Regorafenib mesylate
Based on 100 publication(s) in Google Scholar
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.
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- CAS 番号: 835621-08-4
- 分子式: C22H19ClF4N4O6S
- 分子量:578.92
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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MedChemExpress（MCE）の使用を引用している文献 Regorafenib mesylate
More- Cancer Cell. 2026 Mar 9;44(3):658-675.e12. [Abstract]
- Cell Res. 2020 Sep;30(9):779-793. [Abstract]
- Cancer Discov. 2021 Jul;11(7):1716-1735. [Abstract]
- Cancer Discov. 2019 Dec;9(12):1686-1695. [Abstract]
- J Extracell Vesicles. 2024 Jul;13(7):e12468. [Abstract]
- Autophagy. 2025 Jul;21(7):1523-1543. [Abstract]
- Autophagy. 2020 Jan;16(1):106-122. [Abstract]
- Exp Hematol Oncol. 2016 Jul 29:5:22. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Acta Pharm Sin B. 2026 Jun 18.
- Acta Pharm Sin B. 2026 Apr 24.
- J Exp Clin Cancer Res. 2024 Jul 11;43(1):192. [Abstract]
- J Exp Clin Cancer Res. 2018 Jan 22;37(1):11. [Abstract]
- Adv Sci (Weinh). 2026 Feb 3:e16660. [Abstract]
- Adv Sci (Weinh). 2024 Sep;11(34):e2402327. [Abstract]
- Adv Sci (Weinh). 2023 Aug;10(22):e2206798. [Abstract]
- Cell Rep Med. 2025 Apr 15;6(4):102053. [Abstract]
- Biomaterials. 2022 Oct:289:121800. [Abstract]
- Cell Death Dis. 2020 Nov 15;11(11):982. [Abstract]
- Cancer Lett. 2022 Jan 1:524:161-171. [Abstract]
- Mater Today Bio. 2026 Jul 27:40:103495.
- Adv Healthc Mater. 2023 Jul;12(19):e2203120. [Abstract]
- Acta Pharmacol Sin. 2021 Jan;42(1):108-114. [Abstract]
- NPJ Precis Oncol. 2025 May 27;9(1):156. [Abstract]
- J Transl Med. 2024 Dec 3;22(1):1095. [Abstract]
- J Transl Med. 2024 Aug 28;22(1):792. [Abstract]
- J Transl Med. 2024 May 30;22(1):517. [Abstract]
- Leukemia. 2021 Oct;35(10):2827-2839. [Abstract]
- Int J Biol Macromol. 2025 Sep 7;328(Pt 1):147514. [Abstract]
- Int J Mol Med. 2022 Apr;49(4):51. [Abstract]
- Int J Mol Med. 2020 Feb;45(2):461-474. [Abstract]
- Phytother Res. 2026 Apr 29. [Abstract]
- ACS Appl Mater Interfaces. 2026 Apr 1;18(12):17602-17615. [Abstract]
- Br J Cancer. 2017 Sep 26;117(7):974-983. [Abstract]
- Cell Rep. 2026 Sep 22;45(9):117895. [Abstract]
- Cell Rep. 2025 May 6;44(5):115681. [Abstract]
- J Med Chem. 2015 Apr 9;58(7):2958-2966. [Abstract]
- Biochem Pharmacol. 2025 Nov:241:117183. [Abstract]
- Cells. 2026 Feb 23;15(4):383. [Abstract]
- J Clin Transl Hepatol. 2025 Jan 28;13(1):15-24. [Abstract]
- Cancer Nanotechnol. 2023 May 9.
