Cat. No.: HY-10331

Regorafenib

(Synonyms: BAY 73-4506)

96 Cited Publications

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Based on 96 publication(s) in Google Scholar

Regorafenib (BAY 73-4506) 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 shows very robust antitumor and antiangiogenic activity.

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Pureté: 99.97%
CAS No.: 755037-03-7
Formule: C₂₁H₁₅ClF₄N₄O₃
Masse moléculaire:482.82

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Regorafenib Chemical Structure

CAS No.: 755037-03-7

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (96)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
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Activité biologique

Description

IC₅₀ & Target^[1]

Raf-1

2.5 nM (IC₅₀)

Tie2

311 ± 46 nM (IC₅₀)

VEGFR2

4.2 nM (IC₅₀)

VEGFR1

13 nM (IC₅₀)

BRaf^V600E

19 nM (IC₅₀)

PDGFRβ

22 nM (IC₅₀)

Braf

28 nM (IC₅₀)

VEGFR3

46 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform VEGFR :

Voir tous les produits spécifiques à Isoform PDGFR :

Voir tous les produits spécifiques à Isoform Raf :

Voir tous les produits spécifiques à Isoform Tie :

Tie1
Tie2

Cellular Effect

Cell Line	Type	Value	Description	References
A549	EC₅₀	>1000 nM Compound: Regorafenib	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 27010810]
A549	IC₅₀	2.05 μM Compound: Regorafenib	Antiproliferative activity against human A549 cells after 48 hrs by MTT assay Antiproliferative activity against human A549 cells after 48 hrs by MTT assay	[PMID: 31158755]
A549	CC₅₀	14.15 μM Compound: 26	Cytotoxicity against human A549 cells Cytotoxicity against human A549 cells	[PMID: 33539089]
BaF3	GI₅₀	9.953 μM Compound: 3	Cytotoxicity in mouse parental BA/F3 cells incubated for 72 hrs by MTS assay Cytotoxicity in mouse parental BA/F3 cells incubated for 72 hrs by MTS assay	[PMID: 30204441]
BaF3	IC₅₀	3.89 nM Compound: Regorafenib	Antiproliferative activity against VEGFR2-transformed mouse BaF3 cells assessed as inhibition of cell proliferation incubated for 3 days by MTT assay Antiproliferative activity against VEGFR2-transformed mouse BaF3 cells assessed as inhibition of cell proliferation incubated for 3 days by MTT assay	[PMID: 37429211]
Caco-2	CC₅₀	0.97 μM Compound: REGORAFENIB	Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay	10.21203/rs.3.rs-23951/v1
Caco-2	IC₅₀	1.67 μM Compound: REGORAFENIB	Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging	10.21203/rs.3.rs-23951/v1
GIST430	GI₅₀	3 μM Compound: 3	Cytotoxicity against human GIST430 cells harboring KIT V654A mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay Cytotoxicity against human GIST430 cells harboring KIT V654A mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay	[PMID: 28991465]
GIST430	GI₅₀	>2000 nM Compound: 3	Antiproliferative activity against human GIST430 cells harboring c-KIT exon 11 primary in-frame V560-L576 deletion mutant and exon 13 heterozygous secondary missense V654A mutant assessed as cell growth inhibition after 120 hrs by methylene blue staining Antiproliferative activity against human GIST430 cells harboring c-KIT exon 11 primary in-frame V560-L576 deletion mutant and exon 13 heterozygous secondary missense V654A mutant assessed as cell growth inhibition after 120 hrs by methylene blue staining	[PMID: 31721578]
GIST48	GI₅₀	785 nM Compound: 3	Antiproliferative activity against human GIST48 cells harboring c-KIT exon 11 homozygous primary missense V560D mutant and exon 17 heterozygous secondary D820A mutant assessed as cell growth inhibition after 120 hrs by methylene blue staining based assay Antiproliferative activity against human GIST48 cells harboring c-KIT exon 11 homozygous primary missense V560D mutant and exon 17 heterozygous secondary D820A mutant assessed as cell growth inhibition after 120 hrs by methylene blue staining based assay	[PMID: 31721578]
GIST882	GI₅₀	285 nM Compound: 3	Antiproliferative activity against human GIST882 cells harboring c-KIT exon 13 homozygous primary K642E mutant assessed as cell growth inhibition after 144 hrs by methylene blue staining based assay Antiproliferative activity against human GIST882 cells harboring c-KIT exon 13 homozygous primary K642E mutant assessed as cell growth inhibition after 144 hrs by methylene blue staining based assay	[PMID: 31721578]
GISTT1	GI₅₀	130 nM Compound: 3	Cytotoxicity against human GISTT1 cells assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay Cytotoxicity against human GISTT1 cells assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay	[PMID: 28991465]
GISTT1	GI₅₀	1350 nM Compound: 3	Cytotoxicity against human GISTT1 cells harboring KIT D816E mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay Cytotoxicity against human GISTT1 cells harboring KIT D816E mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay	[PMID: 28991465]
GISTT1	GI₅₀	380 nM Compound: 3	Cytotoxicity against human GISTT1 cells harboring KIT T670I mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay Cytotoxicity against human GISTT1 cells harboring KIT T670I mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay	[PMID: 28991465]
GISTT1	GI₅₀	119 nM Compound: 3	Antiproliferative activity against human GISTT1 cells harboring heterozygous deletion mutation at C-kit exon 11 assessed as cell growth inhibition after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay Antiproliferative activity against human GISTT1 cells harboring heterozygous deletion mutation at C-kit exon 11 assessed as cell growth inhibition after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay	[PMID: 31721578]
HCT-116	IC₅₀	0.16 μM Compound: Regorafenib	Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay	[PMID: 31158755]
HCT-116	IC₅₀	3.5 μM Compound: Regorafenib	Cytotoxicity against human HCT-116 cells assessed as cell growth inhibition by MTT assay Cytotoxicity against human HCT-116 cells assessed as cell growth inhibition by MTT assay	[PMID: 35763868]
