Parsaclisib (INCB050465) | PI3Kδ inhibitor

Chemical Structure : Parsaclisib

CAS No.: 1426698-88-5

Parsaclisib (INCB050465, IBI-376)

Catalog No.: PC-60527Not For Human Use, Lab Use Only.

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

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2 mg	$148	In stock
5 mg	$258	In stock
10 mg	$428	In stock
25 mg	$728	In stock
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Biological Activity

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.

Physicochemical Properties

M.Wt	432.88
Formula	C20H22ClFN6O2
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	>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

References

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.

Parsaclisib (INCB050465, IBI-376)

Biological Activity

Physicochemical Properties

References

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