- Eur J Pharmacol. 2023 Oct 15:957:175986. [Abstract]
- Int J Mol Sci. 2023 Dec 18;24(24):17610. [Abstract]
- Int J Mol Sci. 2022 Sep 14;23(18):10677. [Abstract]
- Int J Mol Sci. 2018 Sep 25;19(10):2915. [Abstract]
- ACS Omega. 2025 Oct 29;10(44):52562-52575. [Abstract]
- ACS Omega. 2024 Jul 23;9(31):33574-33593. [Abstract]
- Neoplasia. 2023 May:39:100897. [Abstract]
- J Cell Mol Med. 2026 Apr;30(7):e71101. [Abstract]
- Oncol Rep. 2018 Aug;40(2):635-646. [Abstract]
- iScience. 2026 May 20;29(6):116005. [Abstract]
- Bioengineering (Basel). 2025 Oct 19;12(10):1121. [Abstract]
- BMC Cancer. 2024 Dec 20;24(1):1562. [Abstract]
- Ther Adv Med Oncol. 2019 May 17:11:1758835919849757. [Abstract]
- J Biotechnol. 2025 Nov 12:410:1-9. [Abstract]
- Oral Oncol. 2025 Mar:162:107222. [Abstract]
- J Pharm Sci. 2023 Sep;112(9):2581-2590. [Abstract]
- Viruses. 2019 Apr 25;11(4):385. [Abstract]
- Toxicol Appl Pharmacol. 2024 Sep:490:117042. [Abstract]
- Mol Carcinog. 2025 Jul 24. [Abstract]
- Exp Cell Res. 2024 Mar 1;436(1):113956. [Abstract]
- Exp Cell Res. 2020 Aug 1;393(1):112054. [Abstract]
- Phytochemistry. 2022 Sep:201:113292. [Abstract]
- PLoS One. 2024 Nov 1;19(11):e0308647. [Abstract]
- PLoS One. 2024 Oct 16;19(10):e0312173. [Abstract]
- Photodiagnosis Photodyn Ther. 2024 Oct:49:104319. [Abstract]
- Fundam Clin Pharmacol. 2021 Oct;35(5):919-929. [Abstract]
- Cancer Manag Res. 2026 Apr 16:18:562346. [Abstract]
- Hereditas. 2025 Jul 31;162(1):148. [Abstract]
- Biochem Biophys Res Commun. 2025 Dec 15:792:152981. [Abstract]
- Biochem Biophys Res Commun. 2024 May 21:709:149812. [Abstract]
- J Chromatogr B Analyt Technol Biomed Life Sci. 2024 Apr 15:1237:124100. [Abstract]
- J Chromatogr B Analyt Technol Biomed Life Sci. 2017 Sep 1:1061-1062:220-224. [Abstract]
- Cell Physiol Biochem. 2016;38(1):160-72. [Abstract]
- Eur J Drug Metab Pharmacokinet. 2021 Sep;46(5):625-635. [Abstract]
- Anticancer Drugs. 2025 Oct 16. [Abstract]
- Biol Pharm Bull. 2015;38(4):582-6. [Abstract]
- Xenobiotica. 2018 Oct;48(10):1059-1071. [Abstract]
- bioRxiv. 2026 Aug 11.
- Preprints. 2026 Aug 20.
- bioRxiv. 2026 Jul 8.
- The Medical College of Wisconsin. 2026.
- bioRxiv. 2026 Apr 15.
- chemRxiv. 2026 Apr 6.
- bioRxiv. 2025 Dec 5.
- bioRxiv. 2025 Nov 20:2025.11.20.689490. [Abstract]
- University of Otago. 2025 Oct 7.
- Hong Kong Polytechnic University. 2025.
- bioRxiv. 2025 Jul 12:2025.07.08.663754. [Abstract]
- Hong Kong Polytechnic University. 2025.
- Patent. US20230101335A1.
- bioRxiv. 2024 Aug 6:2024.03.21.586169. [Abstract]
- bioRxiv. 2024 June 12.
- Research Square Preprint. 2024 Feb 8.
- Cancer Diagn Progn. 2023 Nov 3;3(6):655-659. [Abstract]
- Biomed Pharmacother. 2022 Sep:153:113540. [Abstract]
- Patent. US20210379032A1.
- University of Sao Paulo school. 2018 Oct.
