Details
Stereochemistry | ACHIRAL |
Molecular Formula | C18H14N6O2 |
Molecular Weight | 346.3428 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
NC1=NC(N)=C2N=C(C3=CC=CC(O)=C3)C(=NC2=N1)C4=CC(O)=CC=C4
InChI
InChIKey=UJIAQDJKSXQLIT-UHFFFAOYSA-N
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)
Molecular Formula | C18H14N6O2 |
Molecular Weight | 346.3428 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
TG-100115 is a potent dual inhibitor of PI3K-gamma and PI3K-delta. TG-100115 has broad anti-inflammatory activities. TG-100115 provided potent cardioprotection, reducing infarct development and preserving myocardial function. In murine models of asthma and acute stages of chronic obstructive pulmonary disease, aerosolized TG100-115 demonstrated not only markedly inhibited anti-inflammatory activity but also, in the case of the asthma model, improved functional outcome for the test animals. TG-100115 can be used as a potent TRPM7 kinase inhibitor and a potent inhibitor of breast cancer cell migration.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL3130 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17172449 |
235.0 nM [IC50] | ||
Target ID: CHEMBL3267 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17172449 |
83.0 nM [IC50] | ||
Target ID: CHEMBL1250412 Sources: https://www.ncbi.nlm.nih.gov/pubmed/28161478 |
1.07 µM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Preventing | Unknown Approved UseUnknown |
|||
Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
PubMed
Title | Date | PubMed |
---|---|---|
Phosphoinositide 3-kinase gamma/delta inhibition limits infarct size after myocardial ischemia/reperfusion injury. | 2006 Dec 26 |
|
Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. | 2010 Nov 24 |
|
Comprehensive analysis of kinase inhibitor selectivity. | 2011 Oct 30 |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/17172449
Rat: 0.5 mg/kg
Route of Administration:
Intravenous
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/17172449
TG-100115 had no effects on endothelial cells proliferation even at relatively high concentrations (up to 10 uM). TG-100115 (10 uM) interrupts other VEGF signaling pathways, such as those that culminate in VE-cadherin phosphorylation.
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 09:12:53 GMT 2023
by
admin
on
Sat Dec 16 09:12:53 GMT 2023
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Record UNII |
7ACH1U1E2M
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Record Status |
Validated (UNII)
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Record Version |
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-
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10427712
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DTXSID20218009
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677297-51-7
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7ACH1U1E2M
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DB05552
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