HCT-116	IC₅₀	1.36 μM Compound: Regorafenib	Antitumor activity against human HCT-116 cells assessed as inhibition of cell proliferation incubated for 3 days by MTT assay Antitumor activity against human HCT-116 cells assessed as inhibition of cell proliferation incubated for 3 days by MTT assay	[PMID: 37429211]
HeLa	IC₅₀	2.66 μM Compound: Regorafenib	Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay	[PMID: 31158755]
HepG2	IC₅₀	4.06 μM Compound: Regorafenib	Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay	[PMID: 31158755]
HepG2	IC₅₀	10.43 μM Compound: Reg	Antiproliferative activity against human HepG2 cells measured after 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells measured after 48 hrs by MTT assay	[PMID: 35434624]
HT-29	EC₅₀	>1000 nM Compound: Regorafenib	Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 27010810]
HT-29	IC₅₀	2.87 μM Compound: Regorafenib	Anticancer activity against human HT-29 cells assessed as inhibition of cell proliferation by MTT assay Anticancer activity against human HT-29 cells assessed as inhibition of cell proliferation by MTT assay	[PMID: 32731184]
HT-29	IC₅₀	8.6 μM Compound: Regorafenib	Cytotoxicity against human HT-29 cells assessed as cell growth inhibition by MTT assay Cytotoxicity against human HT-29 cells assessed as cell growth inhibition by MTT assay	[PMID: 35763868]
HT-29	IC₅₀	4.21 μM Compound: Regorafenib	Antitumor activity against human HT-29 cells assessed as inhibition of cell proliferation incubated for 3 days by MTT assay Antitumor activity against human HT-29 cells assessed as inhibition of cell proliferation incubated for 3 days by MTT assay	[PMID: 37429211]
HUVEC	IC₅₀	4.21 nM Compound: Regorafenib	Antiproliferative activity against VEGF-stimulated HUVEC assessed as inhibition of cell proliferation incubated for 3 days by MTT assay Antiproliferative activity against VEGF-stimulated HUVEC assessed as inhibition of cell proliferation incubated for 3 days by MTT assay	[PMID: 37429211]
MCF7	IC₅₀	2.71 μM Compound: Regorafenib	Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 31158755]
MDA-MB-231	IC₅₀	1.21 μM Compound: Regorafenib	Antitumor activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 3 days by MTT assay Antitumor activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 3 days by MTT assay	[PMID: 37429211]
MDA-MB-468	IC₅₀	3.02 μM Compound: Regorafenib	Antitumor activity against human MDA-MB-468 cells assessed as inhibition of cell proliferation incubated for 3 days by MTT assay Antitumor activity against human MDA-MB-468 cells assessed as inhibition of cell proliferation incubated for 3 days by MTT assay	[PMID: 37429211]
MGC-803	IC₅₀	9.46 μM Compound: Reg	Antiproliferative activity against human MGC-803 cells measured after 48 hrs by MTT assay Antiproliferative activity against human MGC-803 cells measured after 48 hrs by MTT assay	[PMID: 35434624]
MOLM-13	GI₅₀	887 nM Compound: 3	Antiproliferative activity against human MOLM13 harboring FLT3-ITD mutant assessed as cell growth inhibition after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay Antiproliferative activity against human MOLM13 harboring FLT3-ITD mutant assessed as cell growth inhibition after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay	[PMID: 31721578]
NCM460	IC₅₀	198.16 μM Compound: Regorafenib	Cytotoxicity against human NCM460 cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against human NCM460 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 31158755]
OVCAR-3	IC₅₀	3.4 μM Compound: Regorafenib	Antitumor activity against human OVCAR-3 cells assessed as inhibition of cell proliferation incubated for 3 days by MTT assay Antitumor activity against human OVCAR-3 cells assessed as inhibition of cell proliferation incubated for 3 days by MTT assay	[PMID: 37429211]
Sf9	IC₅₀	0.005 μM Compound: II; BAY 73-450	Inhibition of human N-terminal GST tagged VEGFR-2 expressed in baculovirus infected Sf9 cells using poly (Glu,Tyr) 4:1 as substrate in presence of ATP by Kinase-Glo luminescence assay Inhibition of human N-terminal GST tagged VEGFR-2 expressed in baculovirus infected Sf9 cells using poly (Glu,Tyr) 4:1 as substrate in presence of ATP by Kinase-Glo luminescence assay	[PMID: 31284081]
Sf9	IC₅₀	116 nM Compound: 3	Inhibition of recombinant N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) (unknown origin) expressed in baculovirus infected Sf9 insect cells using poly (Glu,Tyr) 4:1 as substrate measured after 150 mins in presence of Inhibition of recombinant N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) (unknown origin) expressed in baculovirus infected Sf9 insect cells using poly (Glu,Tyr) 4:1 as substrate measured after 150 mins in presence of	[PMID: 31721578]
Sf9	IC₅₀	82 nM Compound: 3	Inhibition of wild type recombinant GST-tagged FLT3 (Y567 to S993 residues) (unknown origin) expressed in baculovirus infected Sf9 insect cells using Her2 peptide as substrate measured after 4 hrs in presence of ATP by Kinase-Glo Plus reagent-based lumine Inhibition of wild type recombinant GST-tagged FLT3 (Y567 to S993 residues) (unknown origin) expressed in baculovirus infected Sf9 insect cells using Her2 peptide as substrate measured after 4 hrs in presence of ATP by Kinase-Glo Plus reagent-based lumine	[PMID: 31721578]
SK-OV-3	IC₅₀	3.85 μM Compound: Regorafenib	Antitumor activity against human SK-OV-3 cells assessed as inhibition of cell proliferation incubated for 3 days by MTT assay Antitumor activity against human SK-OV-3 cells assessed as inhibition of cell proliferation incubated for 3 days by MTT assay	[PMID: 37429211]
SW-620	IC₅₀	1.17 μM Compound: Regorafenib	Antiproliferative activity against human SW620 cells after 48 hrs by MTT assay Antiproliferative activity against human SW620 cells after 48 hrs by MTT assay	[PMID: 31158755]
T-24	IC₅₀	5.98 μM Compound: Reg	Antiproliferative activity against human T24 cells measured after 48 hrs by MTT assay Antiproliferative activity against human T24 cells measured after 48 hrs by MTT assay	[PMID: 35434624]

