1257628-77-5
1257628-77-5 structure
- Name: GZD824
- Chemical Name: 3-(2-(1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl)-4-methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide
- CAS Number: 1257628-77-5
- Molecular Formula: C29H27F3N6O
- Molecular Weight: 532.560
- Catalog: Biochemical Inhibitor Protein tyrosine kinase
- Create Date: 2016-08-18 21:54:39
- Modify Date: 2024-01-06 20:46:35
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GZD824 is a novel orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT) and Bcr-Abl(T315I) with IC50 of 0.34 nM and 0.68 nM, respectively. IC50 Value: 0.34/0.68 nM(Bce-Abl wt/T315I) [1]Target: Bcr-Abl in vitro: GZD824 potently suppressed proliferation of Bcr-Abl-positive K562 and Ku812 human CML cells with IC(50) values of 0.2 and 0.13 nM, respectively. It also displayed good oral bioavailability (48.7%), a reasonable half-life (10.6 h), and promising in vivo antitumor efficacy.in vivo: GZD824 induced tumor regression in mouse xenograft tumor models driven by Bcr-Abl(WT) or the mutants and significantly improved the survival of mice bearing an allograft leukemia model with Ba/F3 cells harboring Bcr-Abl(T315I) [1]. Clinical trial: GZD824 is on the way of unknown clinical status.
| Name | 3-(2-(1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl)-4-methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide |
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| Synonyms |
4-Methyl-N-{4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl}-3-(1H-pyrazolo[3,4-b]pyridin-5-ylethynyl)benzamide
Benzamide, 4-methyl-N-[4-[(4-methyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-3-[2-(1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl]- GZD824 |
| Description | GZD824 is a novel orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT) and Bcr-Abl(T315I) with IC50 of 0.34 nM and 0.68 nM, respectively. IC50 Value: 0.34/0.68 nM(Bce-Abl wt/T315I) [1]Target: Bcr-Abl in vitro: GZD824 potently suppressed proliferation of Bcr-Abl-positive K562 and Ku812 human CML cells with IC(50) values of 0.2 and 0.13 nM, respectively. It also displayed good oral bioavailability (48.7%), a reasonable half-life (10.6 h), and promising in vivo antitumor efficacy.in vivo: GZD824 induced tumor regression in mouse xenograft tumor models driven by Bcr-Abl(WT) or the mutants and significantly improved the survival of mice bearing an allograft leukemia model with Ba/F3 cells harboring Bcr-Abl(T315I) [1]. Clinical trial: GZD824 is on the way of unknown clinical status. |
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| Related Catalog | |
| References |
| Density | 1.4±0.1 g/cm3 |
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| Boiling Point | 630.4±55.0 °C at 760 mmHg |
| Molecular Formula | C29H27F3N6O |
| Molecular Weight | 532.560 |
| Flash Point | 335.0±31.5 °C |
| Exact Mass | 532.219849 |
| PSA | 77.15000 |
| LogP | 3.93 |
| Vapour Pressure | 0.0±1.8 mmHg at 25°C |
| Index of Refraction | 1.667 |
| Storage condition | -20°C |
| Precursor 1 | |
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| DownStream 0 | |