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Purity: ≥98%
TG100713 is a novel and potent pan-PI3K (phosphatidylinositol 3-kinase) inhibitor with potential anti-inflammatory activity. It inhibits PI3Kγ, PI3Kδ, PI3Kα and PI3Kβ with respective IC50 values of 50 nM, 24 nM, 165 nM, and 215 nM. Pro-inflammatory PI3K isoformsPI3Kγ and PI3Kδ are involved in the inflammation that results in damage to ischemia-damaged tissue after reperfusion. The pro-cell survival functions of phosphoinositide 3-kinases (PI3Ks) are beneficial during tissue iscg the reperfusion phase of hemorrhage. As a result, it's possible that targeting only pro-inflammatory PI3K isoforms with durinase will help to limit the overall tissue damage brought on by ischemia/reperfusion injuries like myocardial infarction.
| Targets |
PI3Kδ (IC50 = 24 nM); PI3Kγ (IC50 = 50 nM); PI3Kα (IC50 = 165 nM); PI3Kβ (IC50 = 215 nM)
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| ln Vitro |
TG100713 (10 μM; 48 or 72 h) strongly inhibits endothelial cell (EC) proliferation[1].
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| ln 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
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| Enzyme Assay |
PI3K reactions are constructed by using recombinant human kinases, 3 μM ATP, phosphatidylinositol substrate, and cofactors, and reaction progression measured by using a luminescent-based detection system to quantify ATP consumption. Commercial screening services are used to conduct protein kinase assays.
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| Cell Assay |
Human umbilical vein endothelial cells (HUVEC) are plated in 96-well cluster plates (5,000 cells/well), cultured in assay medium (containing 0.5% serum and 50 ng/ml VEGF), and their numbers are determined by the XTT assay in the presence or absence of test compounds (10 M).01110 lies an intermediate position (several conformations ≦10 but some >>50 kcal)
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| References |
| Molecular Formula |
C12H10N6O
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| Molecular Weight |
254.2474
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| Exact Mass |
254.09161
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| Elemental Analysis |
C, 56.69; H, 3.96; N, 33.05; O, 6.29
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| CAS # |
925705-73-3
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
C1=CC(=CC(=C1)O)C2=CN=C3C(=N2)C(=NC(=N3)N)N
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| InChi Key |
UOORQSPLBHUQDQ-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
3-(2,4-diaminopteridin-6-yl)phenol
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| Synonyms |
TG100713; TG-100713; TG 100713
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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 |
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| 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: ~2 mg/mL (~7.9 mM)
Water: <1 mg/mL Ethanol: <1 mg/mL |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.9331 mL | 19.6657 mL | 39.3314 mL | |
| 5 mM | 0.7866 mL | 3.9331 mL | 7.8663 mL | |
| 10 mM | 0.3933 mL | 1.9666 mL | 3.9331 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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