4-[2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-[(3S)-3-piperidinylmethoxy]-1H-imidazo[4,5-c]pyridin-4-yl]-2-methyl-3-butyn-2-ol GSK 690693
GSK690693
CAS: 937174-76-0
Molecular Formula: C21H27N7O3
4-[2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-[(3S)-3-piperidinylmethoxy]-1H-imidazo[4,5-c]pyridin-4-yl]-2-methyl-3-butyn-2-ol GSK 690693 - Names and Identifiers
4-[2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-[(3S)-3-piperidinylmethoxy]-1H-imidazo[4,5-c]pyridin-4-yl]-2-methyl-3-butyn-2-ol GSK 690693 - Physico-chemical Properties
| Molecular Formula | C21H27N7O3 |
| Molar Mass | 425.48 |
| Density | 1.41 |
| Boling Point | 683.8±65.0 °C(Predicted) |
| Solubility | DMSO: soluble5mg/mL (clear solution) |
| Appearance | powder |
| Color | white to beige |
| pKa | 13.11±0.29(Predicted) |
| Storage Condition | 2-8°C |
| Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20° for up to 1 month. |
| MDL | MFCD14105605 |
| Use | GSK690693 |
| In vitro study | GSK690693 is highly selective for the Akt subtype relative to most kinases of other families. However, GSK690693 is less selective for members of the AGC kinase family, including PKA, PrkX, and PKC isozymes, with IC50 values of 24 nM, 5 nM, and 2-21 nM, respectively. GSK690693 is also very effective in inhibiting AMPK and DAPK3 of the CAMK family, with IC50 of 50 nM and 81 nM, respectively, and also very good in inhibiting PAK4, 5, and 6 of STE family, the IC50 values were 10 nM, 52 nM, and 6 nM, respectively. In tumor cells, GSK690693 inhibits the phosphorylation of GSK3β, IC50 ranged from 43 nM to 150 nM. Treatment with GSK690693 resulted in nuclear aggregation of the transcription factor FOXO3A in a dose-dependent manner. GSK690693 effectively inhibited the proliferation of T47D, ZR-75-1, BT474, HCC1954, MDA-MB-453, and LNCaP cells with IC50 of 72 nM, 79 nM, 86 nM, 119 nM, 975 nM, and 147 nM. In LNCaP and BT474 cells, greater than 100 nM GSK690693 induced apoptosis. As with the function of AKT during cell survival, GSK690693 can induce apoptosis in the sensitive ALL cell line. |
| In vivo study | In a human breast cancer (BT474) xenograft model, treatment with GSK690693 alone inhibited phosphorylation of GSK3β in a dose-and time-dependent manner. Similarly, GSK690693 caused a decrease in phosphorylation levels of the Akt substrate, PRAS40, and FKHR/FKHRL1. GSK690693 can also cause a sharp rise in blood glucose concentration, and the blood glucose concentration returns to the background level after 8 to 10 hours of drug treatment. In in vivo experiments, treatment with GSK690693 caused a decrease in phosphorylated Akt substrates, effectively inhibiting the growth of xenografts of human SKOV-3 ovarian cancer, LNCaP prostate cancer and BT474,HCC-1954 breast cancer, maximum inhibition of 58% to 75% was achieved at a drug concentration of 30 mg/kg/day. Regardless of the activation mechanism of Akt, GSK690693 showed good efficacy. In a Lck-MyrAkt2 mouse model in which membrane-bound Akt expressed in vivo remains activated, GSK690693 is the most effective drug to delay tumor progression. |
4-[2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-[(3S)-3-piperidinylmethoxy]-1H-imidazo[4,5-c]pyridin-4-yl]-2-methyl-3-butyn-2-ol GSK 690693 - Risk and Safety
| Hazard Symbols | T - Toxic |
| Risk Codes | 25 - Toxic if swallowed |
| Safety Description | 45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) |
| UN IDs | UN 2811 6.1 / PGIII |
| WGK Germany | 3 |
4-[2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-[(3S)-3-piperidinylmethoxy]-1H-imidazo[4,5-c]pyridin-4-yl]-2-methyl-3-butyn-2-ol GSK 690693 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.35 ml | 11.751 ml | 23.503 ml |
| 5 mM | 0.47 ml | 2.35 ml | 4.701 ml |
| 10 mM | 0.235 ml | 1.175 ml | 2.35 ml |
| 5 mM | 0.047 ml | 0.235 ml | 0.47 ml |
