Regorafenib (BAY 73-4506)

Catalog No.: A10250

VEGFR inhibitor

Regorafenib (BAY 73-4506)

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.

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25 mg

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100 mg

Regular Price: $130.00

Special Price $104.00

10mM * 1mL in DMSO

Regular Price: $69.00

Special Price $55.20

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  • 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
  • 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
  • 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

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.
Targets
Target Value
RETIC50: 1.5nM
Raf-1IC50: 2.5nM
VEGFR2IC50: 4.2nM
KitIC50: 7nM
VEGFR1IC50: 13nM
B-Raf(V600E)IC50: 19nM
PDGFRβIC50: 22nM
B-RafIC50: 28nM
VEGFR3IC50: 46nM
FGFR1IC50: 202nM
Tie-2IC50: 311nM
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.
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.

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.

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