- Technical University of Munich. 24.01.2018.
- Am J Dig Dis (Madison). 2015;2(2):95-99.
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VEGFR アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
IC50 & Target
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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) |
体外実験
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:GIST 882, Thyroid TT, MDA-MB-231, HepG2, A375 and SW620 cells
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Concentration:10 μM and 5 nM
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Incubation Time:96 h
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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.
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Cell Line:NIH-3T3/VEGFR2 cells, (CHO)-TIE2 cells, HAoSMCs cells, MCF-7 cells
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Concentration:0, 10, 30, 100, 300, 1000, 3000 nM
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Incubation Time:30 min
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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.
体内実験
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rat GS9L glioblastoma xenograft[1]
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Dosage:10 mg/kg
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Administration:Orally, single dose or daily for 4 days
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Result:Inhibited tumor vasculature and tumor growth in a rat GS9L glioblastoma model.
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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]
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Dosage:0, 3, 10, 30, 100 mg/kg
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Administration:Orally, qd × 9
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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.
化学情報
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CAS 番号 835621-08-4
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分子量 578.92
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分子式 C22H19ClF4N4O6S
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SMILES
O=C(NC1=CC=C(C(C(F)(F)F)=C1)Cl)NC2=CC=C(OC3=CC(C(NC)=O)=NC=C3)C=C2F.CS(O)(=O)=O
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別名
BAY 73-4506 mesylate
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (100)
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Journal Impact Factor
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Most Recent
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Cancer Cell
Chemotherapy triggers immune evasion by fostering LEPR+ Kupffer cell differentiation in liver metastases. [Abstract]2026 Mar 9;44(3):658-675.e12. PMID: 41687606 -
Cell Res
s-HBEGF/SIRT1 circuit-dictated crosstalk between vascular endothelial cells and keratinocytes mediates sorafenib-induced hand-foot skin reaction that can be reversed by nicotinamide. [Abstract]2020 Sep;30(9):779-793. PMID: 32296111 -
Cancer Discov
Exploiting Allosteric Properties of RAF and MEK Inhibitors to Target Therapy-Resistant Tumors Driven by Oncogenic BRAF Signaling. [Abstract]2021 Jul;11(7):1716-1735. PMID: 33568355 -
Cancer Discov
Acquired On-Target Clinical Resistance Validates FGFR4 as a Driver of Hepatocellular Carcinoma. [Abstract]2019 Dec;9(12):1686-1695. PMID: 31575540 -
J Extracell Vesicles
Oxidative stress induces extracellular vesicle release by upregulation of HEXB to facilitate tumour growth in experimental hepatocellular carcinoma. [Abstract]2024 Jul;13(7):e12468. PMID: 38944674 -
Autophagy
Kit-mediated autophagy suppression driven by a viral oncoprotein emerges as a crucial survival mechanism in Merkel cell carcinoma. [Abstract]2025 Jul;21(7):1523-1543. PMID: 40108758 -
Autophagy
2020 Jan;16(1):106-122. PMID: 30909789 -
Exp Hematol Oncol
Effects of molecularly targeted therapies on murine thymus: highly selective mTOR inhibitors induce reversible thymic involution. [Abstract]2016 Jul 29:5:22. PMID: 27478685 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
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J Exp Clin Cancer Res
Combination of dual JAK/HDAC inhibitor with regorafenib synergistically reduces tumor growth, metastasis, and regorafenib-induced toxicity in colorectal cancer. [Abstract]2024 Jul 11;43(1):192. PMID: 38992681 -
J Exp Clin Cancer Res
