| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Targets |
Phosphoinositide 3-kinase gamma (PI3Kγ / PIK3CG). PI3Kγ is a Class IB PI3K that is primarily expressed in leukocytes and plays a critical role in immune cell signaling, migration, and inflammation. AZ2 is a highly selective inhibitor of the active state of PI3Kγ with a pIC50 of 9.3.
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| ln Vitro |
By constitutively activating the PI3K/Akt pathway, AZ2 (0.1~100 nM; 1 hour; SKOV-3 cells) demonstrated high selectivity for PI3Kγ [1].
In vitro, AZ2 demonstrates high selectivity for PI3Kγ with a pIC50 of 9.3. By constitutively activating the PI3K/Akt pathway, AZ2 shows potent inhibition of PI3Kγ in cellular assays at concentrations ranging from 0.1-100 nM. The compound's selectivity for the active state of PI3Kγ distinguishes it from other PI3K inhibitors that may not discriminate between active and inactive conformations. |
| ln Vivo |
In vivo, AZ2 is used in research for inflammatory and immune disorders. Its selectivity for PI3Kγ allows for investigation of the specific role of this kinase in immune cell function and inflammation. The compound's activity in animal models helps to validate PI3Kγ as a therapeutic target for inflammatory diseases. Preclinical studies have explored its efficacy in models of autoimmune and inflammatory conditions.
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| Enzyme Assay |
Cell-free kinase assays for AZ2 use recombinant human PI3Kγ and a lipid substrate (phosphatidylinositol-4,5-bisphosphate, PIP2) in the presence of ATP. The compound is incubated with the enzyme at varying concentrations (0.001-10000 nM) for 30-60 minutes at room temperature. PI3K activity is measured by detecting the production of phosphatidylinositol-3,4,5-trisphosphate (PIP3) using a competitive ELISA, AlphaScreen, or radiometric assay. pIC50 values are calculated from dose-response curves. Selectivity profiling is performed against other PI3K isoforms (α, β, δ) and related kinases.
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| Cell Assay |
Cellular assays for AZ2 use immune cell lines (e.g., macrophages, neutrophils, or T cells) or PI3Kγ-expressing cell lines such as SKOV-3 cells. Cells are seeded in 96-well plates and treated with AZ2 at concentrations ranging from 0.01-1000 nM for 1-24 hours. PI3K/Akt pathway inhibition is assessed by Western blot analysis of phosphorylated AKT (Ser473) and downstream effectors. Cell migration assays are performed using transwell or scratch wound healing assays. Cytokine production is measured by ELISA. IC50 values are determined from dose-response curves.
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| Animal Protocol |
In vivo efficacy studies are conducted in mouse models of inflammatory or immune disorders (e.g., arthritis, colitis, or asthma). AZ2 is administered via oral gavage or intraperitoneal injection at doses typically ranging from 1-30 mg/kg. Disease severity is monitored by clinical scoring, histopathological assessment of tissue, and measurement of inflammatory cytokine levels in serum or tissue. Pharmacodynamic studies assess PI3K/Akt pathway inhibition in target tissues by Western blot or immunohistochemistry.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of AZ2 are consistent with small molecule PI3K inhibitors. The compound is expected to have reasonable oral bioavailability and sufficient plasma exposure for in vivo efficacy studies. Detailed PK parameters (Cmax, Tmax, AUC, t1/2, clearance, volume of distribution) are determined in preclinical species. Metabolic stability and protein binding are assessed using standard in vitro assays. The compound's favorable PK properties support its use in preclinical models of inflammatory diseases.
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| Toxicity/Toxicokinetics |
Toxicological data for AZ2 are limited to preclinical research studies. As a PI3Kγ inhibitor, potential toxicities may include effects on immune function and increased susceptibility to infections. The compound's high selectivity for PI3Kγ over other PI3K isoforms may reduce off-target toxicities. Standard toxicology studies would be required for clinical development. At research-grade doses, the compound is handled with standard laboratory safety precautions.
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| References | |
| Additional Infomation |
AZ2 is a research compound for studying PI3Kγ biology and validating PI3Kγ as a therapeutic target in inflammatory and immune disorders. It is not an approved drug and has not entered clinical trials. The compound is available from chemical suppliers for research purposes only. Its high selectivity for the active state of PI3Kγ makes it a valuable tool for dissecting the role of PI3Kγ in immune cell function. The compound should be stored at -20°C and handled according to standard laboratory safety protocols.
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| Molecular Formula |
C20H23N3O2S
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|---|---|
| Molecular Weight |
369.480523347855
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| Exact Mass |
369.151
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| CAS # |
2231760-33-9
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| PubChem CID |
134163708
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| Appearance |
White to off-white solid powder
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| LogP |
3.1
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
26
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| Complexity |
581
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C(NC1=NC(C)=C(C2C=C(C)C3=C(C=2)CN([C@H](C2CC2)C)C3=O)S1)(=O)C
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| InChi Key |
CNCRCDLWUGCPSJ-LBPRGKRZSA-N
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| InChi Code |
InChI=1S/C20H23N3O2S/c1-10-7-15(18-11(2)21-20(26-18)22-13(4)24)8-16-9-23(19(25)17(10)16)12(3)14-5-6-14/h7-8,12,14H,5-6,9H2,1-4H3,(H,21,22,24)/t12-/m0/s1
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| Chemical Name |
N-[5-[2-[(1S)-1-cyclopropylethyl]-7-methyl-1-oxo-3H-isoindol-5-yl]-4-methyl-1,3-thiazol-2-yl]acetamide
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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 |
| 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 : ~50 mg/mL (~135.33 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.77 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.77 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7065 mL | 13.5325 mL | 27.0651 mL | |
| 5 mM | 0.5413 mL | 2.7065 mL | 5.4130 mL | |
| 10 mM | 0.2707 mL | 1.3533 mL | 2.7065 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.
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