| Hazard Information | Back Directory | [Uses]
BAY 73-4506 (Regorafenib) is a multikinase inhibitor with IC50 of 17, 40 and 69 nM c-KIT, VEGFR2, B-Raf. | [Definition]
ChEBI:Regorafenib is a pyridinecarboxamide obtained by condensation of 4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]pyridine-2-carboxylic acid with methylamine. Used for for the treatment of metastatic colorectal cancer in patients who have previously received chemotherapy, anti-EGFR or anti-VEGF therapy. It has a role as an antineoplastic agent, a tyrosine kinase inhibitor and a hepatotoxic agent. It is an aromatic ether, a pyridinecarboxamide, a member of monochlorobenzenes, a member of (trifluoromethyl)benzenes, a member of monofluorobenzenes and a member of phenylureas. | [in vivo]
Regorafenib mesylate (10 mg/kg, Orally, single dose or daily for 4 days) inhibits tumor vasculature and tumor growth in a rat GS9L glioblastoma model[1].
Regorafenib mesylate (0-100 mg/kg, Orally, qd × 9) exhibits antitumorigenic and antiangiogenic effects in the Colo-205, MDA-MB-231 and 786-O model[1]. | Animal Model: | Rat GS9L glioblastoma xenograft[1] | | Dosage: | 10 mg/kg | | Administration: | Orally, single dose or daily for 4 days | | Result: | Inhibited tumor vasculature and tumor growth in a rat GS9L glioblastoma model. |
| Animal Model: | Female athymic NCr nu/nu mice, Multiple xenograft models, including models derived from CRC (Colo-205), BC (MDA-MB-231) and RCC (786-O) tumors[1] | | Dosage: | 0, 3, 10, 30, 100 mg/kg | | Administration: | Orally, qd × 9 | | Result: | Effectively inhibited growth of the Colo-205, MDA-MB-231 and 786-O model. Significantly reduces tumor MVA, effectively inhibited the RAF/MEK/ERK signaling cascade, and drastically inhibited tumor cell proliferation. |
| [IC 50]
Tie2: 311 ± 46 nM (IC50); Raf-1: 2.5 ± 0.6 nM (IC50); VEGFR2: 4.2 ± 1.6 nM (IC50); VEGFR1: 13 ± 0.4 nM (IC50); BRafV600E: 19 ± 6 nM (IC50); PDGFRβ: 22 ± 3 nM (IC50); B-Raf: 28 ± 10 nM (IC50); VEGFR3: 46 ± 10 nM (IC50) |
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| Company Name: |
Creative Enzymes
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| Tel: |
1-516-855-7709 |
| Website: |
www.creative-enzymes.com |
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