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Regorafenib (BAY 73-4506) Multikinase inhibitor

Name: Regorafenib (BAY 73-4506)
Brand: Selleck Chemicals
SKU: S1178
Availability: InStock
Rating: 5 (216 reviews)

Cat.No.S1178

Regorafenib is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit (c-Kit), RET (c-RET) and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM in cell-free assays, respectively. Regorafenib induces autophagy.

Chemical Structure

Molecular Weight: 482.82

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Quality Control

Batch: Purity: 99.91%

99.91

Related Targets	EGFR PDGFR FGFR c-Met Src MEK CSF-1R FLT3 HER2 c-Kit
Other VEGFR Inhibitors	SAR131675 SU5402 Cediranib (AZD2171) Vatalanib (PTK787) 2HCl Linifanib (ABT-869) Anlotinib (AL3818) Dihydrochloride Apatinib (YN968D1) Apatinib (YN968D1) mesylate Ki8751 ZM 323881 HCl

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
Hep3B	Apoptosis Assay	1–5 μM	48 h		inhibits cell growth	26329608
PLC/PRF/5	Apoptosis Assay	1–5 μM	48 h		inhibits cell growth	26329608
HepG2	Apoptosis Assay	1–5 μM	48 h		inhibits cell growth	26329608
HEK293	Function Assay	0.5 μM	2/4/6 h		reduces GRP78 expression	25858032
GEO	Growth Inhibition Assay	0.01-20 μM	96 h	DMSO	inhibits cell growth in a dose-dependent manner	25838391
SW48	Growth Inhibition Assay	0.01-20 μM	96 h	DMSO	inhibits cell growth in a dose-dependent manner	25838391
HT29	Growth Inhibition Assay	0.01-20 μM	96 h	DMSO	inhibits cell growth in a dose-dependent manner	25838391
SW480	Growth Inhibition Assay	0.01-20 μM	96 h	DMSO	inhibits cell growth in a dose-dependent manner	25838391
SW620	Growth Inhibition Assay	0.01-20 μM	96 h	DMSO	inhibits cell growth in a dose-dependent manner	25838391
HCT116	Growth Inhibition Assay	0.01-20 μM	96 h	DMSO	inhibits cell growth in a dose-dependent manner	25838391
LOVO	Growth Inhibition Assay	0.01-20 μM	96 h	DMSO	inhibits cell growth in a dose-dependent manner	25838391
HCT150	Growth Inhibition Assay	0.01-20 μM	96 h	DMSO	inhibits cell growth in a dose-dependent manner	25838391
SW48-CR	Growth Inhibition Assay	0.01-20 μM	96 h	DMSO	inhibits cell growth in a dose-dependent manner	25838391
GEO-CR	Growth Inhibition Assay	0.01-20 μM	96 h	DMSO	inhibits cell growth in a dose-dependent manner	25838391
KB-31	Growth Inhibition Assay				IC50=5.5±0.3 nM	25753361
KB-G2	Growth Inhibition Assay				IC50=9.1±0.1 nM	25753361
LLC-PK1	Growth Inhibition Assay				IC50=42.0±3.2 nM	25753361
LLC-PK1/MRP2	Growth Inhibition Assay				IC50=82.4±2.7 nM	25753361
HEK293	Growth Inhibition Assay				IC50=11.0±1.2 nM	25753361
HEK293/OATP1B1	Growth Inhibition Assay				IC50=6.2±0.3 nM	25753361
HROC18	Growth Inhibition Assay				IC50=1.3 μM	25309914
HROC24	Growth Inhibition Assay				IC50=4.6 μM	25309914
HROC43	Growth Inhibition Assay				IC50=5.3 μM	25309914
HROC46	Growth Inhibition Assay				IC50=2.4 μM	25309914
RJ345	Function Assay	0.5/5 μM	24 h	DMSO	inhibits the cell migration	25253994
RJ348	Function Assay	0.5/5 μM	24 h	DMSO	inhibits the cell migration	25253994
MCF-7	Function Assay	0.5/5 μM	24 h	DMSO	inhibits the cell migration	25253994
MDA-MB-231	Function Assay	0.5/5 μM	24 h	DMSO	inhibits the cell migration	25253994
HT15	Growth Inhibition Assay	1-20 μM	48 h		inhibits cell growth in a dose-dependent manner	25071018
DLD1	Growth Inhibition Assay	1-20 μM	48 h		inhibits cell growth in a dose-dependent manner	25071018
HT-29	Growth Inhibition Assay	1-20 μM	48 h		inhibits cell growth in a dose-dependent manner	25071018
Hct-116	Growth Inhibition Assay	1-20 μM	48 h		inhibits cell growth in a dose-dependent manner	25071018
HT15	Apoptosis Assay	1-10 μM	48 h		induces cell death in a dose-dependent manner	25071018
DLD1	Apoptosis Assay	1-10 μM	48 h		induces cell death in a dose-dependent manner	25071018
HT-29	Apoptosis Assay	1-10 μM	48 h		induces cell death in a dose-dependent manner	25071018
Hct-116	Apoptosis Assay	1-10 μM	48 h		induces cell death in a dose-dependent manner	25071018