In Vitro

Regorafenib (0-10 μM, 96 h) shows anti-proliferation activity in GIST 882, Thyroid TT, MDA-MB-231, HepG2, A375 and SW620 cells^[1].
Regorafenib (0-3000 nM, 30 min) inhibits the autophosphorylation of VEGFR2, TIE2 and PDGFR-β, and inhibits FGFR and pERK1/2^[1].
Regorafenib 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^[3].

MedChemExpress (MCE) 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.

In Vivo

Regorafenib (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 (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.

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.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 755037-03-7
Appearance Solid
Masse moléculaire 482.82
Formule C₂₁H₁₅ClF₄N₄O₃
Color White to off-white
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
Synonyms

BAY 73-4506
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (96)

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Journal Impact Factor

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

Regorafenib induces lethal autophagy arrest by stabilizing PSAT1 in glioblastoma. [Abstract]

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
Acta Pharm Sin B

2026 Jun 18.
Acta Pharm Sin B

2026 Apr 24.
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)

Deep Learning-Powered Scalable Cancer Organ Chip for Cancer Precision Medicine. [Abstract]

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 Jul 9: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 2:102053. PMID: 40187357
Biomaterials

Automated discovery of nanomaterials via drug aggregation induced emission. [Abstract]

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
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 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.
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):2958-66. PMID: 25790278
Biochem Pharmacol

Pitavastatin overcomes multi-drug resistance in CRC and NSCLC by targeting the NRP1-ZFX axis. [Abstract]

2025 Jul 18:241:117183. 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
Cancer Nanotechnol

2023 May 9.
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). pii: E2915. PMID: 30257515

Regorafenib purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2018 Sep 25;19(10). pii: E2915. [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.
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 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.
J Cell Mol Med

Inactivation of CDK12 Enhances Mitochondrial Efficiency to Suppress DNA Damage. [Abstract]

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

FRET two-hybrid assay-based target drug screening in living cells. [Abstract]

