64924-67-0
Halofuginone hydrobromide
CAS: 64924-67-0
Molecular Formula: C16H17BrClN3O3.HBr
64924-67-0 - Names and Identifiers
64924-67-0 - Physico-chemical Properties
| Molecular Formula | C16H17BrClN3O3.HBr |
| Molar Mass | 495.59 |
| Melting Point | 247° (dec) |
| Solubility | Soluble to 100 mM in DMSO. |
| Appearance | White to white-like powder or crystal |
| Storage Condition | Store at -20°C |
| In vitro study | Halofuginone competitively inhibits prolyl-tRNA synthetase by occupying both the prolineand tRNA-binding pockets of prolyl-tRNA synthetase. The IC 50 s of Halofuginone (1, 10, 100, 1000, 10000 nM; 48 hours) are 114.6 and 58.9 nM in KYSE70 and A549 cells, respectively. The IC 50 s of Halofuginone (1, 10, 100, 1000 nM; 24 hours) for NRF2 protein are 22.3 and 37.2 nM in KYSE70 and A549 cells, respectively. The IC 50 of Halofuginone for global protein synthesis is 22.6 and 45.7 nM in KYSE70 and A549 cells, respectively. Cell Viability Assay Cell Line: KYSE70 cells from human oesophageal cancer harbouring a mutation in the NRF2 gene and A549 cells harbouring the KEAP1 gene mutation Concentration: 1, 10, 100, 1000, 10000 nM Incubation Time: 48 hours Result: The IC 50 s were 114.6 and 58.9 nM in KYSE70 and A549 cells, respectively. Western Blot Analysis Cell Line: KYSE70 cells from human oesophageal cancer harbouring a mutation in the NRF2 gene and A549 cells harbouring the KEAP1 gene mutation Concentration: 1, 10, 100, 1000 nM Incubation Time: 24 hours Result: The IC 50 s for NRF2 protein were 22.3 and 37.2 nM in KYSE70 and A549 cells, respectively. |
| In vivo study | Halofuginone (0.2, 0.5, 1 or 2.5 mg/kg; injected intraperitoneally every other day for 1 month) attenuates progression of OA in anterior cruciate ligament transection (ACLT) mice. Lower concentration (0.2 or 0.5 mg/kg) has minimal effects on subchondral bone and higher concentration (2.5 mg/kg) induces proteoglycan loss in articular cartilage. Halofuginone (0.25 mg/kg; intraperitoneally injected; every day; 16 days) decreases NRF2 protein levels in tumors. While the tumor volumes do not change substantially between treatments with the vehicle, Halofuginone (0.25 mg/kg, intraperitoneally injected, every day) or cisplatin alone. Combined treatment with Halofuginone and Cisplatin significantly suppresses the tumor volume compared to treatment with Halofuginone or cisplatin alone. Animal Model: 3-month-old male C57BL/6J (WT) mice Dosage: 0.2, 0.5, 1 or 2.5 mg/kg Administration: Injected intraperitoneally every other day for 1 month Result: Attenuated progression of OA in ACLT mice. Animal Model: Male nude mice (BALB/C nu/nu mice) (6-8-week) Dosage: 0.25 mg/kg Administration: Intraperitoneally injected; every day; 16 days Result: The combined treatment with Cisplatin significantly suppressed the tumor volume. NRF2 protein levels in tumors were indeed decreased. |
64924-67-0 - Risk and Safety
| Hazard Symbols | Xn - Harmful |
| Risk Codes | 22 - Harmful if swallowed |
| UN IDs | UN2811 - class 6.1 - PG 1 - EHS - Toxic solids, organic, n.o.s., HI: all |
| WGK Germany | 3 |
| RTECS | VA2397066 |
64924-67-0 - Reference Information
| biological activity | Halofuginone hydroxyapatite (RU-19110 hydroxyapatite) is a derivative of Febrifugine with low toxicity, it can be isolated from Dichroa febrifuga. Halofuginone is an ATP-competitive prolyl-tRNA synthetase (prolyl-tRNA synthetase) inhibitor with a Ki of 18.3 nM. Halo fuginone is a specific inhibitor of collagen type I (type-I collagen) synthesis and can alleviate osteoarthritis by inhibiting TGF-β activity. |
