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Regorafenib (Hydrochloride)

Regorafenib (Hydrochloride) Structure
Regorafenib (Hydrochloride) structure
CAS No.
835621-07-3
Chemical Name:
Regorafenib (Hydrochloride)
Synonyms
Regofini;Regafenib HCL;Regorafenib HC;Regorafenib HCl;Regafenib hydrochloride;BAY73-4506 hydrochloride;egorafenib (Hydrochloride);5-Diiodotyrosine Dihydrate;Regorafenib (Hydrochloride);Regorafenib HCl (BAY-73-4506)
CBNumber:
CB52624290
Molecular Formula:
C21H16Cl2F4N4O3
Molecular Weight:
519.2763528
MDL Number:
MFCD22417053
MOL File:
835621-07-3.mol
MSDS File:
SDS
Last updated:2025-07-29 17:31:50
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Regorafenib (Hydrochloride) Properties

storage temp. Store at -20°C
solubility ≥ 25.95 mg/mL in DMSO, ≥ 8.75 mg/mL in EtOH with ultrasonic and warming
form Powder
color White to off-white
InChIKey ACSWJKPZXNIVMY-UHFFFAOYSA-N
SMILES C1(C(NC)=O)=NC=CC(OC2=CC=C(NC(NC3=CC=C(Cl)C(C(F)(F)F)=C3)=O)C(F)=C2)=C1.[H]Cl

Regorafenib (Hydrochloride) price

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
ChemScene CS-0725 Regorafenib(Hydrochloride) 99.58% 835621-07-3 50mg $50 2021-12-16 Buy
ApexBio Technology A3750 Regorafenibhydrochloride 835621-07-3 10mg $65 2021-12-16 Buy
ChemScene CS-0725 Regorafenib(Hydrochloride) 99.58% 835621-07-3 100mg $80 2021-12-16 Buy
American Custom Chemicals Corporation KIN0001550 REGORAFENIB HYDROCHLORIDE 95.00% 835621-07-3 5MG $154 2021-12-16 Buy
AK Scientific 4001AH Regorafenibhydrochloride 835621-07-3 5mg $186 2021-12-16 Buy
Product number Packaging Price Buy
CS-0725 50mg $50 Buy
A3750 10mg $65 Buy
CS-0725 100mg $80 Buy
KIN0001550 5MG $154 Buy
4001AH 5mg $186 Buy

Regorafenib (Hydrochloride) Chemical Properties,Uses,Production

Uses

BAY 73-4506 (Regorafenib) is a multikinase inhibitor with IC50 of 17, 40 and 69 nM c-KIT, VEGFR2, B-Raf.

Synthesis

Regorafenib

755037-03-7

Regorafenib (Hydrochloride)

835621-07-3

GENERAL STEPS: 4-(4-(3-(4-chloro-3-(trifluoromethyl)phenyl)ureido)-3-fluorophenoxy)-N-methylpyridine amide (free base, 2.0 g) was dissolved in anhydrous tetrahydrofuran (15 mL) and 4M HCl/dioxane solution was slowly added (to excess). Upon completion of the reaction, the mixed solution was concentrated under reduced pressure to give 2.32 g of off-white solid. The resulting crude product was dissolved in preheated ethanol (125 mL), appropriate amount of activated carbon was added and heated to reflux for 15 minutes. Subsequently, the hot suspension was filtered through a diatomaceous earth pad (model 521) and cooled to room temperature. The filtrate was placed in a refrigerator overnight to promote crystallization. On the following day, the crystallized product was collected by diafiltration, washed sequentially with cold ethanol and hexane, and air-dried. The mother liquor was further concentrated and the above crystallization process was repeated (overnight in a refrigerator) to collect the second batch of crystalline product and combined with the first batch. Finally, the resulting colorless hydrochloride product was dried in a vacuum oven at 60°C for two days to give a final product of 1.72 g (79% yield). Melting point: 215°C. Elemental analysis (calculated/measured): C 48.57/48.68, H 3.11/2.76, N 10.79/10.60, Cl 13.65/13.63, F 14.63/14.88.

in vitro

Regorafenib potently inhibits VEGFR2 autophosphorylation in NIH-3T3/VEGFR2 cells with an IC50 of 3 nM. In HAoSMCs, regorafenib inhibits PDGFR-β autophosphorylation after stimulation with PDGF-BB, with an IC50 of 90 nM. Regorafenib inhibits the proliferation of VEGF165-stimulated HUVECs, with an IC50 of 3 nMf. Regorafenib causes a concentration-dependent decrease in Hep3B cell growth, having an IC50 of 5 μM. Regorafenib subsequently increases the levels of phospho-c-Jun, a JNK target, but not total c-Jun in Hep3B cells.

in vivo

Regorafenib effectively inhibits growth of the Colo-205 xenografts in the dose range of 10-100 mg/kg reaching a TGI of 75% at day 14 at the 10 mg/kg dose. In the MDA-MB-231 model, regorafenib is highly efficacious at a dose as low as 3 mg/kg, resulting in a significant TGI of 81%, which increases to 93% at doses of 10 and 30 mg/kg, where tumor stasis is reached.

IC 50

VEGFR1: 13 nM (IC50); VEGFR2: 4.2 nM (IC50); VEGFR3: 46 nM (IC50); PDGFRβ: 22 nM (IC50); Braf: 28 nM (IC50); BRafV600E: 19 nM (IC50); Raf-1: 2.5 nM (IC50)

References

[1] Phan, Chiuyen et al. “Isomorphous Crystals Formed by the Similar Supramolecular Motifs in Sorafenib Hydrochloride and Regorafenib Hydrochloride Salts.” 2019. 0.

