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BioChemicals
TG100-115
tcsc0186
TG100-115
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AVAILABLE SIZES
5mg
10mg
50mg
$
137.00
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ORDERING INFORMATION
International
TAICLONE BIOTECH CORP.
order@taiclone.com
+886-2-2735-9682
+886-2-2735-9807
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Product Description
TG100-115 is a selective
PI3Kγ
/
PI3Kδ
inhibitor with
IC
50
s of 83 and 235 nM, respectively.
IC50 & Target: IC50: 83 nM (PI3Kγ), 235 nM (PI3Kδ)
[1]
In Vitro:
TG100-115 inhibits PI3Kγ and PI3Kδ with IC
50
s of 83 and 235 nM, respectively, whereas both PI3Kα and PI3Kβ are relatively unaffected (IC
50
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 IC
50
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]
.
Information
CAS No
677297-51-7
Formula
C
18
H
14
N
6
O
2
Clinical Information
clinicalinformation
Pathway
PI3K/Akt/mTOR
Target
PI3K
Specifications
Purity / Grade
>98%
Solubility
DMSO : 5.45 mg/mL (15.74 mM; Need ultrasonic and warming)
Smiles
smiles
Misc Information
Observed Molecular Weight
346.34
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