TG100713

pan-PI3K inhibitor CAS# 925705-73-3

TG100713

Catalog No. BCC4985----Order now to get a substantial discount!

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Quality Control of TG100713

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Chemical structure

TG100713

3D structure

Chemical Properties of TG100713

Cas No. 925705-73-3 SDF Download SDF
PubChem ID 17751063 Appearance Powder
Formula C12H10N6 M.Wt 238.2
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 10 mM in DMSO
Chemical Name 3-(2,4-diaminopteridin-6-yl)phenol
SMILES C1=CC(=CC(=C1)O)C2=CN=C3C(=N2)C(=NC(=N3)N)N
Standard InChIKey UOORQSPLBHUQDQ-UHFFFAOYSA-N
Standard InChI InChI=1S/C12H10N6O/c13-10-9-11(18-12(14)17-10)15-5-8(16-9)6-2-1-3-7(19)4-6/h1-5,19H,(H4,13,14,15,17,18)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of TG100713

DescriptionInhibitor of PI3-kinase (IC50 values are 24, 50, 165 and 215 nM for PI3Kδ, γ, α and β isoforms respectively). Inhibits endothelial cell proliferation.

TG100713 Dilution Calculator

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TG100713 Molarity Calculator

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Preparing Stock Solutions of TG100713

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 4.1982 mL 20.9908 mL 41.9815 mL 83.9631 mL 104.9538 mL
5 mM 0.8396 mL 4.1982 mL 8.3963 mL 16.7926 mL 20.9908 mL
10 mM 0.4198 mL 2.0991 mL 4.1982 mL 8.3963 mL 10.4954 mL
50 mM 0.084 mL 0.4198 mL 0.8396 mL 1.6793 mL 2.0991 mL
100 mM 0.042 mL 0.2099 mL 0.4198 mL 0.8396 mL 1.0495 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on TG100713

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.

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References on TG100713

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.[Pubmed:17685602]

J Med Chem. 2007 Sep 6;50(18):4279-94.

In studies aimed toward identifying effective and safe inhibitors of kinase signaling cascades that underlie ischemia/reperfusion (I/R) injury, we synthesized a series of pteridines and pyridopyrazines. The design strategy was inspired by the examination of naturally occurring PI3K inhibitors such as wortmannin and quercetin, and building a pharmacophore-based model used for optimization. Structural modifications led to hybrid molecules which incorporated aminopyrimidine and aminopyridine moieties with ATP mimetic characteristics into the pharmacophore motifs to modulate kinase affinity and selectivity. Elaborations involving substitutions of the 2 and 4 positions of the pyrimidine or pyridine ring and the 6 and 7 positions of the central pyrazine ring resulted in in vivo activity profiles which identified potent inhibitors of vascular endothelial growth factor (VEGF) induced vascular leakage. Pathway analysis identified a diaminopteridine-diphenol as a potent and selective phosphatidylinositol-3-kinase (PI3K) inhibitor. The structure-activity relationship studies of various analogues of diaminopteridine-diphenol-based on biochemical assays resulted in potent inhibitors of PI3K.

Phosphoinositide 3-kinase gamma/delta inhibition limits infarct size after myocardial ischemia/reperfusion injury.[Pubmed:17172449]

Proc Natl Acad Sci U S A. 2006 Dec 26;103(52):19866-71.

Although phosphoinositide 3-kinases (PI3Ks) play beneficial pro-cell survival roles during tissue ischemia, some isoforms (gamma and delta) paradoxically contribute to the inflammation that damages these same tissues upon reperfusion. We therefore considered the possibility that selectively inhibiting proinflammatory PI3K isoforms during the reperfusion phase could ultimately limit overall tissue damage seen in ischemia/reperfusion injuries such as myocardial infarction. Panreactive and isoform-restricted PI3K inhibitors were identified by screening a novel chemical family; molecular modeling studies attributed isoform specificity based on rotational freedom of substituent groups. One compound (TG100-115) identified as a selective PI3K gamma/delta inhibitor potently inhibited edema and inflammation in response to multiple mediators known to participate in myocardial infarction, including vascular endothelial growth factor and platelet-activating factor; by contrast, endothelial cell mitogenesis, a repair process important to tissue survival after ischemic damage, was not disrupted. In rigorous animal MI models, TG100-115 provided potent cardioprotection, reducing infarct development and preserving myocardial function. Importantly, this was achieved when dosing well after myocardial reperfusion (up to 3 h after), the same time period when patients are most accessible for therapeutic intervention. In conclusion, by targeting pathologic events occurring relatively late in myocardial damage, we have identified a potential means of addressing an elusive clinical goal: meaningful cardioprotection in the postreperfusion time period.

Description

PI 3-kinase inhibitor,TG100713 is a pan-PI3K inhibitor against PI3Kγ, PI3Kδ, PI3Kα and PI3Kβ with IC50 of 50 nM, 24 nM, 165 nM and 215 nM, respectively.

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