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Regorafenib

Small Molecule Inhibitor FDA Approve
Regorafenib
Regorafenib structure
CAS No.
755037-03-7
Chemical Name:
Regorafenib
Synonyms
Regafenib;regorafinib;BAY 73-4506;Regorafenib;842-2937WAYNE;Regorafenib(W.S);Reggae sorafenib;Fluoro-Sorafenib;Regorafenib, >=98%;Regorafenib C3X-1410
CBNumber:
CB32498792
Molecular Formula:
C21H15ClF4N4O3
Formula Weight:
482.8154128
MOL File:
755037-03-7.mol

Regorafenib Properties

Melting point:
206.0 to 210.0 °C
Boiling point:
513.4±50.0 °C(Predicted)
Density 
1.491±0.06 g/cm3(Predicted)
form 
White powder.
pka
12.04±0.70(Predicted)
CAS DataBase Reference
755037-03-7
FDA UNII
24T2A1DOYB
NCI Dictionary of Cancer Terms
regorafenib
SAFETY
  • Risk and Safety Statements
HS Code  29242990

Regorafenib price More Price(6)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
TCI Chemical R0142 Regorafenib >98.0%(HPLC) 755037-03-7 25mg $102 2020-06-24 Buy
TCI Chemical R0142 Regorafenib >98.0%(HPLC) 755037-03-7 100mg $277 2020-06-24 Buy
Cayman Chemical 18498 Regorafenib ≥98% 755037-03-7 10mg $105 2020-06-24 Buy
Cayman Chemical 18498 Regorafenib ≥98% 755037-03-7 5mg $55 2020-06-24 Buy
Cayman Chemical 18498 Regorafenib ≥98% 755037-03-7 25mg $234 2020-06-24 Buy

Regorafenib Chemical Properties,Uses,Production

Small Molecule Inhibitor

Regorafenib (BAY 73-4506, Stivarga ) is a new oral small molecule multi-kinases inhibitor. It can inhibit the target kinases associated with angiogenesis and tumorigenesis. The pathway influenced by regorafenib and the biomarkers for monitoring the efficacy of regorafenib become hot spots. Because of its wide spectrum kinase inhibitory activity, the utilization of regorafenib in many clinical indications are also carried out extensively. Since regorafenib is approved with the box warning, its side effects can not be ignored.

FDA Approve

Regorafenib (BAY73-4506) is a new type of multikinase inhibitor developed by Bayer, and is the first small molecule kinase inhibitor approved by the U.S. FDA on September 27, 2012 used for fast track colorectal cancer that develops and metastases after conventional treatment. 
Regorafenib achieves good results in some patients with rectal cancer that are resistant to traditional chemotherapy, but not all rectal cancers are sensitive to it. Therefore, the pathway influenced by regorafenib and the biomarkers for monitoring the efficacy of regorafenib become hot spots.

Description

In September 2012, theUSFDAapproved regorafenib for the treatment of patients with metastatic colorectal cancer (CRC), especially those for whom standard therapies have failed, including fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy, an anti-VEGF therapy, and, if KRAS wild type, ananti-EGFRtherapy. Regorafenib is a multikinase inhibitor with potent inhibitory activity versus VEGFRs and PDFRs. Both of these classes of receptors are expressed on tumor cells and affect proliferation and angiogenesis. Regorafenib inhibited growth in murine xenograft models for colon, breast, renal, lung, melanoma, pancreatic, and ovarian tumors when dosed at 10–30 mg/kg. Regorafenib is a fluorinated analog of sorafenib, a multikinase inhibitor co-marketed by Bayer and Onyx for the treatment of kidney and liver cancer. The synthesis of regorafenib is accomplished in two steps from commercially available starting materials. 4-Aminophenol is coupled to 4-chloro-N-methyl- 2-pyridinecarboxamide to give 4-(2-(N-methylcarbamoyl)-4-pyridyloxy)aniline. Subsequent treatment with 4-chloro-3-(trifluoromethyl)phenyl isocycanate affords the urea, regorafenib.

Originator

Bayer (Germany)

Uses

It inhibits PDGFR tyrosine kinase with IC50=83nM. It is useful for the treatment of inflammation and as an anti-proliferative agent.

Uses

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

Uses

Regorafenib (BAY 73-4506) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively

Definition

ChEBI: A pyridinecarboxamide obtained by condensation of 4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]pyridine-2-carboxylic acid with methylamine. Used for for the treatment of metastatic colorectal cancer in patients who have previ usly received chemotherapy, anti-EGFR or anti-VEGF therapy.

brand name

Stivarga

Regorafenib Preparation Products And Raw materials

Raw materials

Preparation Products


Regorafenib Suppliers

Global( 302)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Beijing Cooperate Pharmaceutical Co.,Ltd.
+86-10-60279497 +86(0)15646567669
+86-10-60279497 sales01@cooperate-pharm.com CHINA 1817 55
Jurong Coupling Biotechnology Co., Ltd.
13656108824
coupling278191416@hotmail.com CHINA 184 58
Capot Chemical Co.,Ltd.
+86-571-85586718
+86-571-85864795 sales@capotchem.com China 19929 60
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
info@dakenchem.com CHINA 21821 58
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 22626 55
Hangzhou FandaChem Co.,Ltd.
0086 158 5814 5714 (Mobile
+86-571-56059825 fandachem@gmail.com CHINA 3248 55
Nanjing Finetech Chemical Co., Ltd.
025-85710122 17714198479
025-85710122 sales@fine-chemtech.com CHINA 890 55
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 24723 60
Anqing Chico Pharmaceutical Co., Ltd.
15380796838
chloewu@chicopharm.cn CHINA 341 58
Lianyungang happen teng technology co., LTD
15950718863
wang666xt@163.com CHINA 296 58

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View Lastest Price from Regorafenib manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2018-09-27 China Hot sale Regorafenib with best price and high quality CAS NO.755037-03-7
755037-03-7
US $1.00 / G 100G 99.9% 50000 tons Hebei Ruishun Trade Co.,Ltd
2019-12-25 Regorafenib
755037-03-7
US $4656.00 / KG 1KG 99.0% 1000 tons Shaanxi Dideu Medichem Co. Ltd
2019-08-27 Regorafenib/BAY 73-4506
755037-03-7
US $0.00-0.00 / g 1g 99.0% 200kg/month Beijing Yibai Biotechnology Co., Ltd

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