Anti-tumor effects of ONC201 in combination with VEGF-inhibitors significantly impacts colorectal cancer growth and survival in vivo through complementary non-overlapping mechanisms. [Abstract]2018 Jan 22;37(1):11. PMID: 29357916 -
Adv Sci (Weinh)
2026 Feb 3:e16660. PMID: 41632021 -
Adv Sci (Weinh)
Stabilization of TGF-β Receptor 1 by a Receptor-Associated Adaptor Dictates Feedback Activation of the TGF-β Signaling Pathway to Maintain Liver Cancer Stemness and Drug Resistance. [Abstract]2024 Sep;11(34):e2402327. PMID: 38981014 -
Adv Sci (Weinh)
Donafenib and GSK-J4 Synergistically Induce Ferroptosis in Liver Cancer by Upregulating HMOX1 Expression. [Abstract]2023 Aug;10(22):e2206798. PMID: 37330650 -
Cell Rep Med
CAN-Scan: A multi-omic phenotype-driven precision oncology platform identifies prognostic biomarkers of therapy response for colorectal cancer. [Abstract]2025 Apr 15;6(4):102053. PMID: 40187357 -
Biomaterials
2022 Oct:289:121800. PMID: 36166893 -
Cell Death Dis
A small natural molecule CADPE kills residual colorectal cancer cells by inhibiting key transcription factors and translation initiation factors. [Abstract]2020 Nov 15;11(11):982. PMID: 33191401 -
Cancer Lett
Induction of IL-6Rα by ATF3 enhances IL-6 mediated sorafenib and regorafenib resistance in hepatocellular carcinoma. [Abstract]2022 Jan 1:524:161-171. PMID: 34687791 -
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Adv Healthc Mater
A Novel Patient-Personalized Nanovector Based on Homotypic Recognition and Magnetic Hyperthermia for an Efficient Treatment of Glioblastoma Multiforme. [Abstract]2023 Jul;12(19):e2203120. PMID: 37058273 -
Acta Pharmacol Sin
Osimertinib successfully combats EGFR-negative glioblastoma cells by inhibiting the MAPK pathway. [Abstract]2021 Jan;42(1):108-114. PMID: 32398685 -
NPJ Precis Oncol
Optimized culturing yields high success rates and preserves molecular heterogeneity, enabling personalized screening for high-grade gliomas. [Abstract]2025 May 27;9(1):156. PMID: 40425813 -
J Transl Med
Doxorubicin synergizes bortezomib-induced multiple myeloma cell death by inhibiting aggresome formation and augmenting endoplasmic reticulum/Golgi stress and apoptosis. [Abstract]2024 Dec 3;22(1):1095. PMID: 39623468 -
J Transl Med
Mito-LND and (E)-Akt inhibitor-IV: novel compounds inducing endoplasmic reticulum stress and ROS accumulation against hepatocellular carcinoma. [Abstract]2024 Aug 28;22(1):792. PMID: 39198815 -
J Transl Med
CircDCAF8 promotes the progression of hepatocellular carcinoma through miR-217/NAP1L1 Axis, and induces angiogenesis and regorafenib resistance via exosome-mediated transfer. [Abstract]2024 May 30;22(1):517. PMID: 38816735 -
Leukemia
Downregulation of MTSS1 in acute myeloid leukemia is associated with a poor prognosis, chemotherapy resistance, and disease aggressiveness. [Abstract]2021 Oct;35(10):2827-2839. PMID: 33782537 -
Int J Biol Macromol
vtRNA1-1 drives regorafenib resistance by sustaining cancer stemness via impaired autophagy and altered svRNA biogenesis. [Abstract]2025 Sep 7;328(Pt 1):147514. PMID: 40925433 -
Int J Mol Med
A pre‑clinical model combining cryopreservation technique with precision‑cut slice culture method to assess the in vitro drug response of hepatocellular carcinoma. [Abstract]2022 Apr;49(4):51. PMID: 35179217 -
Int J Mol Med
MicroRNA‑15a‑5p induces pulmonary artery smooth muscle cell apoptosis in a pulmonary arterial hypertension model via the VEGF/p38/MMP‑2 signaling pathway. [Abstract]2020 Feb;45(2):461-474. PMID: 31894295 -
Phytother Res
Flavokawain A Targets CXCR4-Mediated Vasculogenic Mimicry to Reverse Hepatocellular Carcinoma Resistance to Tyrosine Kinase Inhibitors. [Abstract]2026 Apr 29. PMID: 42052746 -
ACS Appl Mater Interfaces
Chlorin e6 and Regorafenib Assemblies to Boost Photodynamic Immunotherapy through PD-L1 Downregulation and Tumor-Associated Macrophage Reprogramming. [Abstract]2026 Apr 1;18(12):17602-17615. PMID: 41855525 -
Br J Cancer
Activation of an AKT/FOXM1/STMN1 pathway drives resistance to tyrosine kinase inhibitors in lung cancer. [Abstract]2017 Sep 26;117(7):974-983. PMID: 28850563
Regorafenib mesylate purchased from MedChemExpress. Usage Cited in: Br J Cancer. 2017 Sep 26;117(7):974-983. [Abstract]
The effect of the AKT inhibitor MK2206 (10 μM) on the expression levels of phosphor-AKT, AKT, and STMN1 in TKI-pretreated NCI-H460 cells. β-actin is used as a loading control.