| Target | Ki: 18.3±0.5 nM (prolyl-tRNA synthetase) |
| in vitro study | Halofuginone competitive attacks prolyl-tRNA synthesis by occupying both the proline and tRNA-binding pockets of prolyl-tRNA synthesis. The IC 50 s of Halofuginone (1, 10, 100, 10000, 114.6 nM; 48 hours) are 58.9 and nM in KYSE70 and A549 cells, review. The IC 50 s of Halofuginone (1, 10, 100, 1000 nM; 24 hours) for NRF2 protein are 22.3 and 37.2 nM in KYSE70 and A549 cells, respectively. The IC 50 of Halofuginone for global protein synthesis is 22.6 and 45.7 nM in KYSE70 and A549 cells, respectively. Cell Viability Assay Cell Line: KYSE70 cells from human oesophageal cancer harbouring a mutation in the NRF2 gene and A549 cells harbouring the KEAP1 gene mutation Concentration: 1, 10, 100, 1000, 10000 nM Incubation Time: 48 hours Result: The IC 50 s were 114.6 and 58.9 nM in KYSE70 and A549 cells respectively. Western Blot Analysis Cell Line: KYSE70 cells from human oesophageal cancer harbouring a mutation in the NRF2 gene and A549 cells harbouring the KEAP1 gene mutation Concentration: 1, 10, 100, 1000 nM Incubation Time: 24 hours Result: The IC 50 s for NRF2 protein were 22.3 and 37.2 nM in KYSE70 and A549 cells, respectively. |
| Cell Line: | KYSE70 cells from human oesophageal cancer harbouring a mutation in the NRF2 gene and A549 cells harbouring the KEAP1 gene mutation KYSE70 cells from human oesophageal cancer harbouring a mutation in the NRF2 gene and A549 cells harbouring the KEAP1 gene mutation |
| Concentration: | 1, 10, 100, 1000, 10000 nM 1, 10, 100, 1000 nM |
| Incubation Time: | 48 hours 24 hours |
| Result: | The IC 50 s were 114.6 and 58.9 nM in KYSE70 and A549 cells, respectively. The IC 50 s for NRF2 protein were 22.3 and 37.2 nM in KYSE70 and A549 cells, respectively. Attenuated progression of OA in ACLT mice. The combined treatment with Cisplatin significantly suppressed the tumor volume. NRF2 protein levels in tumors were indeed decreased. |
| in vivo study | Halofuginone (0.2, 0.5, 1 or 2.5 ↑mg/kg; injected intrarepecified each other day for 1. Lower concentration (0.2 or 0.5 mg/kg) has minimal effects on fetus bone and higher concentration (2.5 mg/kg) induces proteoglycan loss in articular cartilage. Halofuginone (0.25 mg/kg; intraperitoneally injected; every day; 16 days) decreases NRF2 protein levels in tumors. While the tumor volumes do not change substantially between treatments with the vehicle, Halofuginone (0.25 mg/kg, intraperitoneally injected, every day) or cisplatin alone. Combined treatment with Halofuginone and Cisplatin significantly suppresses the tumor volume compared to treatment with Halofuginone or cisplatin alone. Animal Model: 3-month-old male C57BL/6J (WT) mice Dosage: 0.2, 0.5, 1 or 2.5 mg/kg Administration: Injected intraperitoneally every other day for 1 month Result: Attenuated progression of OA in ACLT mice. Animal Model: Male nude mice (BALB/C nu/nu mice) (6-8-week) Dosage: 0.25 mg/kg Administration: Intraperitoneally injected; every day; 16 days Result: The combined treatment with Cisplatin significantly suppressed the tumor volume. NRF2 protein levels in tumors were indeed decreased. |
| Animal Model: | 3-month-old male C57BL/6J (WT) mice Male nude mice (BALB/C nu/nu mice) (6-8-week) |
| Dosage: | 0.2, 0.5, 1 or 2.5 mg/kg 0.25 mg/kg |
| Administration: | Injected intraperitoneally every other day for 1 month Intraperitoneally injected; every day; 16 days |
Last Update：2024-04-10 22:29:15
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