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IOA-244

Chemical Structure : IOA-244

CAS No.: 1305267-37-1

IOA-244 (Roginolisib, MSC2360844, IOA244)

Catalog No.: 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).

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Biological Activity

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.

Physicochemical Properties

M.Wt 526.58
Formula C26H27FN4O5S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
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

References

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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