Research Area
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TGX-221 Chemical Structure
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Biological Activity
TGX-221 is a potent, selective, and cell permeable inhibitor of PI3K p110β .[1,2] Thrombogenix compound TGX-221 is a LY294002 analogue, able to inhibit selectively the PI3Kβ isoform in vitro. The chromone core of LY294002 was replaced with pyrido[1,2-a] pyrimidin-4-one and inserted into an aryl ring moiety, increasing the potency and selectivity against PI3Kβ(IC50=10nM).[1]
TGX-221 is a low-nanomolar range inhibitor, shows about 1000-fold higher selectivity over PI3Kα, and is cell permeable. TGX-221 interfered with shear stress-induced PtdIns(3,4)P2 production and integrin αIIbβ3-mediated adhesion in platelets, suggesting that inhibition of PI3Kβ might have an anti-thrombotic potential in vivo.[1]
References on TGX-221
- [] Biochimica et Biophysica Acta 2008;1784 ：159–185
- [] NATURE MEDICINE MAY 2005 ;11：507－514
Chemical Information
| Molecular Weight (WM): | 364.44 |
|---|---|
| Formula: | C21H24N4O2 |
| CAS No.: | 663619-89-4 |
| Synonyms: |
N/A
|
| Dissolve in (25°C): | DMSO ≥17mg/mL |
| Water <1mg/mL | |
| Ethanol ≥4mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
Quality Control & MSDS
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We treated all of drugs in T47D which has a PI3KCA H1044R mutation with the concentration shown below for 1 hour and performed western blot analysis using antibodies to phospho-AKT(SERINE 472), and total AKT.
We treated all of drugs in T47D which has a PI3KCA H1044R mutation with the concentration shown below for 1 hour and performed western blot analysis using antibodies to phospho-AKT(SERINE 472), and total AKT.
Data independently produced by Saraswati Sukumar of Johns Hopkins University School of Medicine---TGX-221 purchased from Selleck TGX-221 purchased from Selleck
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Click to enlarge
Breast cancer cells were pretreated with 100ng/ml EGF for 15 min and then treated with the indicated concentrations of TGX-221 for 24 hours.
Breast cancer cells were pretreated with 100ng/ml EGF for 15 min and then treated with the indicated concentrations of TGX-221 for 24 hours.
Data independently produced by Dr. Zhang of Tianjin Medical University TGX-221 purchased from Selleck
Check our customer reviews
We treated all of drugs in T47D which has a PI3KCA H1044R mutation with the concentration shown below for 1 hour and performed western blot analysis using antibodies to phospho-AKT(SERINE 472), and total AKT.
|
Data independently produced by Saraswati Sukumar of Johns Hopkins University School of Medicine---TGX-221 purchased from Selleck
Breast cancer cells were pretreated with 100ng/ml EGF for 15 min and then treated with the indicated concentrations of TGX-221 for 24 hours.
|
Data independently produced by Dr. Zhang of Tianjin Medical University
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