GBM5	Apoptosis Assay	0.5–1.0 μM	24 h	DMSO	interacts with lapatinib to induce cell death	24911215
GBM6	Apoptosis Assay	0.5–1.0 μM	24 h	DMSO	interacts with lapatinib to induce cell death	24911215
GBM12	Apoptosis Assay	0.5–1.0 μM	24 h	DMSO	interacts with lapatinib to induce cell death	24911215
GBM14	Apoptosis Assay	0.5–1.0 μM	24 h	DMSO	interacts with lapatinib to induce cell death	24911215
Hep3B	Growth Inhibition Assay	1–2.5 μM	24/48/72 h		inhibits cell growth	24885890
PLC/PRF/5	Growth Inhibition Assay	1–2.5 μM	24/48/72 h		inhibits cell growth	24885890
HepG2	Growth Inhibition Assay	1–2.5 μM	24/48/72 h		inhibits cell growth	24885890
HCT116	Function Assay	10/20/40 μM	24 h		induces PUMA protein and mRNA expression in a dose- and time-dependent manner	24763611
Lim2405	Function Assay	40 μM	24 h		induces PUMA protein and cell apoptosis	24763611
LoVo	Function Assay	40 μM	24 h		induces PUMA protein and cell apoptosis	24763611
Lim1215	Function Assay	40 μM	24 h		induces PUMA protein and cell apoptosis	24763611
SW48	Function Assay	40 μM	24 h		induces PUMA protein and cell apoptosis	24763611
RKO	Function Assay	40 μM	24 h		induces PUMA protein and cell apoptosis	24763611
SW837	Function Assay	40 μM	24 h		induces PUMA protein and cell apoptosis	24763611
SW1463	Function Assay	40 μM	24 h		induces PUMA protein and cell apoptosis	24763611
SW480	Function Assay	40 μM	24 h		induces PUMA protein and cell apoptosis	24763611
Vaco432	Function Assay	40 μM	24 h		induces PUMA protein and cell apoptosis	24763611
Vaco400	Function Assay	40 μM	24 h		induces PUMA protein and cell apoptosis	24763611
DLD1	Function Assay	40 μM	24 h		induces PUMA protein and cell apoptosis	24763611
HT29	Function Assay	40 μM	24 h		induces PUMA protein and cell apoptosis	24763611
PLC/PRF/5	Growth Inhibition Assay	1–5µM	24/48/72 h		inhibits cell growth	23169148
HepG2	Growth Inhibition Assay	1–5µM	24/48/72 h		inhibits cell growth	23169148
Hep3B	Growth Inhibition Assay	1–5µM	24/48/72 h		inhibits cell growth	23169148
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit exon 11 deletion (557 to 558 residues) mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.021 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of TEL-fused PDGFRbeta (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.029 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit exon 11 deletion (557 to 558 residues) and D816H mutant and T670I mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.033 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit exon 11 deletion (557 to 558 residues) and A829P mutant and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.047 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit exon 11 deletion (557 to 558 residues) and N822K mutant and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.049 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of TEL-fused PDGFRalpha (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.051 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit exon 11 deletion (557 to 558 residues) and D820A mutant and D820A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.063 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit exon 11 deletion (557 to 558 residues) and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.094 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit V560D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.108 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit exon 9 AY502 to 503 insertion mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.114 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of KDR (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.114 μM.	30204441
GISTT1	Cytotoxicity assay		72 hrs		Cytotoxicity against human GISTT1 cells assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay, GI50 = 0.13 μM.	28991465
