10161-87-2
10161-87-2 structure
- Name: KRA-533
- Chemical Name: 4-[4-[(2-bromoacetyl)amino]butyl]benzoic acid
- CAS Number: 10161-87-2
- Molecular Formula: C13H16BrNO3
- Molecular Weight: 314.17500
- Catalog: Signaling Pathways GPCR/G Protein Ras
- Create Date: 2018-06-17 19:19:05
- Modify Date: 2024-01-09 12:14:05
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KRA-533 is a potent KRAS agonist. KRA-533 binds to the GTP/GDP binding pocket in the KRAS protein to prevent GTP cleavage, resulting in the accumulation of constitutively active GTP-bound KRAS that triggers both apoptotic and autophagic cell death pathways in cancer cells.
| Name | 4-[4-[(2-bromoacetyl)amino]butyl]benzoic acid |
|---|---|
| Synonyms | KRA-533 |
| Description | KRA-533 is a potent KRAS agonist. KRA-533 binds to the GTP/GDP binding pocket in the KRAS protein to prevent GTP cleavage, resulting in the accumulation of constitutively active GTP-bound KRAS that triggers both apoptotic and autophagic cell death pathways in cancer cells. |
|---|---|
| Related Catalog | |
| Target |
KRAS[1] |
| In Vitro | KRA-533 (10 μM; 48 hours; HCC827 cells) enhances KRAS activity to a greater extent[1]. KRA-533 (0~15 μM; 48 hours; H157 cells) enhances KRAS activity in a dose-dependent manner, which is associated increased levels of pERK, ratio of active caspase 3/procaspase 3 and PARP cleavage, leading to apoptotic cell death[1]. KRA-533 (10 μM; 10 days; H292 cells) mediates cell growth suppression than those without KRAS mutation. KRA-533 (5~15 μM) can directly bind to WT, G12C, G12D and G13D mutant KRAS proteins. KRA-533 activates WT KRAS to increase its activity in a dose-dependent manner. KRA-533 further enhances the activities of active KRAS mutants[1]. Western Blot Analysis[1] Cell Line: HCC827 cells Concentration: 10 μM Incubation Time: 48 hours Result: Enhanced KRAS activity to a greater extent. Apoptosis Analysis[1] Cell Line: H157 cells Concentration: 0~15 μM Incubation Time: 48 hours Result: Enhanced KRAS activity in a dose-dependent manner, which was associated increased levels of pERK, ratio of active caspase 3/procaspase 3 and PARP cleavage, leading to apoptotic cell death. |
| In Vivo | KRA-533 (0~30 mg/kg; 28 days) suppresses tumor growth in a dose-dependent manner in lung cancer mutant KRAS xenografts and induces apoptosis and autophagy in tumor tissues in a dose-dependent manner[1]. KRA-533 shows optimal therapeutic index between 7.5 mg/kg and 30 mg/kg doses[1]. Animal Model: Nu/Nu nude mice[1] Dosage: 0~30 mg/kg Administration: I.p. Result: Suppressed tumor growth in a dose-dependent manner in lung cancer mutant KRAS xenografts and induced apoptosis and autophagy in tumor tissues in a dose-dependent manner. |
| References |
| Density | 1.428g/cm3 |
|---|---|
| Boiling Point | 530.4ºC at 760 mmHg |
| Molecular Formula | C13H16BrNO3 |
| Molecular Weight | 314.17500 |
| Flash Point | 274.6ºC |
| Exact Mass | 313.03100 |
| PSA | 66.40000 |
| LogP | 2.60950 |
| Vapour Pressure | 4.43E-12mmHg at 25°C |
| Index of Refraction | 1.574 |
| Storage condition | 2-8°C |