GSK2292767 |
Catalog No.GC15679
One-Click Copy Product Info
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PI3Kδ inhibitor,potent and selective
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1254036-66-2
Sample solution is provided at 25 µL, 10mM.
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pKi: 10.1
GSK2292767 is a potent and selective PI3Kδ inhibitor.
Phosphoinositide 3-kinase δ (PI3Kδ), a lipid kinase belonging to the class 1 PI3K family with the closely homologous isoforms α and β, catalyzes the phosphorylation of phosphatidylinositol 4,5-bisphosphate, triggering various downstream biological events suvch as cell growth, proliferation, differentiation, and survival.
In vitro: GSK2292767 was found to be greater than 100-fold selective against a panel of in-house kinases and in the Millipore panel. Moreover, GSK2292767 could inhibit both IFNγ and IL-2 production in a concentration-dependent manner in a human lung parenchyma assay, with pIC50s of 8.7 and 8.5, respectively [1].
In vivo: In a rat PK study, the in vivo clearance for GSK2292767 was significantly higher than that for its analog GSK2269557. The oral bioavailability was also low (F < 2%), which was consistent with the data observed for GSK2269557. In a rabbit cardiac ventricular wedge assay, no effect on QT interval, Tp e, or QRS and no significant risk of TdP arrhythmias was observed for GSK2292767 over the concentration range tested, thus indicating GSK2292767 could successfully mitigate the risk associated with GSK2269557. Moreover, GSK2292767 was found to protect against eosinophil recruitment with an ED50 of 35 μg/kg in the brown Norway rat acute OVA model, which was similar to GSK2269557 [1].
Clinical trial: The safety, tolerability and pharmacokinetics of single and repeat soses of GSK2292767 in healthy participants smokinf cigarettes is proposed, but this study is not yet open for participant recruitment [https://clinicaltrials.gov/ct2/show/NCT03045887].
Reference:
[1] Down K et al. Optimization of Novel Indazoles as Highly Potent and Selective Inhibitors of Phosphoinositide 3-Kinase δ for the Treatment of Respiratory Disease. J Med Chem. 2015 Sep 24;58(18):7381-99.
| Cas No. | 1254036-66-2 | SDF | |
| Chemical Name | N-(5-(4-(5-(((2R,6S)-2,6-dimethylmorpholino)methyl)oxazol-2-yl)-1H-indazol-6-yl)-2-methoxypyridin-3-yl)methanesulfonamide | ||
| Canonical SMILES | CS(=O)(NC1=CC(C2=CC3=C(C(C4=NC=C(CN5C[C@@H](C)O[C@@H](C)C5)O4)=C2)C=NN3)=CN=C1OC)=O | ||
| Formula | C24H28N6O5S | M.Wt | 512.58 |
| Solubility | DMF: 16 mg/ml,DMF:PBS(pH7.2) (1:2): 0.3 mg/ml,DMSO: 14 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9509 mL | 9.7546 mL | 19.5091 mL |
| 5 mM | 390.2 μL | 1.9509 mL | 3.9018 mL |
| 10 mM | 195.1 μL | 975.5 μL | 1.9509 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 3 reference(s) in Google Scholar.)