上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。
Regorafenib (BAY 73-4506) mesylate 是一种口服有效的多靶点受体酪氨酸激酶 (tyrosine kinase) 抑制剂，抑制 VEGFR1/2/3，PDGFRβ，Kit，RET 和 Raf-1 的 IC50 分别为 13/4.2/46，22，7，1.5 和 2.5 nM。Regorafenib mesylate 显示出非常强的抗肿瘤和抗血管生成活性。
| 生物活性 |
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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| IC50 & Target |
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Raf-1
2.5 ± 0.6 nM (IC50)
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VEGFR2
4.2 ± 1.6 nM (IC50)
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VEGFR1
13 ± 0.4 nM (IC50)
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BRafV600E
19 ± 6 nM (IC50)
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PDGFRβ
22 ± 3 nM (IC50)
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B-Raf
28 ± 10 nM (IC50)
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VEGFR3
46 ± 10 nM (IC50)
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体外研究
(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].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
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. |
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体内研究
(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].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
| 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. |
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| 分子量 |
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| Formula |
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| CAS 号 |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| 参考文献 |
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[1]. Wilhelm SM, et al. Regorafenib (BAY 73-4506): a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity. Int J Cancer, 2011, 129(1), 245-255.
[2]. Carr BI, et al. Fluoro-Bay 43-9006 (Regorafenib) effects on hepatoma cells: growth inhibition, quiescence, and recovery. J Cell Physiol, 2013, 228(2), 292-297.
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