a potent, selective and non-ATP-competitive PI3Kδ inhibitor with IC50 of 19 nM, selective over PI3Kβ (0.43 uM), Vps34 (9 uM) and PI3Kα (10.1 uM).

规格 价格 库存 数量
5 mg ￥1580 In stock
10 mg ￥2480 In stock
25 mg ￥4280 In stock
50 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

IOA-244 (Roginolisib, MSC2360844) is a potent, selective and non-ATP-competitive PI3Kδ inhibitor with IC50 of 19 nM, selective over PI3Kβ (0.43 uM), Vps34 (9 uM) and PI3Kα (10.1 uM).
IOA-244 effectively inhibits proliferation of SU-DHL-6 (PI3Kδ harboring) with a GI50 of 0.24 uM.
IOA-244 limits proliferation of lymphoma cancer cells expressing high levels of PI3Kδ.
IOA-244 inhibits regulatory T cell proliferation while having limited antiproliferative effects on conventional CD4+ T cells and no effect on CD8+ T cells.
IOA-244 sensitized the tumors to anti-PD-1 treatment in CT26 colorectal and Lewis lung carcinoma lung cancer models, with similar activity in the Pan-02 pancreatic and A20 lymphoma syngeneic mouse models.

物理化学性质&存储条件

分子量 526.58
分子式 C26H27FN4O5S
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

(6-fluoro-1-(4-(morpholinomethyl)phenyl)-5,5-dioxido-1,4-dihydrothiochromeno[4,3-c]pyrazol-3-yl)(morpholino)methanone

参考文献

1. Haselmayer P, et al. Front Immunol 2014;5:233.

2. Johnson Z, et al. Cancer Res Commun. 2023 Apr 14;3(4):576-591.

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