Wuhan Han Sheng New Material Technology Co.，Ltd(expird)
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CAS NO.64924-67-0
| 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. |
Wuhan Han Sheng New Material Technology Co. Ltd is a professional company which specialized in manufacturing and selling chemical raw materials, chemical products, pharmaceutical intermediates, veterinary medicine intermediates, dye intermediates, pigments, cosmetics raw materials and chemical reagents.
We have long term cooperation pharmaceutical raw material production plant and a reagent research and development center, with a rich professional background and strong competitive advantage. We have a professional and experienced team and we promise clients to provide the best quality, price and service. During the business cooperation with clients, we always adhere principle of Honesty, Trustworthiness and win-win policy. We guarantee 100% qualification of our products pass through the standard of USA, Mexico, UK, Australia, Canada, Brazil, France, Germany, Spain, Belgium, Sweden, the Netherlands and so on.
Our products are used for pharmaceuticals, pesticides, synthetic dyes, organic chemicals, inorganic chemicals, coatings, spices and essence, cosmetics and toilet products, soaps and synthetic detergents, surfactants, printing inks and their auxiliaries, adhesives, photosensitive materials, magnetic materials, catalysts, reagents, water treatment agents and polymer flocculants, papermaking auxiliaries, leather auxiliaries, synthetic materials auxiliaries, textile printing and dyeing agents and finishing agents, food additives Feed additives, animal drugs, etc.
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