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit exon 11 deletion (557 to 558 residues) and V654A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.231 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit exon 11 deletion (557 to 558 residues) and D816H mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.29 μM.	30204441
GISTT1	Cytotoxicity assay		72 hrs		Cytotoxicity against human GISTT1 cells harboring KIT T670I mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay, GI50 = 0.38 μM.	28991465
BA/F3	Growth inhibition assay		72 hrs		Inhibition of PDGFRalpha V561D/D842V mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.522 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit V560D/V654A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.549 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit exon 9 AY502 to 503 insertion and D816 mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.833 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit V560D/D816H mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.834 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit exon 11 deletion (560 to 578 residues) mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.943 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit exon 9 AY502 to 503 insertion and V654 mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 1.27 μM.	30204441
GISTT1	Cytotoxicity assay		72 hrs		Cytotoxicity against human GISTT1 cells harboring KIT D816E mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay, GI50 = 1.35 μM.	28991465
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit D816V mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 2.371 μM.	30204441
GIST430	Cytotoxicity assay		72 hrs		Cytotoxicity against human GIST430 cells harboring KIT V654A mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay, GI50 = 3 μM.	28991465
BA/F3	Cytotoxicity assay		72 hrs		Cytotoxicity in mouse parental BA/F3 cells incubated for 72 hrs by MTS assay, GI50 = 9.953 μM.	30204441
U-2 OS	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	29435139
A673	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
DAOY	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
Saos-2	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
BT-37	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
RD	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
BT-12	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
MG 63 (6-TG R)	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
NB1643	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
OHS-50	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
SJ-GBM2	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
SK-N-MC	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
NB-EBc1	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
LAN-5	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
Rh18	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 97 mg/mL (200.9 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	2% DMSO 1 30% PEG 300 2 5% Tween 80 3 ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (10.36mM)	Taking the 1 mL working solution as an example, add 20 μL of 250 mg/ml clarified DMSO stock solution to 300 μL PEG300, mix evenly to clarify it; add 50 μL Tween-80 to the above system, mix evenly to clarify it; Then continue to add 630 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	2%DMSO 1 98% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (10.36mM)	Taking the 1 mL working solution as an example, add 20 μL of 250 mg/ml clarified DMSO stock solution to 980 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (10.36mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	482.82	Formula	C₂₁H₁₅ClF₄N₄O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	755037-03-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Fluoro-Sorafenib, BAY 73-4506			Smiles	CNC(=O)C1=NC=CC(=C1)OC2=CC(=C(C=C2)NC(=O)NC3=CC(=C(C=C3)Cl)C(F)(F)F)F

