IC-87114

ArtNr	S1268-10
Hersteller	Selleckchem
CAS-Nr.	371242-69-2
Menge	10 mg
Quantity options	1 mg 10 mg 1 g 10 g 200 mg 5 mg 50 mg 5 g
Kategorie	Oncology Neuroscience Neuroinflammation Metabolism Diabetes Glucose Homeostasis Aging & Neurological Disorders Inhibitors & Compound Libraries Small Molecules By Organ Heart & Blood Cancer Bone Cancer
Typ	Inhibitors
Specific against	other
Smiles	CC1=C2C(=CC=C1)N=C(N(C2=O)C3=CC=CC=C3C)CN4C=NC5=C(N=CN=C54)N
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	371242-69-2'
Similar products	IC-87114
Lieferbar
Manufacturer - Targets	PI3K
Storage Conditions	2 years -80 in solvent
Molecular Weight	397, 43
Administration	Oral gavage
Animal Models	Wild-type or PI3Kdelta mutant (p110deltaD910A) mice (C57BL/6 or BALB/c)
Cell lines	Human bone marrow mononuclear cells (BMMCs) and CD34+ cells
Concentrations	0â€“100 uM
Dosages	15 mg/kgâ€“60 mg/kg
Formulation	Dissolved in 75% PEG200
IC50	0.5 uM, 0.5 uM, 0.5 uM, 0.5 uM, 0.5 uM, 0.5 uM
In vitro	IC-87114 selectively inhibits PI3Kdelta and not sensitive to PI3Kalpha, beta, and gamma. In human neutrophils, IC87114 (5 uM) potently inhibits N-formyl-methionyl-leucyl-phenylalanine (fMLP)-stimulated phosphatidylinositol triphosphate (PIP3) biosynthesis and chemotaxis. IC87114 (5 uM) also inhibits polarized morphology and spreading of neutrophils. [1] In human acute myeloid leukemia (AML) blast cells, such as bone marrow mononuclear cells (BMMCs), IC87114 (10 uM) inhibits both constitutive and Flt-3-stimulated Akt phosphorylation and cell proliferation. [2] It is also found that IC87114 (5 uMâ€“30 uM) inhibits SCF- or IL-3-stimulated BMMC responses, which are not observed in PI3Kdelta mutant (p110deltaD910A) cells. [3] In anti-CD3-stimulated mice CD62L+ (naive) and CD62L (effector/memory) CD4+ T cells, IC87114 inhibits proliferation and interferon-gamma (IFN-gamma) production. The IC50 values of IC87114 are: (1) 1.2 uM and 40 nM, for CD62L+ and CD62L cell proliferation, respectively, (2) 120 nM and 1 nM, or IFN-gamma production of CD62L+ and CD62L cells, respectively. Similar effects by IC87114 are also observed in human T cells. [4] 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. [5]
In vivo	In mice, IC87114 (15 mg/kgâ€“60 mg/kg) inhibits the allergic response in the back skin and ear. [3] 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-gamma, and tumor necrosis factor-alpha (TNF-alpha). [4]
Incubation Time	48 hours
Kinase Assay	PI3K kinase assay, Phosphatidylinositol-(4, 5)-bisphosphate (PIP2) containing phospholipid liposomes are prepared. Briefly, bovine PIP2 and phosphatidylserine (1:2 molar ratio) are vacuum-dried and resuspended at 1 mM PIP2 in 20 mM HEPES-KOH, pH 7.4, 50 mM NaCl, and 5 mM EDTA. The lipid suspension is subjected to a brief sonication, followed by 5 freeze-thaw cycles and then 20 extrusion cycles to produce the liposomes. The assay is conducted in 60 uL reaction volumes in 20 mM HEPES, pH 7.4, buffer containing 1 nM PI3K, 1 uM PIP2, 200 uM ATP, 1 uCi [gamma-32P]ATP, 5 mM MgCl2, plus 50 ug/mL horse IgG as carrier protein. The reaction is incubated for 10 min at room temperature, quenched in 140 uL of 1 M K2PO4, 30 mM EDTA, pH 8.0, captured onto a 96-well polyvinylidene difluoride filter plate, and washed five times with 1 M K2PO4. The filter is allowed to dry completely, and the bound radioactivity is quantitated. IC87114 dilutions are assayed in a final concentration of 1% (w/w) DMSO.
Method	For AML cell proliferation assay, BMMCs are isolated and cultured in alpha-medium with 5% fetal calf serum (FCS) with or without FLT-3 ligand (10 ng/mL) for 48 hours and with or without IC87114. [3H]-thymidine (1 uCi [37 kBq]) is added for a final 6 hours and the amount of radioactivity incorporated is determined by trichloracetic acid precipitation. CD34+ cells from cord blood are cultured in stem cell factor (SCF, 20 ng/mL), FLT-3 ligand (10 ng/mL), and Tpo (20 nM) for 48 hours with or without 10 uM IC87114 and pulsed for 12 hours with [3H]-thymidine.
Solubility (25C)	DMSO 0.66 mg/mL, Water <1 mg/mL, Ethanol <1 mg/mL
Information	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.
Chemical Name	2-((6-amino-9H-purin-9-yl)methyl)-5-methyl-3-o-tolylquinazolin-4(3H)-one

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