TG100-115

Modify Date: 2024-01-06 18:33:11

TG100-115 Structure
TG100-115 structure
Common Name TG100-115
CAS Number 677297-51-7 Molecular Weight 346.343
Density 1.5±0.1 g/cm3 Boiling Point 699.6±65.0 °C at 760 mmHg
Molecular Formula C18H14N6O2 Melting Point N/A
MSDS N/A Flash Point 376.9±34.3 °C

 Use of TG100-115


TG100-115 is a selective PI3Kγ/PI3Kδ inhibitor with IC50s of 83 and 235 nM, respectively.

 Names

Name 3-[2,4-diamino-7-(3-hydroxyphenyl)pteridin-6-yl]phenol
Synonym More Synonyms

 TG100-115 Biological Activity

Description TG100-115 is a selective PI3Kγ/PI3Kδ inhibitor with IC50s of 83 and 235 nM, respectively.
Related Catalog
Target

PI3Kγ:83 nM (IC50)

PI3Kδ:235 nM (IC50)

In Vitro TG100-115 inhibits PI3Kγ and PI3Kδ with IC50s of 83 and 235 nM, respectively, whereas both PI3Kα and PI3Kβ are relatively unaffected (IC50 values >1 μM). As a gauge of general specificity, TG100-115 is also assayed against a 133 protein kinase panel, none of which are inhibited at IC50 values <1 μM. TG100-115 potently inhibits 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[1].
In Vivo To correlate these in vivo responses with the molecular target of interest, PI3K pathway signaling is monitored through western blot analyses of Akt phosphorylation (a PI3K-mediated event). VEGF injection i.v. in mice induces a rapid Akt phosphorylation readily detectable in lung lysates, pretreatment with TG100-115 blocks this response. Blockade is seen with TG100-115 doses as low as 0.5 mg/kg and persists over a period of several hours. In initial dose-ranging studies, generally equivalent responses are observed using TG100-115 doses of 0.5-10 mg/kg, and we therefore elected to conduct a statistically powered test at the lowest dose. Animals dosed with TG100-115 as a single 0.5 mg/kg i.v. bolus 30 min after reperfusion developed smaller infarcts vs. vehicle-treated controls. Measuring infarct area as percent of total LV ischemic area, infarct size is reduced by 35% (P=0.04). Viable tissue within the ischemic zone is increased by 37% (P=0.04), directly demonstrating the cardioprotective effect of PI3Kγ/δ inhibition[1].
Kinase 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. Protein kinase assays are performed by using commercial screening services[1].
Cell Assay Human umbilical vein EC plated in 96-well cluster plates (5,000 cells/well) are cultured in assay medium (containing 0.5% serum and 50 ng/mL VEGF) in the presence or absence of test compounds (e.g., TG100-115) (10 μM), and cell numbers are quantified by XTT assay 24, 48, or 72 h later[1].
Animal Admin Rats[1] Sprague-Dawley rats (175-200 g) are dosed i.v. with either TG100-115 (1 mg/kg) or vehicle, and 1-4 h later Evans blue dye is administered i.v. as 500 μl of a 2% sterile saline solution. Immediately after dye injection, animals are injected intradermally on each shaved flank with 100 μL of saline, VEGF (2 μg/mL stock), or histamine (10 μg/mL stock). Thirty minutes later, injection sites are photographed.
References

[1]. Doukas J, et al. 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.

 Chemical & Physical Properties

Density 1.5±0.1 g/cm3
Boiling Point 699.6±65.0 °C at 760 mmHg
Molecular Formula C18H14N6O2
Molecular Weight 346.343
Flash Point 376.9±34.3 °C
Exact Mass 346.117828
PSA 144.79000
LogP 0.99
Vapour Pressure 0.0±2.3 mmHg at 25°C
Index of Refraction 1.803
Storage condition -20℃

 Synthetic Route

~93%

TG100-115 Structure

TG100-115

CAS#:677297-51-7

Literature: TargeGen, Inc. Patent: US2005/282814 A1, 2005 ;

~91%

TG100-115 Structure

TG100-115

CAS#:677297-51-7

Literature: Palanki, Moorthy S. S.; Dneprovskaia, Elena; Doukas, John; Fine, Richard M.; Hood, John; Kang, Xinshan; Lohse, Dan; Martin, Michael; Noronha, Glenn; Soll, Richard M.; Wrasidlo, Wolfgang; Yee, Shiyin; Zhu, Hong Journal of Medicinal Chemistry, 2007 , vol. 50, # 18 p. 4279 - 4294

 Synonyms

3,3'-(2,4-diaminopteridine-6,7-diyl)diphenol
TG-100-115
Phenol, 3,3'-(2,4-diamino-6,7-pteridinediyl)bis-
3,3'-(2,4-Diamino-6,7-pteridinediyl)diphenol
3,3'-(2,4-DIAMINO-6,7-PTERIDINEDIYL)BISPHENOL
6,7-bis-(3-hydroxyphenyl)-pteridine-2,4-diamine
S1352_Selleck
3-[2,4-diamino-6-(3-hydroxyphenyl)pteridin-7-yl]phenol
TG100-115
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