Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Regorafenib Hydrochloride (BAY73-4506 hydrochloride) is a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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5 mg | 在庫あり | ¥ 7,000 | |||
10 mg | 在庫あり | ¥ 11,000 | |||
25 mg | 在庫あり | ¥ 17,000 | |||
50 mg | 在庫あり | ¥ 22,500 | |||
100 mg | 在庫あり | ¥ 34,000 | |||
500 mg | 在庫あり | ¥ 85,000 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 12,000 |
説明 | Regorafenib Hydrochloride (BAY73-4506 hydrochloride) is a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity |
ターゲット&IC50 | BRAF:28 nM, B-Raf (V600E):19 nM, PDGFRβ:22 nM, Raf-1:2.5 nM, VEGFR1:13 nM, VEGFR3:46 nM, VEGFR2:4.2 nM |
In vitro | Regorafenib inhibits additional angiogenic kinases (VEGFR1/3, platelet-derived growth factor receptor-β and fibroblast growth factor receptor 1) and the mutant oncogenic kinases KIT, RET and B-RAF. |
In vivo | Regorafenib administered once orally at 10 mg/kg significantly decreased the extravasation of Gadomer in the vasculature of rat GS9L glioblastoma tumor xenografts.?In a daily (qd)×4 dosing study, the pharmacodynamic effects persisted for 48 hr after the last dosing and correlated with tumor growth inhibition (TGI).?A significant reduction in tumor microvessel area was observed in a human colorectal xenograft after qd×5 dosing at 10 and 30 mg/kg.?Regorafenib exhibited potent dose-dependent TGI in various preclinical human xenograft models in mice, with tumor shrinkages observed in breast MDA-MB-231 and renal 786-O carcinoma models.?Pharmacodynamic analyses of the breast model revealed strong reduction in staining of proliferation marker Ki-67 and phosphorylated extracellular regulated kinases 1/2[1]. |
別名 | BAY73-4506 hydrochloride |
分子量 | 519.28 |
分子式 | C21H16Cl2F4N4O3 |
CAS No. | 835621-07-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 5.6 mg/mL (10.78 mM)
You can also refer to dose conversion for different animals. 詳細
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Regorafenib Hydrochloride 835621-07-3 Angiogenesis Apoptosis Autophagy MAPK Tyrosine Kinase/Adaptors PDGFR VEGFR Raf c-RET Raf kinases inhibit Inhibitor RET BAY73-4506 Hydrochloride Vascular endothelial growth factor receptor Regorafenib BAY 73-4506 BAY73-4506 hydrochloride Platelet-derived growth factor receptor inhibitor