WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 202892
CAS#: 677297-51-7
Description: TG100-115, inhibited PI3K γ and -δ(IC50 values of 83 and 235 nM, respectively), whereas both PI3Kα and -β were relatively unaffected (IC50 values>1 μM). As a gauge of general specificity, TG100-115 was also assayed against a 133 protein kinase panel, none of which was inhibited at IC50 values <1 μM.
MedKoo Cat#: 202892
Name: TG100-115
CAS#: 677297-51-7
Chemical Formula: C18H14N6O2
Exact Mass: 346.11782
Molecular Weight: 346.34276
Elemental Analysis: C, 62.42; H, 4.07; N, 24.27; O, 9.24
Synonym: TG100115; TG-100115; TG 100115; TG-100-115; TG100-115 ; TG 100-115.
IUPAC/Chemical Name: 3-[2,4-diamino-6-(3-hydroxyphenyl)pteridin-7-yl]phenol
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)
SMILES Code: OC1=CC=CC(C2=NC3=NC(N)=NC(N)=C3N=C2C4=CC=CC(O)=C4)=C1
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >5 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 346.34276 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
1: Doukas J, Eide L, Stebbins K, Racanelli-Layton A, Dellamary L, Martin M, Dneprovskaia E, Noronha G, Soll R, Wrasidlo W, Acevedo LM, Cheresh DA. Aerosolized phosphoinositide 3-kinase gamma/delta inhibitor TG100-115 [3-[2,4-diamino-6-(3-hydroxyphenyl)pteridin-7-yl]phenol] as a therapeutic candidate for asthma and chronic obstructive pulmonary disease. J Pharmacol Exp Ther. 2009 Mar;328(3):758-65. Epub 2008 Dec 4. PubMed PMID: 19056934.
2: Doukas J, Wrasidlo W, Noronha G, Dneprovskaia E, Hood J, Soll R. Isoform-selective PI3K inhibitors as novel therapeutics for the treatment of acute myocardial infarction. Biochem Soc Trans. 2007 Apr;35(Pt 2):204-6. PubMed PMID: 17371238.
3: 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. Epub 2006 Dec 15. PubMed PMID: 17172449; PubMed Central PMCID: PMC1702529.
TG100-115 [3-[2,4-diamino-6-(3-hydroxyphenyl)pteridin-7-yl]phenol], as a form of anti-inflammatory therapy for respiratory diseases such as asthma and chronic obstructive pulmonary disease (COPD). To determine pharmacokinetic profiles, aerosolized formulations of the drug were delivered to mice by a nose-only inhalation route, yielding high pulmonary TG100-115 levels with minimal systemic exposure. Safety assessments were favorable, with no clinical or histological changes noted after 21 days of daily dosing. In a murine asthma model, aerosolized TG100-115 markedly reduced the pulmonary eosinophilia and the concomitant interleukin-13 and mucin accumulation characteristic of this disease. As a functional benefit, interventional dosing schedules of this inhibitor also reduced airway hyper-responsiveness. To model the pulmonary neutrophilia characteristic of COPD, mice were exposed to either intranasal lipopolysaccharide or inhaled smoke. Aerosolized TG100-115 again inhibited these inflammatory patterns, most notably in the smoke model, where interventional therapy overcame the steroid-resistant nature of the pulmonary inflammation. In conclusion, aerosolized TG100-115 displays pharmacokinetic, safety, and biological activity profiles favorable for further development as a therapy for both asthma and COPD. Furthermore, these studies support the hypothesis that PI3K delta and gamma are suitable molecular targets for these diseases. (see: J Pharmacol Exp Ther. 2009 Mar;328(3):758-65. Epub 2008 Dec 4. http://www.ncbi.nlm.nih.gov/pubmed/19056934)
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