IC-87114 371242-69-2

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Molecular Weight: 397.43 IC-87114 is a selective PI3Kδ inhibitor with IC50 of 0.5 μM, 58-fold more selective for PI3Kδ than PI3Kγ, and over 100-fold more selective than PI3Kα/β.


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 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).


Protocol(Only for Reference)


Kinase Assay:


[1]

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 μL reaction volumes in 20 mM HEPES, pH 7.4, buffer containing 1 nM PI3K, 1 µM PIP2, 200 µM ATP, 1 µCi [γ-32P]ATP, 5 mM MgCl2, plus 50 µg/mL horse IgG as carrier protein. The reaction is incubated for 10 min at room temperature, quenched in 140 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.

Cell Assay:


[2]

Cell lines	Human bone marrow mononuclear cells (BMMCs) and CD34+ cells
Concentrations	0–100 μM
Incubation Time	48 hours
Method	For AML cell proliferation assay, BMMCs are isolated and cultured in α-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 μCi [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 μM IC87114 and pulsed for 12 hours with [3H]-thymidine.

Animal Study:


[3]

Animal Models	Wild-type or PI3Kδ mutant (p110δD910A) mice (C57BL/6 or BALB/c)
Formulation	Dissolved in 75% PEG200
Dosages	15 mg/kg–60 mg/kg
Administration	Oral gavage
Solubility	30% PEG400/0.5% Tween80/5% propylene glycol, 30 mg/mL
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Baboon	Dog	Monkey	Rabbit	Guinea pig	Rat	Hamster	Mouse
Weight (kg)	12	10	3	1.8	0.4	0.15	0.08	0.02
Body Surface Area (m2)	0.6	0.5	0.24	0.15	0.05	0.025	0.02	0.007
Km factor	20	20	12	12	8	6	5	3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×	mouse Km(3)	= 11.2 mg/kg
	rat Km(6)

Chemical Information

Molecular Weight (MW)	397.43
Formula	C22H19N7O
CAS No.	371242-69-2

Storage	3 years -20℃Powder
	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms

Solubility (25°C) *	In vitro	DMSO	0.66 mg/mL (1.66 mM)
		Water	<1 mg/mL (
		Ethanol	<1 mg/mL (
	In vivo	30% PEG400/0.5% Tween80/5% propylene glycol	30 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Name	2-((6-amino-9H-purin-9-yl)methyl)-5-methyl-3-o-tolylquinazolin-4(3H)-one

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