PI3kδ inhibitor 1 |
| カタログ番号GC36911 |
PI3kδインヒビター 1 は、IC50 が 3.8 nM の強力で選択的な PI3Kδ インヒビターです。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1332075-63-4
Sample solution is provided at 25 µL, 10mM.
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PI3kδ inhibitor 1 is a potent and selective PI3Kδ inhibitor with an IC50 of 3.8 nM. PI3Kδ|3.8 nM (IC50)
PI3kδ inhibitor 1 (Compound 3) is a potent inhibitor of PI3Kδ that is 200-400 fold selective for all three remaining Class I PI3K isoforms and extremely selective relative to 239 kinases tested in SelectScreen service (0/239 kinases showing >50% inhibition when tested at 1 μM; mTOR, DNA-PK, VPS34, PI4Kα and PI4Kβ are inhibited at 10% or less when tested at 1 μM; PIKC2A and PIKC2B are inhibited at 11% and 42%, respectively, at this same concentration and show less than 10% inhibition when tested at 0.1 μM; the PIKK family kinases ATM and ATR are not assessed)[1].
The pharmacokinetic properties of PI3kδ inhibitor 1 (Compound 3) are evaluated in mice and rats when dosed IV and orally. Good plasma exposures and reasonable half-lives are observed upon oral dosing, a reflection of high oral bioavailability (80% and 90% at a low dose for mouse and rat, respectively), moderate volume of distribution, and moderate clearance. PI3kδ inhibitor 1 has moderate terminal elimination half-life (t1/2=2.6 h, 2.9 h, 5 h, 2.6, 3.8 and 4.8 h for mouse (5 mg/kg, po), mouse (20 mg/kg, po), mouse (40 mg/kg, po), rat (5 mg/kg, po), rat (10 mg/kg, po), rat (30 mg/kg, po)). Plasma exposures and Cmax levels increase with dose in both mice and rats, important in that inflammatory disease models utilize these two species. Plasma protein binding for PI3kδ inhibitor 1 ranges from 80-88% in rodents and is consistent with values obtained in human plasma (86%)[1].
[1]. Sutherlin DP, et al. Potent and selective inhibitors of PI3Kδ: obtaining isoform selectivity from the affinity pocket and tryptophan shelf. Bioorg Med Chem Lett. 2012 Jul 1;22(13):4296-302.
Animal experiment: | Mice and Rats[1]Female mice are dosed IV (intravenously) with PI3kδ inhibitor 1 in 5% DMSO/5% Cremephor and PO (orally) as an MCT suspension (0.5% methylcellulose/0.2% Tween-80). The IV (1 mg/kg) and PO (5, 20 and 40 mg/kg) studies are performed in CD-1 mice while the higher dose studies are performed in the Balb/c strain. Male Sprague-Dawley rats are dosed with the same IV (1 mg/kg) and PO (5, 10 and 30 mg/kg) formulations as those used for mice. |
References: [1]. Sutherlin DP, et al. Potent and selective inhibitors of PI3Kδ: obtaining isoform selectivity from the affinity pocket and tryptophan shelf. Bioorg Med Chem Lett. 2012 Jul 1;22(13):4296-302. | |
| Cas No. | 1332075-63-4 | SDF | |
| Canonical SMILES | CC(O)(C1CCN(CC2=NC3=C(N4CCOCC4)N=C(C5=C(F)C=CC6=C5C=CN6)N=C3C=C2)CC1)C | ||
| Formula | C28H33FN6O2 | M.Wt | 504.6 |
| 溶解度 | Soluble in DMSO | 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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.9818 mL | 9.9088 mL | 19.8177 mL |
| 5 mM | 0.3964 mL | 1.9818 mL | 3.9635 mL |
| 10 mM | 0.1982 mL | 0.9909 mL | 1.9818 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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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 ddH2O, 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
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 35 reference(s) in Google Scholar.)
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