TG100-115

Alias: TG100115; TG-100115; TG 100115; TG-100-115; TG100-115 ; TG 100-115
Cat No.:V0129 Purity: ≥98%
TG100-115 is a novel, potent and selective PI3Kγ/δ inhibitor with potential cardioprotecting effects.
TG100-115 Chemical Structure CAS No.: 677297-51-7
Product category: PI3K
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

TG100-115 is a novel, potent and selective PI3Kγ/δ inhibitor with potential cardioprotecting effects. With an IC50 of 83 nM and 235 nM, respectively, it barely affects PI3Kγ/δ and inhibits PI3Kα/β.

Biological Activity I Assay Protocols (From Reference)
Targets
PI3Kγ (IC50 = 83 nM); PI3Kδ (IC50 = 235 nM); PI3Kβ (IC50 = 1.2 μM)
ln Vitro
TG100-115 inhibits PI3Kγ and -δ, with IC50 of 83 and 235 nM, respectively. TG100-115 is not active for PI3Kα and -β, with IC50 of 1.2 and 1.3 mM. TG100-115 (up to 10 M) has no impact on VEGF-stimulated ERK phosphorylation or cell proliferation in human umbilical vein endothelial cells (HUVECs). The VEGF signaling pathways that result in VE-cadherin phosphorylation are among those that are disrupted by TG100-115 (10 M). [1] The VEGF-induced rise in the overall level of VE-cadherin in HUVECs is inhibited by TG100-115 (10 M). mTOR and p70S6 kinase, which are both downstream of PI3K, are both phosphorylated by VEGF and are inhibited by TG100-115. The phosphorylation of Akt induced by FGF is also inhibited by TG100-115 (125 nM to 10 M). [2]
ln Vivo
TG100-115 (1–5 mg/kg) lessens edema formation and inflammation in rats in Miles assay models. TG100-115 (0.5-5 mg/kg) offers powerful cardioprotection in rigorous rodent and porcine models of myocardial ischemia (MI), restricts the growth of infarcts, and maintains myocardial function. [1] The fact that TG100-115 (5 mg/kg) significantly reduces vascular permeability (VP) in mice in response to Sema3A or VEGF suggests that both substances may rely on PI3Kγ/δ for VP induction. [3] Aerosolized TG100-115 significantly lowers pulmonary eosinophilia in a mouse asthma model and inhibits interleukin-13 and mucin accumulation. [4]
Enzyme Assay
To achieve linear kinetics over 90 minutes, 40 mL of reaction buffer (20 mM Tris/4 mM MgCl2/10 mM NaCl, pH 7.4) containing 50 mM D-myo-phosphatidylinositol 4,5-bisphosphate substrate and the desired PI3K isoform is aliquoted to 96-well plates. Then, 2.5 mL of a DMSO stock containing TG100-115 is added, bringing the final concentration range of 100 mM to 1 nM. The Ultra 384 instrument is used to measure luminosity. Reactions are started by adding 10 mL of ATP to a final concentration of 3 mM. After 90 minutes, 50 mL of Kinase-Glo reagent is added to quantify residual ATP levels. Additionally, control reactions without either the substrate or TG100-115 are carried out.
Cell Assay
In assay medium containing 0.5% serum and 50 ng/ml VEGF, cells plated in 96-well cluster plates (5 103 cells/well) are cultured in the presence or absence of TG100-115. Cell numbers are then quantified by XTT assay 24–48–72 hours later.
Animal Protocol
Rat: TG100-115 (1 mg/kg) or vehicle is injected intravenously into Sprague-Dawley rats (175-200 g), and 1-4 hours later, 500 μl of a 2% sterile saline solution containing Evans blue dye is injected. Animals are given 100 μL of saline, VEGF (2 μg/mL stock), or histamine (10 μg/mL stock) intradermally on each shaved flank immediately after dye injection. Injection sites are photographed 30 minutes after administration.
References

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

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

[3]. Blood . 2008 Mar 1;111(5):2674-80.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C18H14N6O2
Molecular Weight
346.3428
Exact Mass
346.11782
Elemental Analysis
C, 62.42; H, 4.07; N, 24.27; O, 9.24
CAS #
677297-51-7
Appearance
Solid powder
SMILES
C1=CC(=CC(=C1)O)C2=NC3=C(N=C(N=C3N=C2C4=CC(=CC=C4)O)N)N
InChi Key
UJIAQDJKSXQLIT-UHFFFAOYSA-N
InChi Code
InChI=1S/C18H14N6O2/c19-16-15-17(24-18(20)23-16)22-14(10-4-2-6-12(26)8-10)13(21-15)9-3-1-5-11(25)7-9/h1-8,25-26H,(H4,19,20,22,23,24)
Chemical Name
3-[2,4-diamino-6-(3-hydroxyphenyl)pteridin-7-yl]phenol
Synonyms
TG100115; TG-100115; TG 100115; TG-100-115; TG100-115 ; TG 100-115
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~9 mg/mL (~26 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In Vivo)
5%DMSO+30%PEG 300+ddH2O: 0.4mg/mL (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.8873 mL 14.4367 mL 28.8734 mL
5 mM 0.5775 mL 2.8873 mL 5.7747 mL
10 mM 0.2887 mL 1.4437 mL 2.8873 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.

Calculator

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What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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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.

Clinical Trial Information
NCT Number Status Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00103350 Completed Drug: TG100-115 Myocardial Infarction TargeGen January 2005 Phase 1
Phase 2
Biological Data
  • TG100-115

  • TG100-115
  • TG100-115
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