835621-08-4
835621-08-4 structure
- Name: Regorafenib
- Chemical Name: 4-{4-[3-(4-chloro-3-trifluoromethylphenyl)-ureido]-3-fluorophenoxy}-pyridine-2-carboxylic acid methylamide mesylate
- CAS Number: 835621-08-4
- Molecular Formula: C22H19ClF4N4O6S
- Molecular Weight: 578.92100
- Catalog: Signaling Pathways Autophagy Autophagy
- Create Date: 2017-03-15 06:09:50
- Modify Date: 2024-01-14 20:37:15
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Regorafenib (BAY 73-4506) mesylate is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib mesylate shows very robust antitumor and antiangiogenic activity[1].
| Name | 4-{4-[3-(4-chloro-3-trifluoromethylphenyl)-ureido]-3-fluorophenoxy}-pyridine-2-carboxylic acid methylamide mesylate |
|---|---|
| Synonyms |
4(4-[3-(4-chloro-3-trifluoromethylphenyl)-ureido]-3-fluorophenoxy)-pyridine-2-carboxylic acid methylamide mesylate
Regorafenib |
| Description | Regorafenib (BAY 73-4506) mesylate is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib mesylate shows very robust antitumor and antiangiogenic activity[1]. |
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| Related Catalog | |
| Target |
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) |
| In Vitro | Regorafenib mesylate (0-10 μM, 96 h) shows anti-proliferation activity in GIST 882, Thyroid TT, MDA-MB-231, HepG2, A375 and SW620 cells[1]. Regorafenib mesylate (0-3000 nM, 30 min) inhibits the autophosphorylation of VEGFR2, TIE2 and PDGFR-β, and inhibits FGFR and pERK1/2[1]. Regorafenib mesylate causes a concentration-dependent decrease in Hep3B cell growth, with an IC50 of 5 μM. Regorafenib subsequently increases the levels of phospho-c-Jun, a JNK target, but not total c-Jun in Hep3B cells[2]. Cell Proliferation Assay[1] Cell Line: GIST 882, Thyroid TT, MDA-MB-231, HepG2, A375 and SW620 cells Concentration: 10 μM and 5 nM Incubation Time: 96 h Result: Showed anti-proliferation activity in GIST 882, Thyroid TT, MDA-MB-231, HepG2, A375 and SW620 cells, with IC50 values of 45 ± 20, 34 ± 8, 401 ± 88, 560 ± 200, 900, 967 ± 287 nM. respectively. Western Blot Analysis[1] Cell Line: NIH-3T3/VEGFR2 cells, (CHO)-TIE2 cells, HAoSMCs cells, MCF-7 cells Concentration: 0, 10, 30, 100, 300, 1000, 3000 nM Incubation Time: 30 min Result: Inhibited the autophosphorylation of VEGFR2, TIE2 and PDGFR-β, with IC50 values of 3, 31, and 90 nM, respectively, inhibited FGFR signaling in MCF-7 breast cancer (BC) cells stimulated with FGF10, and showed inhibition of phosphorylated FGFR substrate 2 (pFRS2) and the downstream signaling kinase pERK1/2. |
| 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. |
| References |
| Molecular Formula | C22H19ClF4N4O6S |
|---|---|
| Molecular Weight | 578.92100 |
| Exact Mass | 578.06500 |
| PSA | 155.10000 |
| LogP | 6.81050 |