GDC-0032
Modify Date: 2024-01-02 19:19:41
GDC-0032 structure
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Common Name | GDC-0032 | ||
|---|---|---|---|---|
| CAS Number | 1282512-48-4 | Molecular Weight | 460.531 | |
| Density | 1.4±0.1 g/cm3 | Boiling Point | 783.3±70.0 °C at 760 mmHg | |
| Molecular Formula | C24H28N8O2 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | 427.5±35.7 °C | |
Use of GDC-0032Taselisib (GDC-0032) is a potent β-sparing small molecule inhibitor of PI3K, with Ki values of 0.29 nM, 0.91 nM, 0.97 nM for PI3Kα, PI3Kβ and PI3Kγ, respectively. |
| Name | Taselisib |
|---|---|
| Synonym | More Synonyms |
| Description | Taselisib (GDC-0032) is a potent β-sparing small molecule inhibitor of PI3K, with Ki values of 0.29 nM, 0.91 nM, 0.97 nM for PI3Kα, PI3Kβ and PI3Kγ, respectively. |
|---|---|
| Related Catalog | |
| Target |
PI3Kα:0.29 nM (Ki) PI3Kβ:9.1 nM (Ki) PI3Kδ:0.12 nM (Ki) PI3Kγ:0.97 nM (Ki) |
| In Vitro | Taselisib (GDC-0032) (100 nM) inhibits AKT/mTOR signaling in PIK3CA mutant cell lines but not in cells with loss or mutation of PTEN; Taselisib (GDC-0032) enhances radiation-induced apoptosis and inhibits growth in head and neck cancer cell lines that are sensitive to its single-agent activiy[1]. Taselisib (GDC-0032) enhances the effects of MEK1/2 inhibition on both BRAFV600E/PTENNull human melanoma cells autochthonous mouse melanomas[2]. |
| In Vivo | Taselisib (GDC-0032) (5 mg/kg, p.o.) potently impairs PI3K signaling and enhances the efficacy of fractionated radiotherapy; Taselisib (GDC-0032) and radiation is more effective than either treatment alone in nude mice implanted with subcutaneous Cal-33 xenografts[1]. The vehicle-treated BRAFV600E/PTENNull melanoma-bearing mice experiencs initial tumor regression after treatment with Taselisib (GDC-0032) (22.5 mg/kg, p.o.)[2]. |
| Cell Assay | Cells are seeded in replicates of 6 in 96-well plates with 500 to 5,000 cells/well overnight and then treated with Taselisib (GDC-0032). After 4 days, the media are removed and the cells are fixed with 4% glutaraldehyde for 30 minutes. Fixed cells are stained with 0.1% crystal violet for 2 minutes, then washed, and dissolved in 10% acetic acid. |
| Animal Admin | Six-week-old Nu/Nu mice are injected bilaterally with 5×105 cells resuspended in 200 μL of culture media and Matrigel mixed in a 1:1 ratio. After tumors reache approximately 100 to 200 cm3, mice are randomized into treatment arms with 8 to 10 tumors per group. Taselisib (GDC-0032) (5 mg/kg) is dissolved in a vehicle containing 0.5% methylcellulose with 0.2% TWEEN-80 and is administered via daily oral gavage. |
| References |
| Density | 1.4±0.1 g/cm3 |
|---|---|
| Boiling Point | 783.3±70.0 °C at 760 mmHg |
| Molecular Formula | C24H28N8O2 |
| Molecular Weight | 460.531 |
| Flash Point | 427.5±35.7 °C |
| Exact Mass | 460.233521 |
| PSA | 119.66000 |
| LogP | 0.69 |
| Vapour Pressure | 0.0±2.7 mmHg at 25°C |
| Index of Refraction | 1.709 |
| Storage condition | -20℃ |
![2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)-1H-pyrazol-1-yl)-2-methylpropanoic acid structure](https://www.chemsrc.com/caspic/303/1282513-03-4.png)
![IMidazo[1,2-d][1,4]benzoxazepine, 9-bromo-5,6-dihydro-2-[3-Methyl-1-(1-Methylethyl)-1H-1,2,4-triazol-5-yl]- structure](https://www.chemsrc.com/caspic/205/1282514-63-9.png)
![ethyl 2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)-1H-pyrazol-1-yl)-2-methylpropanoate structure](https://www.chemsrc.com/caspic/157/1282514-64-0.png)
![9-bromo-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepine structure](https://www.chemsrc.com/caspic/351/1282516-67-9.png)
![9-bromo-2,3-diiodo-5,6-dihydrobenzo[f ]imidazo[1,2-d][1,4]oxazepine structure](https://www.chemsrc.com/caspic/303/1282516-68-0.png)
![9-bromo-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepine-2-carboxamide structure](https://www.chemsrc.com/caspic/427/1282516-65-7.png)
| 2-{4-[2-(1-Isopropyl-3-methyl-1H-1,2,4-triazol-5-yl)-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide |
| GDC-0032 |
| RG7604 |
| 1H-Pyrazole-1-acetamide, 4-[5,6-dihydro-2-[3-methyl-1-(1-methylethyl)-1H-1,2,4-triazol-5-yl]imidazo[1,2-d][1,4]benzoxazepin-9-yl]-α,α-dimethyl- |
| S7103,GDC0032,RG7604 |
| UNII-L08J2O299M |
| 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f ]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide |
| 2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)-1H-pyrazol-1-yl)-2-methylpropanamide |
| 2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)-1H-pyrazol-1-yl)-2-methylpropanoic acid |
| Taselisib |