| Identification | Back Directory | [Name]
2-[(6-Amino-9H-purin-9-yl)methyl]-5-methyl-3-(2-methylphenyl)-4(3H)-quinazolinone | [CAS]
371242-69-2 | [Synonyms]
IC-87114
IC-87114, >=98%
IC-87114 (PIK-293)
IC-87114 (IC87114)
IC87114 (PI3-K delta inhibitor)
2-[(6-Amino-9H-purin-9-yl)methyl]-5-methyl-3-(2-methylphenyl)-4(3H)-quinazolinone
4(3H)-Quinazolinone, 2-[(6-aMino-9H-purin-9-yl)Methyl]-5-Methyl-3-(2-Methylphenyl)-
2-[(6-Amino-9H-purin-9-yl)methyl]-5-methyl-3-(2-methylphenyl)-4(3H)-quinazolinone IC-87114 | [Molecular Formula]
C22H19N7O | [MDL Number]
MFCD09970845 | [MOL File]
371242-69-2.mol | [Molecular Weight]
397.43 |
| Chemical Properties | Back Directory | [Boiling point ]
673.7±65.0 °C(Predicted) | [density ]
1.43 | [storage temp. ]
Store at -20°C | [solubility ]
insoluble in H2O; insoluble in EtOH; ≥6.62 mg/mL in DMF | [form ]
White powder solid. | [pka]
3.90±0.10(Predicted) | [color ]
White to gray | [CAS DataBase Reference]
371242-69-2 |
| Hazard Information | Back Directory | [Definition]
ChEBI: A member of the class of quinazolines that is quinazolin-4(3H)-one carrying (6-amino-9H-purin-9-yl)methyl, 2-methylphenyl and methyl substituents at positions 2, 3 and 5 respectively. | [Uses]
IC 87114 is a selective PI3Kδ inhibitor. | [target]
PI3Kδ | [storage]
Store at -20°C | [References]
[1]. workman p, van montfort rl. pi(3) kinases: revealing the delta lady. nat chem biol. 2010 feb;6(2):82-3.
[2]. puri kd, doggett ta, douangpanya j, hou y, tino wt, wilson t, graf t, clayton e, turner m, hayflick js, diacovo tg. mechanisms and implications of phosphoinositide 3-kinase delta in promoting neutrophil trafficking into inflamed tissue. blood. 2004 may 1;103(9):3448-56.
[3]. soond dr, bj?rgo e, moltu k, dale vq, patton dt, torgersen km, galleway f, twomey b, clark j, gaston js, taskén k, bunyard p, okkenhaug k. pi3k p110delta regulates t-cell cytokine production during primary and secondary immune responses in mice and humans. blood. 2010 mar 18;115(11):2203-13. |
| Questions And Answer | Back Directory | [Description]
IC-87114 is a selective PI3Kδ inhibitor with IC50 of 0.5 μM in a cell-free assay, 58-fold more selective for PI3Kδ than PI3Kγ, and over 100-fold more selective than PI3Kα/β. | [In vitro]
IC-87114 selectively inhibits PI3Kδ and not sensitive to PI3Kα, β, and γ. In human neutrophils, IC87114 (5 µM) potently inhibits N-formyl-methionyl-leucyl-phenylalanine (fMLP)-stimulated phosphatidylinositol triphosphate (PIP3) biosynthesis and chemotaxis. IC87114 (5 µM) also inhibits polarized morphology and spreading of neutrophils. In human acute myeloid leukemia (AML) blast cells, such as bone marrow mononuclear cells (BMMCs), IC87114 (10 µM) inhibits both constitutive and Flt-3-stimulated Akt phosphorylation and cell proliferation. It is also found that IC87114 (5 µM–30 µM) inhibits SCF-or IL-3-stimulated BMMC responses, which are not observed in PI3Kδ mutant (p110δD910A) cells. In anti-CD3-stimulated mice CD62L+ (naive) and CD62L− (effector/memory) CD4+ T cells, IC87114 inhibits proliferation and interferon-gamma (IFN-γ) production. The IC50 values of IC87114 are: (1) 1.2 µM and 40 nM, for CD62L+ and CD62L− cell proliferation, respectively; (2) 120 nM and 1 nM, for IFN-γ production of CD62L+ and CD62L− cells, respectively. Similar effects by IC87114 are also observed in human T cells. A recent study reveals that in chromaffin cells, IC87114 enhances the transient increase of PtdIns(4,5)P2, which results in a potentiation of exocytosis. | [In vivo]
In mice, IC87114 (15 mg/kg–60 mg/kg) inhibits the allergic response in the back skin and ear. In mice induced with anti-CD3 or ConA, IC87114 (30 mg/kg) reduces hypersensitivity responses and decreases plasma levels of cytokines, such as IL-2, IL-4, IL-17, IFN-γ, and tumor necrosis factor-α (TNF-α). |
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