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 Jul 25:117042. PMID: 39067772
Mol Carcinog

Venetoclax Synergizes With Regorafenib for Colorectal Cancer by Targeting BCL-2. [Abstract]

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

Cytotoxic metabolites from the marine-associated Streptomyces sp. ZZ1944. [Abstract]

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 Aug 22:104319. PMID: 39181490
Fundam Clin Pharmacol

Inhibition of organic cation transporter 3 activity by tyrosine kinase inhibitors. [Abstract]

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

Regorafenib promotes ferroptosis in acute myeloid leukemia by upregulating NOX4. [Abstract]

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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]

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Biochem Biophys Res Commun

Allosteric SHP2 inhibition enhances regorafenib's effectiveness in colorectal cancer treatment. [Abstract]

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Investigation of the effect of plasma albumin levels on regorafenib-induced hepatotoxicity using a validated liquid chromatography-tandem mass spectrometry method. [Abstract]

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Cell Physiol Biochem

Triggering of Suicidal Erythrocyte Death by Regorafenib. [Abstract]

2016;38(1):160-72. PMID: 26765545
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Differential Inhibition of Equilibrative Nucleoside Transporter 1 (ENT1) Activity by Tyrosine Kinase Inhibitors. [Abstract]

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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
The Medical College of Wisconsin

2026.
bioRxiv

2026 Apr 15.
chemRxiv

2026 Apr 6.
bioRxiv

2025 Dec 5.
bioRxiv

Hidden-driver inference reveals synergistic brain-penetrant therapies for medulloblastoma. [Abstract]

2025 Nov 20:2025.11.20.689490. PMID: 41332625
University of Otago

2025 Oct 7.
Hong Kong Polytechnic University

2025.
bioRxiv

Closing the loop: Teaching single-cell foundation models to learn from perturbations. [Abstract]

2025 Jul 12:2025.07.08.663754. PMID: 40672312
Hong Kong Polytechnic University

2025.
Patent

US20230101335A1.
bioRxiv

Low-Cost Robotic Manipulation of Live Microtissues for Cancer Drug Testing. [Abstract]

2024 Aug 6:2024.03.21.586169. PMID: 38586030
bioRxiv

2024 June 12.
Research Square Preprint

2024 Feb 8.
Cancer Diagn Progn

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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
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.

Solvant et solubilité

In Vitro:

DMSO : 125 mg/mL (258.90 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0712 mL

10.3558 mL

20.7117 mL

5 mM

0.4142 mL

2.0712 mL

4.1423 mL

10 mM

0.2071 mL

1.0356 mL

2.0712 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 7.5 mg/mL (15.53 mM); Clear solution

This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 2

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: 2.75 mg/mL (5.70 mM); Suspended solution; Need ultrasonic

Protocol 3

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.18 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (278 KB)
SDS (396 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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]. Heng DY, et al. Targeted therapy for metastatic renal cell carcinoma: current treatment and future directions. Ther Adv Med Oncol, 2010, 2(1), 39-49. [Content Brief]

[3]. 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]

[4]. Wagner J, et al. Anti-tumor effects of ONC201 in combination with VEGF-inhibitors significantly impacts colorectal cancer growth and survival in vivo through complementary non-overlapping mechanisms. J Exp Clin Cancer Res. 2018 Jan 22;37(1):11. [Content Brief]

[5]. Matsuoka K, et al. Effective Sequential Combined Chemotherapy with Tipiracil and Regorafenib in Human Colorectal Cancer Cells. Int J Mol Sci. 2018 Sep 25;19(10). pii: E2915. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0712 mL	10.3558 mL	20.7117 mL	51.7791 mL
	5 mM	0.4142 mL	2.0712 mL	4.1423 mL	10.3558 mL
	10 mM	0.2071 mL	1.0356 mL	2.0712 mL	5.1779 mL
	15 mM	0.1381 mL	0.6904 mL	1.3808 mL	3.4519 mL
	20 mM	0.1036 mL	0.5178 mL	1.0356 mL	2.5890 mL
	25 mM	0.0828 mL	0.4142 mL	0.8285 mL	2.0712 mL
	30 mM	0.0690 mL	0.3452 mL	0.6904 mL	1.7260 mL
	40 mM	0.0518 mL	0.2589 mL	0.5178 mL	1.2945 mL
	50 mM	0.0414 mL	0.2071 mL	0.4142 mL	1.0356 mL
	60 mM	0.0345 mL	0.1726 mL	0.3452 mL	0.8630 mL
	80 mM	0.0259 mL	0.1294 mL	0.2589 mL	0.6472 mL
	100 mM	0.0207 mL	0.1036 mL	0.2071 mL	0.5178 mL

Regorafenib

96 Cited Publications

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Chemical Information

Publications (96)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table