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$0.00 - Mostafa Khater, .et al. Gβγ translocation to the Golgi apparatus activates ARF1 to spatiotemporally regulate G protein-coupled receptor signaling to MAPK, J Biol Chem, 2021, Jan-Jun, 296:100805 PMID: 34022220
- Mostafa Khater, .et al. G protein βγ translocation to the Golgi apparatus activates MAPK via p110γ-p101 heterodimers, J Biol Chem, 2021, Jan 22;296:100325 PMID: 33493514
- Pridham KJ, .et al. PIK3CB/p110β is a selective survival factor for glioblastoma, Neuro Oncol, 2018, Mar 27;20(4):494-505 PMID: 29016844
Biological Activity
TGX-221 is a potent, selective, and cell permeable inhibitor of PI3K p110β.
Targets
| Target | Value |
|---|---|
| p110β | IC50: 5nM |
| p110δ | IC50: 0.1μM |
| p110α | IC50: 5μM |
| p110γ | IC50: >10μM |
| C2α | IC50: >10μM |
| PI4K | IC50: >10μM |
| Abl | IC50: >10μM |
| EGFR | IC50: >10μM |
| Fyn | IC50: >10μM |
| HER2 | IC50: >10μM |
| Insulin Receptor | IC50: >10μM |
| CaseinKinase2 | IC50: >10μM |
| CDK2/CyclinA | IC50: >10μM |
| ERK1 | IC50: >10μM |
| p38α | IC50: >10μM |
| p70S6K | IC50: >10μM |
| PKA | IC50: >10μM |
| PKC | IC50: >10μM |
| CaMK | IC50: >10μM |
| In vitro (25°C) | DMSO | 11 mg/mL (30.18 mM) | |
| Water | Insoluble | ||
| Ethanol | Insoluble | ||
| In vivo | 1% DMSO+30% polyethylene glycol+1% Tween 80 | 28 mg/mL | |
|
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
|||
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 27.44 mL | 137.21 mL | 274.42 mL |
| 0.5 mM | 5.49 mL | 27.44 mL | 54.88 mL |
| 1 mM | 2.74 mL | 13.72 mL | 27.44 mL |
| 5 mM | 0.55 mL | 2.74 mL | 5.49 mL |
*The above data is based on the productmolecular weight 364.4 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Catalog Num | A10923 |
|---|---|
| Actions | Inhibitor |
| CAS No. | 663619-89-4 |
| Formula | C21H24N4O2 |
| M. Wt | 364.4 |
| Purity | >98% |
| Synonyms | TGX221 |
| SMILES | CC1=CN2C(=O)C=C(N=C2C(=C1)C(C)NC3=CC=CC=C3)N4CCOCC4 |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
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