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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.

Availability: In stock

Package Price Qty
25 mg
$50.00
100 mg
$130.00
10mM * 1mL in DMSO
$69.00
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  • 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
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  • 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
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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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