InterPAD - DETAILS

Regorafenib, 755037-03-7, BAY 73-4506, Stivarga, 4-(4-(3-(4-Chloro-3-(trifluoromethyl)phenyl)ureido)-3-fluorophenoxy)-N-methylpicolinamide, Regorafenibum, BAY73-4506, Regorafenib (BAY 73-4506), BAY-73-4506, 4-[4-({[4-Chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide, UNII-24T2A1DOYB, REGORAFENIB ANHYDROUS, 24T2A1DOYB, CHEBI:68647, Bay-734506, 4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]-3-fluorophenoxy]-N-methylpyridine-2-carboxamide, CHEMBL1946170, DTXSID60226441, 4-(4-(((4-chloro-3-(trifluoromethyl)phenyl)carbamoyl)amino)-3-fluorophenoxy)-n-methylpyridine-2-carboxamide, Regorafenib-13C-d3, Stivarga (TN), 2-Pyridinecarboxamide,4-[4-[[[[4-chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-, UNII-MGN125FS9D, REGORAFENIB (USP-RS), CHEBI:68646, DTXSID70144349, REGORAFENIB (USP MONOGRAPH), Regorafenib [INN], 835621-08-4, Regorafenib [USAN:INN], C21H15ClF4N4O3, 4-(4-(((4-chloro-3-(trifluoromethyl)phenyl)carbamoyl}amino)-3-fluorophenoxy)-N-methylpyridine-2-carboxamide, REGORAFENIB [MI], Regorafenib (USAN/INN), REGORAFENIB [VANDF], BAY73-4506 hydrochloride, REGORAFENIB [WHO-DD], MLS006010303, Regorafenib crystalline form I, SCHEMBL432230, Regorafenib,BAY 73-4506, GTPL5891, DTXCID8066840, DTXCID60148932, EX-A058, L01XE21, BCPP000352, HMS3654K16, HMS3672E15, 755037-03-7 , Regorafenib, BCP02105, BKD17855, BDBM50363397, MFCD16038047, NSC763932, NSC800865, s1178, AKOS015951107, AM81251, BCP9000384, CCG-269571, CS-0170, DB08896, NSC-763932, NSC-800865, SB16819, NCGC00263138-01, NCGC00263138-13, NCGC00263138-19, 4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]-3-fluoro-phenoxy]-N-methyl-pyridine-2-carboxamide, AC-25075, AC-31116, AS-16304, HY-10331, SMR004701370, FT-0674338, NS00040710, R0142, SW218097-2, BAY 73-4506 , Fluoro-Sorafenib, cas:835621-07-3;Regorafenib hydrochloride, Regorafenib (BAY73-4506,Fluoro-Sorafenib), A25020, D10138, Regorafenib (BAY73-4506,Fluoro-Sorafenib)?, AB01565826_02, SR-01000941571, Q3891664, SR-01000941571-1, BRD-K16730910-001-02-4, Z2235801830, 755037-03-7 (anhydrous); 1019206-88-2 (hydrate), 2-Pyridinecarboxamide, 4-[4-[[[[4-chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-, 4-[4-({[4-Chloro-3-(trifluoromethy)phenyl]carbamoyl}amino)-3-fluorophenoxy]-1-methylpyridine-2-carboxamide, 4{4-[3-(4-chloro-3-trifluoromethylphenyl)-ureido]-3-fluorophenoxy}-pyridine-2-carboxylic acid methylamide, Regorafenib;1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(2-fluoro-4-(2-(methylcarbamoyl)pyridin-4-yloxy)phenyl)urea

No.	Title	Href
1	Regorafenib in combination with silybin as a novel potential strategy for the treatment of metastatic colorectal cancer. Oncotarget. 2017 Aug 7;8(40):68305-68316. doi: 10.18632/oncotarget.20054.	`Click`
2	Synergistic effect of toosendanin and regorafenib against cell proliferation and migration by regulating WWOX signaling pathway in hepatocellular carcinoma. Phytother Res. 2021 Aug;35(8):4567-4578. doi: 10.1002/ptr.7174.	`Click`
3	Regorafenib and ginsenoside combination therapy: inhibition of HepG2 cell growth through modulating survivin and caspase-3 gene expression. Clin Transl Oncol. 2020 Sep;22(9):1491-1498. doi: 10.1007/s12094-019-02283-9.	`Click`
4	Chlorogenic Acid Improves the Regorafenib Effects in Human Hepatocellular Carcinoma Cells. Int J Mol Sci. 2018 May 19;19(5):1518. doi: 10.3390/ijms19051518.	`Click`

No.

Title

Href

Regorafenib in combination with silybin as a novel potential strategy for the treatment of metastatic colorectal cancer. Oncotarget. 2017 Aug 7;8(40):68305-68316. doi: 10.18632/oncotarget.20054.

Click

Synergistic effect of toosendanin and regorafenib against cell proliferation and migration by regulating WWOX signaling pathway in hepatocellular carcinoma. Phytother Res. 2021 Aug;35(8):4567-4578. doi: 10.1002/ptr.7174.

Click

Regorafenib and ginsenoside combination therapy: inhibition of HepG2 cell growth through modulating survivin and caspase-3 gene expression. Clin Transl Oncol. 2020 Sep;22(9):1491-1498. doi: 10.1007/s12094-019-02283-9.

Click

Chlorogenic Acid Improves the Regorafenib Effects in Human Hepatocellular Carcinoma Cells. Int J Mol Sci. 2018 May 19;19(5):1518. doi: 10.3390/ijms19051518.

