TG100713 |
カタログ番号GC16231
One-Click Copy Product Info
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TG100713 は PI3K の阻害剤であり、PI3Kδ、γ、α、β アイソフォームの IC50 はそれぞれ 24、50、165、215 nM です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 925705-73-3
Sample solution is provided at 25 µL, 10mM.
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IC50 (PI3Kγ, PI3Kδ, PI3Kα and PI3Kβ): 50 nM, 24 nM, 165 nM and 215 nM
TG100713 is a pan-PI3K inhibitor against PI3Kγ, PI3Kδ, PI3Kα and PI3Kβ.
PI3Kγ and PI3Kδ are a pair of pro-inflammatory PI3K isoforms that contribute to the inflammation that damages ischemia tissues upon reperfusion. Phosphoinositide 3-kinases (PI3Ks) are benefit to pro-cell survival roles during tissue iscg the reperfusion phhemia. Therefore, it is possible that selectively inhibiting pro-inflammatory PI3K isoforms durinase could ultimately control overall tissue damage caused by ischemia/reperfusion injuries such as myocardial infarction.
In vitro: Modeling studies suggested that the freedom of conformational rotation permitted by ring substituents controls isoform selectivity. Although substituent ring of TG100-115, TG100713, and TG101110 all require energy minima at 30–40°, angles diverge of each compound results in paying differing penalties from this range. TG100-115 displays the greatest barrier to rotation and finally is the most isoform selective, TG100713 has the most conformational flexibility (ring A being almost freely rotatable with maxima ≈5 kcal; 1 kcal = 4.18 kJ), suggesting the least selective, and TG101110 lies an intermediate position (several conformations ≦10 but some >>50 kcal) [1].
In vivo: The minimum structure which satisfies all three requirements is shown in TG100713, which so far has also displayed the best PI3K binding activity. Interestingly, the SAR profiles generating correlate quite well with the results of the initial in vivo screen further supports the involvement of PI3K as a target for inhibiting vascular permeability in related compounds [2].
Clinical trial: So far, no clinical study has been conducted.
References:
[1] Doukas J, Wrasidlo W, Noronha G, Dneprovskaia E, Fine R, Weis S, Hood J, Demaria A, Soll R, Cheresh D. Phosphoinositide 3-kinase gamma/delta inhibition limits infarct size after myocardial ischemia/reperfusion injury. Proc Natl Acad Sci U S A. 2006 Dec 26; 103(52):19866-71.
[2] Palanki MS, Dneprovskaia E, Doukas J, Fine RM, Hood J, Kang X, Lohse D, Martin M, Noronha G, Soll RM, Wrasidlo W, Yee S, Zhu H. Discovery of 3,3'-(2,4-diaminopteridine-6,7-diyl)diphenol as an isozyme-selective inhibitor of PI3K for the treatment of ischemia reperfusion injury associated with myocardial infarction. J Med Chem. 2007 Sep 6;50(18):4279-94. Epub 2007 Aug 9.
| Cas No. | 925705-73-3 | SDF | |
| Chemical Name | 3-(2,4-diaminopteridin-6-yl)phenol | ||
| Canonical SMILES | C1=CC(=CC(=C1)O)C2=CN=C3C(=N2)C(=NC(=N3)N)N | ||
| Formula | C12H10N6 | M.Wt | 254.25 |
| 溶解度 | DMSO: 10 mM | 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 | 3.9331 mL | 19.6657 mL | 39.3314 mL |
| 5 mM | 786.6 μL | 3.9331 mL | 7.8663 mL |
| 10 mM | 393.3 μL | 1.9666 mL | 3.9331 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 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: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 1 reference(s) in Google Scholar.)