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Regorafenib monohydrate

Regorafenib monohydrate Structure
Regorafenib monohydrate structure
CAS No.
1019206-88-2
Chemical Name:
Regorafenib monohydrate
Synonyms
Regorafenib hydrate;Refined Sunflower Oil;4-[4-[[[[4-Chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-2-pyridinecarboxamide hydrate;Regorafenib H2O;Regfini hydrate;Regfenib monohydrate;Regorafenib (200 mg);Regorafenib monohydrate;BAY 73-4506 Monohydrate;Regorafenibhydrate USP/EP/BP
CBNumber:
CB52641189
Molecular Formula:
C21H17ClF4N4O4
Molecular Weight:
500.83
MDL Number:
MOL File:
1019206-88-2.mol
MSDS File:
SDS
TDS File:
TDS
Last updated:2026-07-27 17:00:41
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Regorafenib monohydrate Properties

storage temp. 2-8°C
solubility ≥25.05 mg/mL in DMSO; insoluble in H2O
form solid
color Light yellow to orange
InChI 1S/C21H15ClF4N4O3.H2O/c1-27-19(31)18-10-13(6-7-28-18)33-12-3-5-17(16(23)9-12)30-20(32)29-11-2-4-15(22)14(8-11)21(24,25)26;/h2-10H,1H3,(H,27,31)(H2,29,30,32);1H2
InChIKey ZOPOQLDXFHBOIH-UHFFFAOYSA-N
SMILES O(C1C=CC(NC(=O)NC2C=CC(Cl)=C(C(F)(F)F)C=2)=C(F)C=1)C1=CC=NC(C(=O)NC)=C1.O
FDA UNII MGN125FS9D
UNSPSC Code 41116107
NACRES NA.24

SAFETY

Risk and Safety Statements

Symbol(GHS)  Health Hazard (GHS08)Environment (GHS09)
GHS08,GHS09
Signal word  Warning
Hazard statements  H361fd-H373-H410
Precautionary statements  P201-P273-P308+P313
target organs Liver
WGK Germany  WGK 3
Storage Class 11 - Combustible Solids
Hazard Classifications Aquatic Acute 1
Aquatic Chronic 1
Repr. 2
STOT RE 2
Excepted Quantities Max Inner Pack (30g or 30ml) and Max Outer Pack (1Kg or 1L)

Regorafenib monohydrate price

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Biosynth FR103988 Regorafenib monohydrate 1019206-88-2 2g $162.26 2026-06-04 Buy
Biosynth FR103988 Regorafenib monohydrate 1019206-88-2 5g $259.6 2026-06-04 Buy
Biosynth FR103988 Regorafenib monohydrate 1019206-88-2 10g $454.3 2026-06-04 Buy
Biosynth FR103988 Regorafenib monohydrate 1019206-88-2 25g $973.5 2026-06-04 Buy
Biosynth FR103988 Regorafenib monohydrate 1019206-88-2 50g $1622.5 2026-06-04 Buy
Product number Packaging Price Buy
FR103988 2g $162.26 Buy
FR103988 5g $259.6 Buy
FR103988 10g $454.3 Buy
FR103988 25g $973.5 Buy
FR103988 50g $1622.5 Buy

Regorafenib monohydrate Chemical Properties, Uses, Production

Description

Regorafenib monohydrate (BAY 73-4506) is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor with potent anti-tumour and anti-angiogenic activity. It is approved for the treatment of metastatic colorectal cancer, advanced gastrointestinal mesenchymal stromal tumours and hepatocellular carcinoma.

Uses

4-[4-[[4-Chloro-3-(trifluoromethyl)phenyl]carbamoylamino]-3-fluorophenoxy]-N-methylpyridine-2-carboxamide Hydrate can be used as an anti-tumor drug.

Definition

ChEBI: Regorafenib hydrate is a hydrate that is the monohydrate form of anhydrous regorafenib. Used for for the treatment of metastatic colorectal cancer in patients who have previously received chemotherapy, anti-EGFR or anti-VEGF therapy. It has a role as an antineoplastic agent, a tyrosine kinase inhibitor and a hepatotoxic agent. It contains a regorafenib.