Mechanism of Action

Targets/IC₅₀/Ki	RET (Cell-free assay) 1.5 nM Raf-1 (Cell-free assay) 2.5 nM VEGFR2 (Cell-free assay) 4.2 nM Kit (Cell-free assay) 7 nM VEGFR1 (Cell-free assay) 13 nM B-Raf (V600E) (Cell-free assay) 19 nM PDGFRβ (Cell-free assay) 22 nM B-Raf (Cell-free assay) 28 nM VEGFR3 (Cell-free assay) 46 nM
In vitro	Regorafenib strongly prevents VEGFR2 autophosphorylation in NIH-3T3/VEGFR2 cells with IC50 of 3 nM. In HAoSMCs, this compound suppresses PDGFR-β autophosphorylation after stimulation with PDGF-BB, with an IC50 of 90 nM. It also inhibits FGFR signaling in MCF-7 breast cancer (BC) cells stimulated with FGF10. This chemical very potently inhibited the mutant receptors KIT^K642E and RET^C634W, with IC50 of approximately 20 nM and 10 nM, respectively. It inhibits the proliferation of VEGF¹⁶⁵-stimulated HUVECs, with an IC50 of approximately 3 nM. This compound prevents the proliferation of FGF2-stimulated HUVECs and of PDGF-BB-stimulated HAoSMCs with IC50 of 127 nM and 146 nM, respectively. It targets both tumor cell proliferation and tumor vasculature through inhibition of receptors of tyrosine kinases (VEGFR, KIT, RET, FGFR, and PDGFR) and serine/threonine kinases (Raf and p38MAPK). This chemical suppresses growth of human Hep3B, PLC/PRF/5 and HepG2 cells in a concentration- and time-dependent manner.
Kinase Assay	Kinase assays
Kinase Assay	In vitro assays using recombinant VEGFR2 (murine aa785–aa1367), VEGFR3 (murine aa818–aa1363), PDGFRβ (aa561–aa1106), Raf-1 (aa305–aa648) and BRafV600E (aa409–aa765) kinase domains are performed. Initial in vitro kinase inhibition profiling is performed at a fixed 1 μM concentration of this compound. Inhibitory concentration of 50% (IC50) values are determined from selected responding kinases, e.g., VEGFR1 and RET. TIE2 kinase inhibition is measured with a homogeneous time-resolved fluorescence (HTRF) assay using a recombinant fusion protein of glutathione-S-transferase, the intracellular domain of TIE2 and the peptide biotin-Ahx-EPKDDAYPLYSDFG as substrate.
In vivo	Regorafenib reveals potent dose-dependent TGI in various preclinical human xenograft models in mice, with tumor shrinkages in breast MDA-MB-231 and renal 786-O carcinoma models. This compound prevents not only the growth of syngeneic primary 4T1 breast tumors growing orthotopically in the fat pad, but also suppresses the formation of tumor metastasis in the lung.
References	[1] https://pubmed.ncbi.nlm.nih.gov/21170960/ [2] https://pubmed.ncbi.nlm.nih.gov/21789125/ [3] https://pubmed.ncbi.nlm.nih.gov/22777740/

Applications

Methods	Biomarkers	PMID
Western blot	PUMA / p53 Bim / Bid / Bak / Bcl-Xl / Mcl-1 p-p65(S536) / p65 p-FGFR2 / p-FRS2α / p-AKT / p-MAPK / p-P90RSK / FGFR2 / AKT / MAPK / p90RSK Cyclin D / Cyclin E / Cyclin A / Cyclin B / p27 / p21 p-STAT3 / STAT3 / PARP / Caspase-9	24763611
Immunofluorescence	p65 F-actin / Vimentin / E-cadherin	24763611
Growth inhibition assay	GI50 Cell viability	29573334

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06321055	Not yet recruiting	Advanced Gastrointestinal Stromal Tumor	Bayer	March 20 2024	--
NCT06137170	Active not recruiting	Metastatic Colorectal Cancer	Bayer	March 1 2024	--
NCT06029010	Completed	Metastatic Colorectal Cancer	Bayer	August 31 2023	--
NCT05370807	Recruiting	Melanoma Stage III\|Melanoma Stage IV	Universitair Ziekenhuis Brussel	October 3 2022	Phase 2

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

Question 1:
How to resuspend it for in vivo studies?

Answer:
For in vivo study, we recommend to use 2% DMSO+30% PEG 300+5% Tween 80+ddH2O up to 5mg/ml for it.

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