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Cell Rep
Hepatocellular carcinoma organoids enable drug discovery and combination therapy across heterogeneous tumors. [Abstract]2026 Sep 22;45(9):117895. PMID: 42636109 -
Cell Rep
OTUD4 inhibits ferroptosis by stabilizing GPX4 and suppressing autophagic degradation to promote tumor progression. [Abstract]2025 May 6;44(5):115681. PMID: 40338740 -
J Med Chem
Ensemble-based virtual screening for cannabinoid-like potentiators of the human glycine receptor α1 for the treatment of pain. [Abstract]2015 Apr 9;58(7):2958-2966. PMID: 25790278 -
Biochem Pharmacol
Pitavastatin overcomes multi-drug resistance in CRC and NSCLC by targeting the NRP1-ZFX axis. [Abstract]2025 Nov:241:117183. PMID: 40684995 -
Cells
A Comprehensive Adenoid Cystic Carcinoma-Derived Organoid Platform for Disease Modeling and Drug Screening Captures Interpatient Heterogeneity. [Abstract]2026 Feb 23;15(4):383. PMID: 41744826 -
J Clin Transl Hepatol
HBx Facilitates Drug Resistance in Hepatocellular Carcinoma via CD133-regulated Self-renewal of Liver Cancer Stem Cells. [Abstract]2025 Jan 28;13(1):15-24. PMID: 39801781 -
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Eur J Pharmacol
Regorafenib activates oxidative stress by inhibiting SELENOS and potentiates oxaliplatin-induced cell death in colon cancer cells. [Abstract]2023 Oct 15:957:175986. PMID: 37598924 -
Int J Mol Sci
Therapeutic Potential of Regorafenib in Cisplatin-Resistant Bladder Cancer with High Epithelial-Mesenchymal Transition and Stemness Properties. [Abstract]2023 Dec 18;24(24):17610. PMID: 38139437 -
Int J Mol Sci
Chidamide plus Tyrosine Kinase Inhibitor Remodel the Tumor Immune Microenvironment and Reduce Tumor Progression When Combined with Immune Checkpoint Inhibitor in Naïve and Anti-PD-1 Resistant CT26-Bearing Mice. [Abstract]2022 Sep 14;23(18):10677. PMID: 36142591 -
Int J Mol Sci
Effective Sequential Combined Chemotherapy with Trifluridine/Tipiracil and Regorafenib in Human Colorectal Cancer Cells. [Abstract]2018 Sep 25;19(10):2915. PMID: 30257515
Regorafenib mesylate purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2018 Sep 25;19(10):2915. [Abstract]
Effects on the expression of phosphorylated extracellular signal-related kinase (p-ERK), ERK, thymidylate synthase (TS), and markers of cell death in SW620, HCT 116, and HT-29 cells using various Regorafenib treatment schedules.