Biological Activity

regorafenib monohydrate is a multitargetedinhibitor of tyrosine kinase with ic50 values of 13nm, 4.2nm, 46nm, 2.5nm, 28nm, 19nm, 202nm, 22nm, 7nm, 1.5nm and 311nm, respectively for vegfr-1, mvegfr-2, mvegfr-3, raf-1, braf wt, brafv600e, fgfr-1, pdgfr-β, c-kit, retand tie2 [1].regorafenib is a multikinase inhibitor of both intracellular and membrane-bound rtks. it shows potent inhibition of angiogenic and stromal rtks like vegf receptors-1-3, pdgfr-β and fgf receptor-1 with ic50 values ranging from4.2 to 311nm in biochemical assays. it also inhibits oncogenic rtks, such as ret and c-kit, with ic50 values ranging from 1.5 to 28nm in cellular assays [1].regorafenib is reported to have anti-tumor efficacy to various tumors including breast, pancreas, thyroid, melanoma, gist, and crc with a mean ic50 value less than 1μm. these inhibition effects of tumor growth are also found in mouse xenograft models after the treatment of regorafenib at dose ranging from 10 to 100 mg/kg [1].

Mechanism of action

The mechanism of anticancer action of Regorafenib monohydrate is similar to that of Regorafenib, an oral multikinase inhibitor that blocks tyrosine kinases that are active in angiogenesis, cancer development and growth, and maintenance of the tumour microenvironment. It is superior to sorafenib in blocking both vascular endothelial growth factor receptor and TIE2, a molecule with an important role in angiogenesis.

Clinical Use

Regorafenib was approved by the U.S. Food and Drug Administration (FDA) in September 2012 for the treatment of metastatic colorectal cancer in patients who have previously undergone fluoropyrimidine-, oxaliplatin-, and irinotecan-based therapies. The FDA expanded the approved use of the drug to include patients with advanced gastrointestinal stromal tumors (GIST) that cannot be surgically removed and no longer respond to imatinib and sunitinib, two other drugs approved for treatment of GIST. Regorafenib, marketed under the trade name Stivarga®, was discovered and developed by Bayer Pharmaceuticals and marketed jointly with Onyx Pharmaceuticals. The active metabolites of the drug inhibit multiple targets within a variety of kinase families including those in the RET, VEGF, FGFR, PTK, and Abl pathways.

Side effects

Common side effects of regorafenib monohydrate include hand-foot skin reaction, diarrhea, nausea, vomiting, decreased appetite, fatigue, hypertension, and fever.

Synthesis

Among several published synthesis, the most likely process scale synthesis will be highlighted from the two published syntheses, and this is described in the scheme. Commercially available picolinic acid (148) was heated with thionyl chloride to provide the crude intermediate 4-chloro-2- pyridyl acid chloride which was subsequently reacted with aqueous methyl amine in toluene to give 4- chloro-2-methylcarboxamide as its hydrochloride salt 149 in quantitative yield after treatment with acetyl chloride in toluene and ethanol. The hydrochloride salt was free based with sodium hydroxide and then immediately reacted with imine 150 (formed upon exposure to 4-amino-3-fluorophenol (153) in refluxing 3-methyl 2-butanone) in base to provide diaryl ether 151 in 84% yield. Reaction of amine 151 with the commercially available isocyanate 152 ultimately delivered regorafenib hydrate (XXIII) in 83% yield.

Synthesis_1019206-88-2

References

[1] crona dj, keisler md, walko cm.regorafenib: a novel multitargeted tyrosine kinase inhibitor for colorectal cancer and gastrointestinal stromal tumors.ann pharmacother. 2013 dec;47(12):1685-96.