Regorafenib (Hydrochloride) Preparation Products And Raw materials

Raw materials

Regorafenib Tetrahydrofuran 1,3-DIOXANE Hydrochloric acid

Preparation Products

Regorafenib (Hydrochloride) Suppliers

Global( 139)Suppliers
Supplier Tel Email Country ProdList Advantage
Yangzhou Qinyuan Pharmatech Co.,ltd
+86-18752526868 +86-18752526868 jennysun@yzqyyykj.com China 83 58
Hebei Yanxi Chemical Co., Ltd. 		+8618531123677 faithe@yan-xi.com China 5853 58
Henan Bao Enluo International TradeCo.，LTD 		+86-17331933971 deasea125996@gmail.com China 2472 58
Capot Chemical Co.,Ltd. 		+8613336195806 sales@capot.com China 29731 60
Beijing Cooperate Pharmaceutical Co.,Ltd 		010-60279497 sales01@cooperate-pharm.com CHINA 1803 55
Nanjing Finetech Chemical Co., Ltd. 		025-85710122 17714198479 sales@fine-chemtech.com CHINA 885 55
ATK CHEMICAL COMPANY LIMITED 		+undefined-21-51877795 ivan@atkchemical.com China 33024 60
career henan chemical co 		+86-0371-86658258 +8613203830695 sales@coreychem.com China 29855 58
Zhejiang ZETian Fine Chemicals Co. LTD 		+8618957127338 stella@zetchem.com China 2136 58
SHANDONG ZHI SHANG CHEMICAL CO.LTD 		+86 18953170293 sales@sdzschem.com China 2930 58
Supplier Advantage
Yangzhou Qinyuan Pharmatech Co.,ltd
58
Hebei Yanxi Chemical Co., Ltd. 		58
Henan Bao Enluo International TradeCo.，LTD 		58
Capot Chemical Co.,Ltd. 		60
Beijing Cooperate Pharmaceutical Co.,Ltd 		55
Nanjing Finetech Chemical Co., Ltd. 		55
ATK CHEMICAL COMPANY LIMITED 		60
career henan chemical co 		58
Zhejiang ZETian Fine Chemicals Co. LTD 		58
SHANDONG ZHI SHANG CHEMICAL CO.LTD 		58

View Lastest Price from Regorafenib (Hydrochloride) manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Regorafenib (Hydrochloride) pictures 2025-06-20 Regorafenib (Hydrochloride)
835621-07-3
 US $0.00 / kg 1kg 0.99 20tons Hebei Yanxi Chemical Co., Ltd.
Regorafenib (Hydrochloride) pictures 2024-10-31 Regorafenib (Hydrochloride)
835621-07-3
 US $0.00 / g 10g 99% 10tons Yangzhou Qinyuan Pharmatech Co.,ltd
Regorafenib (Hydrochloride) pictures 2023-07-26 Regorafenib (Hydrochloride)
835621-07-3
 US $50.00 / kg 1kg 99.9% 10000MT Henan Bao Enluo International TradeCo.，LTD

Regorafenib (Hydrochloride) Spectrum

Regorafenib (Hydrochloride)(835621-07-3)1HNMR

835621-07-3(Regorafenib (Hydrochloride))Related Search:

4-(4-(3-(4-chloro-3-(trifluoroMethyl)phenyl)ureido)-3-fluorophenoxy)-2-(MethylcarbaMoyl)pyridine 1-oxide (S,S')-3-METHYL-1-(2-PIPERIDINOPHENYL)BUTYLAMINE, N-ACETYL-GLUTAMATE SALT 4-[4-[[[[4-Chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-2-pyridinecarboxamide hydrate Regorafenib Bortezomib
Abiraterone

1of2

BAY73-4506 hydrochloride 4-[4-[[[[4-Chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-2-pyridinecarboxamide hydrochloride Regafenib HCL Regafenib hydrochloride 2-Pyridinecarboxamide,4-[4-[[[[4-chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-, monohydrochloride 4-[4-({[4-Chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]-N-methyl-2-pyridinecarboxamide hydrochloride (1:1) 4-(4-(3-(4-Chloro-3-(trifluoromethyl)phenyl)ureido)-3-fluorophenoxy)-N-methylpicolinamide hydr Regorafenib (Hydrochloride) 5-Diiodotyrosine Dihydrate egorafenib (Hydrochloride) Regorafenib HCl (BAY-73-4506) Powder Regorafenib Hydrochloride CAS Regorafenib Hydrochloride/BAY73-4506 hydrochloride Regorafenib HC 4-[4-[[4-Chloro-3-(trifluoromethyl)phenyl]carbamoylamino]-3-fluorophenoxy]-N-methylpyridine-2-carboxamide hydrochloride Regorafenib HCl Regofini 2-Pyridinecarboxamide, 4-[4-[[[[4-chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-, hydrochloride (1:1) 4-[4-[[[[4-chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-2-Pyridinecarboxamide hydrochloride (1:1) 4-4-4-Chloro-3-(trifluoromethyl)phenylaminocarbonylamino-3-fluorophenoxy-N-methylpyridin-2-carboxamide HCl 4-(4-(3-(4-Chloro-3-(trifluoromethyl)phenyl)ureido)-3-fluorophenoxy)-N-methylpicolinamide hydrochloride Regorafenib Hydrochloride, 10 mM in DMSO 835621-07-3 C21H15ClF4N4O3HCl C21H16Cl2F4N4O3 C21H15ClF4N4O3ClH