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ACS Omega
Association Study of OATP1B3 Polymorphisms on Hepatic Uptake and Drug-Drug Interaction In Vitro. [Abstract]2025 Oct 29;10(44):52562-52575. PMID: 41244417 -
ACS Omega
Regorafenib Attenuates Osteoclasts Differentiation by Inhibiting the NF-κB, NFAT, ERK, and p38 Signaling Pathways. [Abstract]2024 Jul 23;9(31):33574-33593. PMID: 39130575 -
Neoplasia
Regorafenib induces NOX5-mediated endoplasmic reticulum stress and potentiates the anti-tumor activity of cisplatin in non-small cell lung cancer cells. [Abstract]2023 May:39:100897. PMID: 36940556
Regorafenib mesylate purchased from MedChemExpress. Usage Cited in: Neoplasia. 2023 May:39:100897. [Abstract]
Regorafenib (0-40 µM; 36 h) markedly increases the expression of cleaved caspase-3, while decreases the expression of anti-apoptotic protein Bcl-2, in both H1299 and PC-9 cells.
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J Cell Mol Med
2026 Apr;30(7):e71101. PMID: 41896195 -
Oncol Rep
Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues. [Abstract]2018 Aug;40(2):635-646. PMID: 29917168 -
iScience
Phospho-JNK agonists show promising effects for the treatment of hepatocellular carcinoma. [Abstract]2026 May 20;29(6):116005. PMID: 42211113 -
Bioengineering (Basel)
Precision Oncology for High-Grade Gliomas: A Tumor Organoid Model for Adjuvant Treatment Selection. [Abstract]2025 Oct 19;12(10):1121. PMID: 41155119 -
BMC Cancer
Regorafenib induces DNA damage and enhances PARP inhibitor efficacy in pancreatic ductal carcinoma. [Abstract]2024 Dec 20;24(1):1562. PMID: 39707244 -
Ther Adv Med Oncol
Axitinib overcomes multiple imatinib resistant cKIT mutations including the gatekeeper mutation T670I in gastrointestinal stromal tumors. [Abstract]2019 May 17:11:1758835919849757. PMID: 31205508 -
J Biotechnol
2025 Nov 12:410:1-9. PMID: 41238124 -
Oral Oncol
Application of patient derived xenograft model in personalized drug screening for chondrosarcoma of head and neck: A preclinical study. [Abstract]2025 Mar:162:107222. PMID: 39999643 -
J Pharm Sci
Monoacylglycerol lipase inhibitor JJKK048 ameliorates ABCG2 transporter-mediated regorafenib resistance induced by hypoxia in triple negative breast cancer cells. [Abstract]2023 Sep;112(9):2581-2590. PMID: 37220829 -
Viruses
Screening of an FDA-Approved Drug Library with a Two-Tier System Identifies an Entry Inhibitor of Severe Fever with Thrombocytopenia Syndrome Virus. [Abstract]2019 Apr 25;11(4):385. PMID: 31027241 -
Toxicol Appl Pharmacol
Liquidambaric acid inhibits the proliferation of hepatocellular carcinoma cells by targeting PPARα-RXRα to down-regulate fatty acid metabolism. [Abstract]2024 Sep:490:117042. PMID: 39067772 -
Mol Carcinog
2025 Jul 24. PMID: 40705959 -
Exp Cell Res
Inhibition of RhoGEF/RhoA alleviates regorafenib resistance and cancer stemness via Hippo signaling pathway in hepatocellular carcinoma. [Abstract]2024 Mar 1;436(1):113956. PMID: 38341081 -
Exp Cell Res
Network-based analysis with primary cells reveals drug response landscape of acute myeloid leukemia. [Abstract]2020 Aug 1;393(1):112054. PMID: 32376287 -
Phytochemistry
2022 Sep:201:113292. PMID: 35780923 -
PLoS One
A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]2024 Nov 1;19(11):e0308647. PMID: 39485774 -
PLoS One
The correlation between cellular O-GlcNAcylation and sensitivity to O-GlcNAc inhibitor in colorectal cancer cells. [Abstract]2024 Oct 16;19(10):e0312173. PMID: 39413067 -
Photodiagnosis Photodyn Ther
