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  2. PI3K
  3. IPI-3063

IPI-3063 

Cat. No.: HY-111510 Purity: 98.80%
Handling Instructions

IPI-3063 is a potent and selective PI3K p110δ inhibitor with an IC50 of 2.5 ± 1.2 nM.

For research use only. We do not sell to patients.

IPI-3063 Chemical Structure

IPI-3063 Chemical Structure

CAS No. : 1425043-73-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 220 In-stock
Estimated Time of Arrival: December 31
2 mg USD 120 In-stock
Estimated Time of Arrival: December 31
5 mg USD 220 In-stock
Estimated Time of Arrival: December 31
10 mg USD 360 In-stock
Estimated Time of Arrival: December 31
25 mg USD 720 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

IPI-3063 is a potent and selective PI3K p110δ inhibitor with an IC50 of 2.5 ± 1.2 nM.

IC50 & Target[1]

p110δ

2.5 nM (IC50)

p110α

1170 nM (IC50)

p110β

1508 nM (IC50)

p110γ

2187 nM (IC50)

In Vitro

IPI-3063 inhibits p110α, p110β, and p110γ with IC50s of 1171±533 nM, 1508±624 nM, and 2187±1529 nM, respectively. IPI-3063 potently reduces mouse B cell proliferation, survival, and plasmablast differentiation while increasing antibody class switching to IgG1. IPI-3063 is a p110δ selective compound with an IC50=0.1 nM in p110δ-specific cell-based assays and cellular IC50 values for the other class I PI3K isoforms are at least 1,000-fold higher (IC50=1901±1318 nM for p110α, IC50=102.8±35.7 nM for p110β, IC50=418.8±117.2 nM for p110γ). IPI-3063 is very potent in reducing p-AKT (significant effect at 1 nM). IPI-3063 also reduces p-ERK1/2 with a significant effect at 10 nM. IPI-3063 is very potent, achieving a significant decrease in B cell survival when present at 10 nM[1].

Molecular Weight

455.51

Formula

C₂₅H₂₅N₇O₂

CAS No.

1425043-73-7

SMILES

N#CC1=C(N[[email protected]](C2=CC3=C(C(N2C(C)C)=O)C(C(C=C4)=CN(C)C4=O)=CC=C3)C)N=CN=C1N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 83.33 mg/mL (182.94 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1953 mL 10.9767 mL 21.9534 mL
5 mM 0.4391 mL 2.1953 mL 4.3907 mL
10 mM 0.2195 mL 1.0977 mL 2.1953 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

Human recombinant PI3K-α, PI3K-β, PI3K-δ, and PI3K-γ are used. Phosphatidylinositol 4,5 bis phosphate (diC8-PtdIns(4,5)P2) is used. PI3K-α, β, and δ are heterodimers consisting of full length p110α, p110β, or p110δ catalytic subunit and the p85α regulatory subunit. PI3K-γ is a monomer of the p110γ catalytic subunit. Samples of kinase (10 nM-α, β, and δ; 20 nM-γ) are incubated with IPI-3063 for 30 min at room temperature in reaction buffer (15 mM HEPES pH 7.4, 20 mM NaCl, 1 mM EGTA, 0.02% Tween 20, 10 mM MgCl2, 0.2 mg/mL bovine-γ-globulins) followed by addition of ATP/diC8-PtdIns(4,5)P2 mixture to give final concentrations of 3 mM ATP and 500 µM diC8-PtdIns(4,5)P2. Reactions are incubated at room temperature for 2 h, with PI3K activity is assessed. Plates are read on plate reader in luminescence mode[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

Peripheral blood mononuclear cells (PBMCs) are first purified from blood by density gradient centrifugation. Human B cells are then purified from PBMCs by negative selection. B-cell purity is increased from 4% to >70% as measured by FACS analysis using anti-CD19 PE conjugated antibody. Purified B cells are seeded at a final concentration of 0.1×106 cells/mL and cultured with 2 µg/mL human CD40L+5 µg/mL anti-human IgM/IgG+100 µg/mL hIL-2+100 µg/mL hIL-21. All B cells are cultured in RPMI 1640 supplemented with 10% (vol/vol) heat-inactivated FCS, 5 mM Hepes, 2 mM L-glutamine, 100 U/mL Penicillin, 100 µg/mL Streptomycin, 50 µM 2-mercaptoethanol. Purified human B cells are pretreated with IPI-3063 (0.1, 1, 10, and 100 nM) for 30 min, then stimulated with human CD40L+anti-human IgM/IgG+human IL-2+human IL-21 for 120 h[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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KeyWords:

IPI-3063 | IPI3063 | IPI 3063 | PI3K | Phosphoinositide 3-kinase | Inhibitor | inhibitor | inhibit

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IPI-3063
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