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Purity: ≥98%
IPI-3063 is a potent and selective PI3K p110δ inhibitor with IC50 of 2.5 ± 1.2 nM and IC50 values of >1000 nM for other classes of PI3K isoforms (p110α, p110β, p110γ). IPI-3063 inhibits p110α, p110β, and p110γ with respective IC50 values of 1171±533 nM, 1508 nM, and 2187±1529 nM. IPI-3063 significantly increases antibody class switching to IgG1 while significantly decreasing mouse B cell proliferation, survival, and plasmablast differentiation. IPI-3063 has a significant effect at 1 nM and is very effective at lowering p-AKT. Additionally, at 10 nM, IPI-3063 significantly lowers p-ERK1/2. IPI-3063 is extremely potent; at 10 nM, it significantly reduces B cell survival.
| Targets |
p110δ (IC50 = 2.5 nM); p110α (IC50 = 1170 nM); p110β (IC50 = 1508 nM); p110γ (IC50 = 2187 nM)
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| ln Vitro |
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. IPI-3063 significantly lowers mouse B cell survival, proliferation, and plasmablast differentiation[1].
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| ln Vivo |
IPI-3063 has good pharmacokinetics in mice[1].
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| Enzyme Assay |
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 and are heterodimers made up of the p85α regulatory subunit and the full-length p110α, p110β, or p110δ catalytic subunit. The catalytic subunit p110γ has a monomer called PI3K-γ. 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 for 2 hours at room temperature, and PI3K activity is measured. Plate readers are used to read plates in luminescence mode.
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| Cell Assay |
Purified mouse B cells are incubated for 48 hours in either interleukin-4 (IL-4) or B-cell activating factor (BAFF), along with varying concentrations of IPI-3063 and IPI-443.
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| Animal Protocol |
Brown Norway rats
50 mg/kg oral administration |
| References |
| Molecular Formula |
C25H25N7O2
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| Molecular Weight |
455.52
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| Exact Mass |
455.207
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| Elemental Analysis |
C, 65.92; H, 5.53; N, 21.52; O, 7.02
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| CAS # |
1425043-73-7
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| Related CAS # |
IPI-3063; IPI 3063; IPI3063.;
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| Appearance |
Solid powder
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| SMILES |
C[C@@H](C1=CC2=C(C(=CC=C2)C3=CN(C(=O)C=C3)C)C(=O)N1C(C)C)NC4=NC=NC(=C4C#N)N
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| InChi Key |
OBHAYOJCPNWKBL-HNNXBMFYSA-N
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| InChi Code |
InChI=1S/C25H25N7O2/c1-14(2)32-20(15(3)30-24-19(11-26)23(27)28-13-29-24)10-16-6-5-7-18(22(16)25(32)34)17-8-9-21(33)31(4)12-17/h5-10,12-15H,1-4H3,(H3,27,28,29,30)/t15-/m0/s1
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| Chemical Name |
4-amino-6-[[(1S)-1-[8-(1-methyl-6-oxopyridin-3-yl)-1-oxo-2-propan-2-ylisoquinolin-3-yl]ethyl]amino]pyrimidine-5-carbonitrile
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~91 mg/mL (~117.1 mM)
Ethanol: ~12 mg/mL (~26.3 mM) |
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| Solubility (In Vivo) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1953 mL | 10.9765 mL | 21.9529 mL | |
| 5 mM | 0.4391 mL | 2.1953 mL | 4.3906 mL | |
| 10 mM | 0.2195 mL | 1.0976 mL | 2.1953 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Inhibition of p110δ, but not p110γ, reduces p-AKT and p-ERK1/2 in αIgM + IL-4 stimulated mouse B cells.Front Immunol.2017 Jun 30;8:747. |
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IPI-3063 potently inhibits mouse B cell survival.Front Immunol.2017 Jun 30;8:747. |
 IPI-3063 potently inhibits mouse B cell proliferation.Front Immunol.2017 Jun 30;8:747. |
 IPI-3063 potently inhibits human B cell proliferation.Front Immunol.2017 Jun 30;8:747. |
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 IPI-3063 potently promotes mouse B cell antibody switching and inhibits plasmablast differentiation.Front Immunol.2017 Jun 30;8:747. |
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