Last Update：2024-01-02 23:10:35
4-[2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-[(3S)-3-piperidinylmethoxy]-1H-imidazo[4,5-c]pyridin-4-yl]-2-methyl-3-butyn-2-ol GSK 690693 - Reference Information
| biological activity | GSK690693 is a pan-Akt inhibitor that targets Akt1/2/3. in cell-free tests, IC50 is 2 nM/13 nM/9 nM, and is also sensitive to AGC kinase family: PKA,PrkX and PKC isoenzymes. GSK690693 can also effectively inhibit AMPK and DAPK3 of CAMK family, with corresponding IC50 values of 50 nM and 81 nM respectively. GSK690693 can affect the activity of Unc-51-like autophagy activating kinase 1 (ULK1) and effectively inhibit the activation of STING-dependent IRF3. Phase 1. |
| target | TargetValue ULK1 () STING () AMPK () Akt1 (Cell-Free Assay) 2 nM PKCη (Cell-Free Assay) 2 nM |
| Target | Value |
| ULK1 () | |
| STING () | |
| AMPK () | |
| Akt1 (Cell-free assay) | 2 nM |
| PKCη (Cell-free assay) | 2 nM |
| in vitro study | compared with most kinases of other families, GSK690693 have a high degree of selectivity for Akt subtypes. However, GSK690693 has low selectivity for AGC kinase family members, including PKA, PrkX, and PKC isoenzymes, IC50 is 24 nM, 5 nM, and 2-21 nM respectively. GSK690693 can also effectively inhibit AMPK and DAPK3 of CAMK family, IC50 is 50 nM and 81 nM respectively, and can also well inhibit PAK4, 5, and 6 ,IC50 of STE family 10 nM, 52 nM respectively, and 6 nM. In tumor cells, GSK690693 inhibit the phosphorylation of GSK3β, the treatment of IC50 from 43 nM to 150 nM. GSK690693 will lead to the aggregation of transcription factor FOXO3A in the nucleus in a dose-dependent manner. GSK690693 effectively inhibit the proliferation of T47D, ZR-75-1, BT474, HCC1954, MDA-MB-453, and LNCaP cells with IC50 of 72 nM, 79 nM, 86 nM, 119 nM, 975 nM, respectively, and 147 nM. In LNCaP and BT474 cells, greater than 100 nM GSK690693 induce apoptosis. Like the function of AKT in cell survival, GSK690693 can induce apoptosis in sensitive ALL cell lines. |
| in vivo study | in human breast cancer (BT474) xenograft model, GSK690693 therapy alone will inhibit the phosphorylation of GSK3β, which has dose-and time-dependent properties. Similarly, GSK690693 caused a decrease in phosphorylation levels of Akt substrates, PRAS40, and FKHR/FKHRL1. GSK690693 can also lead to a sharp rise in blood glucose concentration. Blood glucose concentration returns to background level after 8 to 10 hours of drug treatment. In in vivo experiments, treatment with GSK690693 caused a decrease in phosphorylated Akt substrate, effectively inhibiting the growth of human SKOV-3 ovarian cancer, LNCaP prostate cancer, and xenografts of BT474,HCC-1954 breast cancer, with a maximum inhibition rate of 58% to 75% at a drug concentration of 30 mg/kg/day. Regardless of the activation mechanism of Akt, GSK690693 has shown good efficacy. In a Lck-MyrAkt2 mouse model, membrane-bound Akt expressed in vivo has been activated and GSK690693 is the most effective drug to delay tumor progression. |
Last Update：2024-04-09 22:09:11
![4-[2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-[(3S)-3-piperidinylmethoxy]-1H-imidazo[4,5-c]pyridin-4-yl]-2-methyl-3-butyn-2-ol GSK 690693](http://res.chembk.com/assets/images/structure/311979.gif)
Supplier List
Product Name: GSK690693 Visit Supplier Webpage Request for quotation
CAS: 937174-76-0
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 937174-76-0
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
Product Name: GSK690693 Visit Supplier Webpage Request for quotation
CAS: 937174-76-0
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 937174-76-0
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
View History
4-[2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-[(3S)-3-piperidinylmethoxy]-1H-imidazo[4,5-c]pyridin-4-yl]-2-methyl-3-butyn-2-ol GSK 690693
G-30028
G-30028