Regorafenib (Synonyms: BAY 73-4506)

Name: Regorafenib
Brand: MedChemExpress
SKU: HY-10331
Rating: 5.0 (62 reviews)

Cat. No.: HY-10331 Purity: 99.93%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

For research use only. We do not sell to patients.

Regorafenib Chemical Structure

CAS No. : 755037-03-7

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 66	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 66	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 38	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 120	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 180	In-stock	Estimated Time of Arrival: December 31
500 mg	USD 390	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 62 publication(s) in Google Scholar

Other Forms of Regorafenib:

59 Publications Citing Use of MCE Regorafenib

: Regorafenib purchased from MedChemExpress. Usage Cited in: Neoplasia. 2023 Mar 18;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.

: 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.

: 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.

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Tie2

Biological Activity
Purity & Documentation
References
Customer Review

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)

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]
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]
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	> 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]
GIST430	GI₅₀	3000 nM 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]
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	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]
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]
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]
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	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]
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]
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]
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]
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]
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]
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.

Clinical Trial

Molecular Weight

482.82

Formula

C₂₁H₁₅ClF₄N₄O₃

CAS No.

755037-03-7

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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

Please enter your animal formula composition:

DMSO +

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Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.93%

Select Batch:

Data Sheet (278 KB) SDS (393 KB)

COA (245 KB) LCMS (86 KB) Elemental Analysis Report (102 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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 Related Classifications

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Regorafenib (Synonyms: BAY 73-4506)

Customer Review

Other Forms of Regorafenib:

59 Publications Citing Use of MCE Regorafenib

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Regorafenib (Synonyms: BAY 73-4506)

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Other Forms of Regorafenib:

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59 Publications Citing Use of MCE Regorafenib

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