Regorafenib enhances the efficacy of photodynamic therapy in hepatocellular carcinoma through MAPK signaling pathway suppression. [Abstract]2024 Oct:49:104319. PMID: 39181490 -
Fundam Clin Pharmacol
2021 Oct;35(5):919-929. PMID: 33523504 -
Cancer Manag Res
Regorafenib-Induced Stress Response Alters the Bioenergetic Profile of Osteosarcoma Cells and Modulates Gene Expression Associated with Metabolic regulation-a Potential Mechanism of Osteosarcoma Treatment-Related Adaptation. [Abstract]2026 Apr 16:18:562346. PMID: 42016157 -
Hereditas
EPHX1 enhances drug resistance to regorafenib by activating the JAK/STAT signaling pathway in hepatocellular carcinoma cell lines. [Abstract]2025 Jul 31;162(1):148. PMID: 40745342 -
Biochem Biophys Res Commun
2025 Dec 15:792:152981. PMID: 41242297 -
Biochem Biophys Res Commun
Allosteric SHP2 inhibition enhances regorafenib's effectiveness in colorectal cancer treatment. [Abstract]2024 May 21:709:149812. PMID: 38564942 -
J Chromatogr B Analyt Technol Biomed Life Sci
Simultaneous determination of 11 oral targeted antineoplastic drugs and 2 active metabolites by LC-MS/MS in human plasma and its application to therapeutic drug monitoring in cancer patients. [Abstract]2024 Apr 15:1237:124100. PMID: 38547701 -
J Chromatogr B Analyt Technol Biomed Life Sci
Investigation of the effect of plasma albumin levels on regorafenib-induced hepatotoxicity using a validated liquid chromatography-tandem mass spectrometry method. [Abstract]2017 Sep 1:1061-1062:220-224. PMID: 28750235 -
Cell Physiol Biochem
2016;38(1):160-72. PMID: 26765545 -
Eur J Drug Metab Pharmacokinet
Differential Inhibition of Equilibrative Nucleoside Transporter 1 (ENT1) Activity by Tyrosine Kinase Inhibitors. [Abstract]2021 Sep;46(5):625-635. PMID: 34275128 -
Anticancer Drugs
A genome-wide screen identified ARHGAP35 as a regulator of regorafenib resistance in liver cancer. [Abstract]2025 Oct 16. PMID: 41176659 -
Biol Pharm Bull
Regorafenib is transported by the organic anion transporter 1B1 and the multidrug resistance protein 2. [Abstract]2015;38(4):582-6. PMID: 25739790 -
Xenobiotica
Substrate-dependent effects of molecular-targeted anticancer agents on activity of organic anion transporting polypeptide 1B1. [Abstract]2018 Oct;48(10):1059-1071. PMID: 29034773 -
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bioRxiv
Hidden-driver inference reveals synergistic brain-penetrant therapies for medulloblastoma. [Abstract]2025 Nov 20:2025.11.20.689490. PMID: 41332625 -
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bioRxiv
2025 Jul 12:2025.07.08.663754. PMID: 40672312 -
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bioRxiv
2024 Aug 6:2024.03.21.586169. PMID: 38586030 -
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Cancer Diagn Progn
Recombinant Methioninase Lowers the Effective Dose of Regorafenib Against Colon-Cancer Cells: A Strategy for Widespread Clinical Use of a Toxic Drug. [Abstract]2023 Nov 3;3(6):655-659. PMID: 37927805 -
Biomed Pharmacother
Advantage of clinical colchicine concentration to promote sorafenib or regorafenib anti-cancer effects on hepatocellular carcinoma. [Abstract]2022 Sep:153:113540. PMID: 36076618 -
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純度とドキュメンテーション
参考文献
[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. [Content Brief]
[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. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Regorafenib mesylate 関連分類
HY-10331B 関連分類
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