Regorafenib (BAY 73-4506)

Name: Regorafenib (BAY 73-4506)
Brand: Adooq Bioscience
SKU: A10250
Rating: 100 (9 reviews)

Catalog No.: A10250

VEGFR inhibitor

Product Citations (9)

Regorafenib (BAY 73-4506) Chemical Structure

CAS NO. 755037-03-7

Regorafenib (BAY 73-4506) is a multikinase inhibitor with IC50 of 17, 40 and 69 nM c-KIT, VEGFR2, B-Raf. Regorafenib (BAY 73-4506) is an orally bioavailable multikinase inhibitor targeting both the tumor and its vasculature.

Availability: In stock

Package	Price	Qty
25 mg	$50.00
100 mg	$130.00
10mM * 1mL in DMSO	$69.00
Custom Size	Get quote

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Products are for laboratory research use only. Not for human use. We do not sell to patients.

Adooq Products cited in reputable paper

Publications Citing Use of Adooq Regorafenib (BAY 73-4506)

Paula Sagmeister, .et al. Comparative Response of HCC Cells to TKIs: Modified in vitro Testing and Descriptive Expression Analysis, J Hepatocell Carcinoma, 2022, Jul 9;9:595-607 PMID: 35845819
Majid Momeny, .et al. Cediranib, a pan-inhibitor of vascular endothelial growth factor receptors, inhibits proliferation and enhances therapeutic sensitivity in glioblastoma cells, Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
Jindal A, .et al. Milciclib and sorafenib synergistically downregulate c-Myc to suppress tumor growth in an orthotopic murine model of human hepatocellular carcinoma, J Transl Sci, 2020, 7: 1-10
Makoto Koyama, .et al. Low-dose trametinib and Bcl-xL antagonist have a specific antitumor effect in KRAS-mutated colorectal cancer cells, Int J Oncol, 2020, Sep 2 PMID: 32901840
Mariko Fujisawa, .et al. Involvement of the Interferon Signaling Pathways in Pancreatic Cancer Cells, Anticancer Res, 2020, 40: 4445-4455 PMID: 32727774
Majid Momeny, .et al. Cediranib, an inhibitor of vascular endothelial growth factor receptor kinases, inhibits proliferation and invasion of prostate adenocarcinoma cells, Eur J Pharmacol, 2020, 882:173298
Sunil Kumar Yadava, .et al. Low Temperature, Easy Scaling Up Method for Development of Smart Nanostructure Hybrid Lipid Capsules for Drug Delivery Application, Colloids Surf B Biointerfaces, 2020, Mar 2;190:110927 PMID: 32169777
Takeshi Uenaka, .et al. In silico drug screening by using genome-wide association study data repurposed dabrafenib, an anti-melanoma drug, for Parkinson's disease, Hum Mol Genet, 2018, Nov 15; 27(22): 3974-3985 PMID: 30137437
Yi Xu, .et al. Knockdown of delta-5-desaturase promotes the anti-cancer activity of dihomo-γ-linolenic acid and enhances the efficacy of chemotherapy in colon cancer cells expressing COX-2, Free Radic Biol Med, 2016, Jul; 96: 67-77 PMID: 27101738

Biological Activity

Targets

Target	Value
RET	IC50: 1.5nM
Raf-1	IC50: 2.5nM
VEGFR2	IC50: 4.2nM
Kit	IC50: 7nM
VEGFR1	IC50: 13nM
B-Raf(V600E)	IC50: 19nM
PDGFRβ	IC50: 22nM
B-Raf	IC50: 28nM
VEGFR3	IC50: 46nM
FGFR1	IC50: 202nM
Tie-2	IC50: 311nM

Solubility *

In vitro (25°C)	DMSO	88 mg/mL (182.26 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	2% DMSO+30% PEG 300+5% Tween 80+ddH2O	4 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Preparing Stock Solutions

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.1 mM	20.71 mL	103.56 mL	207.13 mL
0.5 mM	4.14 mL	20.71 mL	41.43 mL
1 mM	2.07 mL	10.36 mL	20.71 mL
5 mM	0.41 mL	2.07 mL	4.14 mL

*The above data is based on the productmolecular weight 482.8. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Chemical Properties

Catalog Num	A10250
Actions	Inhibitor
CAS No.	755037-03-7
Formula	C21H15ClF4N4O3
M. Wt	482.8
Purity	>98%
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
Storage	Store lyophilized at -20ºC, keep desiccated. In lyophilized form, the chemical is stable for 36 months. In solution, store at -20ºC and use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.