Regorafenib monohydrate synthesis

755037-03-7
1019206-88-2
Synthesis of Regorafenib monohydrate from Regorafenib

Regorafenib monohydrate Preparation Products And Raw materials

Raw materials

Regorafenib

Preparation Products

Regorafenib monohydrate Suppliers

Global Suppliers ( 275)
Supplier Tel Email Country ProdList Advantage
Yangzhou QinYuan Pharmaceutical Co., Ltd. 0514-80939770 13773367191 yzqyyykj@163.com China 253 55
Beijing Sai Siyuan Biomedical Technology Co., Ltd. 010-87925700 13522399152 1664478984@qq.com China 11 58
Shandong Tianhong biology medicine co., ltd 0530-0530-7396636 15315308127 3519386@qq.com China 29 58
Suzhou Chuangdendrobium Biotechnology Co., LTD 15556222336 997669055@qq.com China 76 58
Zhengzhou Science Pharmaceutical Technology Co., Ltd 0371-65936683 19043967036 zzsciencepublic@zzscience.com China 102 58
Shanghai Hope Chem Co., Ltd.， +21-18501659228 18501659228 info@hope-chem.com China 538 55
Jiangsu Purun Biomedical Co., Ltd. 025-85607381 15366090669 dingyi@purejs.cn China 59 58
Shanghai Boyle Chemical Co., Ltd. sales@boylechem.com China 2915 55
Jinan Trio PharmaTech Co., Ltd. 0531-88811783 sales@trio-pharmatech.com China 1856 62
Shanghai Feibo Chemical Technology Co., Ltd 021-58955608,2250286 15921236618 blinkzeng@gmail.com China 522 62
Supplier Advantage
Yangzhou QinYuan Pharmaceutical Co., Ltd. 55
Beijing Sai Siyuan Biomedical Technology Co., Ltd. 58
Shandong Tianhong biology medicine co., ltd 58
Suzhou Chuangdendrobium Biotechnology Co., LTD 58
Zhengzhou Science Pharmaceutical Technology Co., Ltd 58
Shanghai Hope Chem Co., Ltd.， 55
Jiangsu Purun Biomedical Co., Ltd. 58
Shanghai Boyle Chemical Co., Ltd. 55
Jinan Trio PharmaTech Co., Ltd. 62
Shanghai Feibo Chemical Technology Co., Ltd 62

Related articles

View Latest Price from Regorafenib monohydrate manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Regorafenib Hydrate pictures 2026-09-18 Regorafenib Hydrate
1019206-88-2
 1g More Than 99% 100kg/Month BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.
Regorafenib Hydrate. pictures 2026-09-18 Regorafenib Hydrate.
1019206-88-2
 1g More Than 99% 100kg/Month BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.
4-[4-[[[[4-Chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-2-pyridinecarboxamide hydrate USP/EP/BP pictures 2026-08-20 4-[4-[[[[4-Chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-2-pyridinecarboxamide hydrate USP/EP/BP
1019206-88-2
 $1.10 1g 99.9% 100 Tons Min Dideu Industries Group Limited
  • Regorafenib Hydrate pictures
  • Regorafenib Hydrate
    1019206-88-2
  • $0.00
  • More Than 99%
  • BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.

Regorafenib monohydrate Spectrum

4-[4-[[[[4-Chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-2-pyridinecarboxamide hydrate(1019206-88-2)1HNMR

1019206-88-2 (Regorafenib monohydrate) Related Search:

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4-(4-Amino-3-fluorophenoxy)-N-methylpicolinamide 918504-65-1 1110813-31-4

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Regorafenib monohydrate Regorafenib (BAY 73-4506)Monohydrate BAY 73-4506 Monohydrate Regorafenib monohydrate 4-[4-[[[[4-Chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-2-pyridinecarboxamide hydrate 4-[4-({[4-Chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]-N-methyl-2-pyridinecarboxamide hydrate (1:1) Regorafenib monohydrate (BAY 73-4506) 4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]-3-fluorophenoxy]-N-methylpyridine-2-carboxamide,hydrate Regorafenib H2O 4-(4-(3-(4-chloro-3-(trifluoromethyl)phenyl)ureido)-3-fluorophenoxy)-N-methylpicolinamide hydrate Regorafenibhydrate USP/EP/BP 4-[4-[[[[4-Chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-2-pyridinecarboxamide hydrate USP/EP/BP 4-[4-[[[[4-Chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-2-pyridi Regfenib monohydrate Regorafenib (200 mg) 4-(4-(3-(4-chloro-3-(trifluoromethyl)phenyl)ureido)-3-fluorophenoxy)-N-methylpicolinamide hydrate , Regorafenib monohydrate Regfini hydrate Regorafenib monohydrate, 10 mM in DMSO Regorafenib monohydrate (BAY 73-4506 monohydrate) 2-Pyridinecarboxamide, 4-[4-[[[[4-chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-, hydrate (1:1) 4-[4-[[[[4-Chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-2-pyridinecarboxamide hydrate Regorafenib hydrate Refined Sunflower Oil 1019206-88-2 C21H17ClF4N4O4 C21H15ClF4N4O3H2O API