Nemiralisib


CAS No. : 1254036-71-9

(Synonyms: GSK2269557 (free base))

1254036-71-9
Price and Availability of CAS No. : 1254036-71-9
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1mg $84 In-stock
5mg $144 In-stock
10mg $228 In-stock
25mg $492 In-stock
50mg $852 In-stock
100mg $1440 In-stock
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Cat. No. : HY-19535A
M.Wt: 440.54
Formula: C26H28N6O
Purity: >98 %
Solubility: DMSO : 33.33 mg/mL (75.66 mM; Need ultrasonic)
Introduction of 1254036-71-9 :

Nemiralisib (GSK2269557 free base) is a potent and highly selective PI3Kδ inhibitor with a pKi of 9.9. IC50 & Target: pKi: 9.9 (PI3Kδ)[1]
pIC50: 5.3 (PI3Kα), 5.8 (PI3Kβ), 5.2 (PI3Kγ)[1] In Vitro: Nemiralisib (GSK2269557 free base) is highly selective for PI3Kδ, with >1000-fold selectivity over the closely related isoforms PI3Kα (pIC50=5.3), PI3Kβ (pIC50=5.8) and PI3Kγ (pIC50=5.2). Nemiralisib inhibits IFNγ in the peripheral blood mononuclear (PBMC) assay with an pIC50 of 9.7[1]. In Vivo: To assess the suitability of the series for inhaled delivery clearance data in rat microsomes and subsequently in vivo pharmacokinetic data from Sprague Dawley male rats is obtained. Compounds (e.g., Nemiralisib) are administered by the oral or intravenous routes, at a dose level of 3 and 1mg/kg respectively (n=2 rats/route). Nemiralisib free base is active in a disease relevant brown norway rat acute OVA model of Type 2 helper T-cells (Th2)-driven lung inflammation[1].

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