TG100-115
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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.


Price and Availability

Size
Price

5mg
USD 90
50mg
USD 350
500mg
USD 1650
5g
USD 4950
50g
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Size
Price

10mg
USD 150
100mg
USD 550
1g
USD 2450
10g
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100g
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Size
Price

25mg
USD 250
200mg
USD 950
2g
USD 3450
20g
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TG100-115; purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. Delivery time: overnight (USA/Canada); 3-5 days (worldwide). Shipping fee: from $30.00 (USA); from $45.00 (Canada); from $70.00 (international).


Chemical Structure

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Theoretical Analysis

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


Technical Data

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).

Harmonized System Code:
293490


Additional Information

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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References

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.