Click

Name	Regorafenib
PubChem CID	11167602
Molecular Weight	482.8g/mol
Synonyms	Regorafenib, 755037-03-7, BAY 73-4506, Stivarga, 4-(4-(3-(4-Chloro-3-(trifluoromethyl)phenyl)ureido)-3-fluorophenoxy)-N-methylpicolinamide, Regorafenibum, BAY73-4506, Regorafenib (BAY 73-4506), BAY-73-4506, 4-[4-({[4-Chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide, UNII-24T2A1DOYB, REGORAFENIB ANHYDROUS, 24T2A1DOYB, CHEBI:68647, Bay-734506, 4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]-3-fluorophenoxy]-N-methylpyridine-2-carboxamide, CHEMBL1946170, DTXSID60226441, 4-(4-(((4-chloro-3-(trifluoromethyl)phenyl)carbamoyl)amino)-3-fluorophenoxy)-n-methylpyridine-2-carboxamide, Regorafenib-13C-d3, Stivarga (TN), 2-Pyridinecarboxamide,4-[4-[[[[4-chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-, UNII-MGN125FS9D, REGORAFENIB (USP-RS), CHEBI:68646, DTXSID70144349, REGORAFENIB (USP MONOGRAPH), Regorafenib [INN], 835621-08-4, Regorafenib [USAN:INN], C21H15ClF4N4O3, 4-(4-(((4-chloro-3-(trifluoromethyl)phenyl)carbamoyl}amino)-3-fluorophenoxy)-N-methylpyridine-2-carboxamide, REGORAFENIB [MI], Regorafenib (USAN/INN), REGORAFENIB [VANDF], BAY73-4506 hydrochloride, REGORAFENIB [WHO-DD], MLS006010303, Regorafenib crystalline form I, SCHEMBL432230, Regorafenib,BAY 73-4506, GTPL5891, DTXCID8066840, DTXCID60148932, EX-A058, L01XE21, BCPP000352, HMS3654K16, HMS3672E15, 755037-03-7 , Regorafenib, BCP02105, BKD17855, BDBM50363397, MFCD16038047, NSC763932, NSC800865, s1178, AKOS015951107, AM81251, BCP9000384, CCG-269571, CS-0170, DB08896, NSC-763932, NSC-800865, SB16819, NCGC00263138-01, NCGC00263138-13, NCGC00263138-19, 4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]-3-fluoro-phenoxy]-N-methyl-pyridine-2-carboxamide, AC-25075, AC-31116, AS-16304, HY-10331, SMR004701370, FT-0674338, NS00040710, R0142, SW218097-2, BAY 73-4506 , Fluoro-Sorafenib, cas:835621-07-3;Regorafenib hydrochloride, Regorafenib (BAY73-4506,Fluoro-Sorafenib), A25020, D10138, Regorafenib (BAY73-4506,Fluoro-Sorafenib)?, AB01565826_02, SR-01000941571, Q3891664, SR-01000941571-1, BRD-K16730910-001-02-4, Z2235801830, 755037-03-7 (anhydrous); 1019206-88-2 (hydrate), 2-Pyridinecarboxamide, 4-[4-[[[[4-chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-, 4-[4-({[4-Chloro-3-(trifluoromethy)phenyl]carbamoyl}amino)-3-fluorophenoxy]-1-methylpyridine-2-carboxamide, 4{4-[3-(4-chloro-3-trifluoromethylphenyl)-ureido]-3-fluorophenoxy}-pyridine-2-carboxylic acid methylamide, Regorafenib;1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(2-fluoro-4-(2-(methylcarbamoyl)pyridin-4-yloxy)phenyl)urea
Drug Type	Small molecule
Formula	C₂₁H₁₅ClF₄N₄O₃
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
InChI	1S/C21H15ClF4N4O3/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)
InChIKey	FNHKPVJBJVTLMP-UHFFFAOYSA-N
CAS Number	755037-03-7
ChEMBL ID	CHEMBL1946170
ChEBI ID	CHEBI:68647
TTD ID	D09GDD
Drug Bank ID	DB08896
KEGG ID	D10138
Toxicity	Organism	Test Type	Route(Dose)
	rat	LD50	intraperitoneal(165 mg/kg)
	mouse	LD50	intraperitoneal(254 mg/kg)
	rat	LD50	oral(322 mg/kg)
Structure			Download 2D MOL 3D MOL

Pair Name	Toosendanin, Regorafenib
Partner Name	Toosendanin
Disease Info	[ICD-11: 2C12]	Hepatocellular carcinoma		Investigative
Biological Phenomena	Inhibition-->Cell metastasis
Gene Regulation	Down-regulation	Expression	DVL2	hsa1856
	Up-regulation	Phosphorylation	GSK3B	hsa2932
	Down-regulation	Expression	MMP2	hsa4313
	Down-regulation	Expression	MMP9	hsa4318
	Down-regulation	Expression	MYC	hsa4609
	Down-regulation	Phosphorylation	STAT3	hsa6774
	Up-regulation	Expression	WWOX	hsa51741
In Vitro Model	MHCC97-L	Adult hepatocellular carcinoma	Homo sapiens (Human)	CVCL_4973
Result	TSN and RGF combination (TRC) synergistically inhibited the proliferation and migration of MHCC-97L cells. The upregulation of WWOX (WW-domain containing oxidoreductase) played a vital role in the HCC cell growth treated with TRC

Pair Name	Ginsenoside, Regorafenib
Partner Name	Ginsenoside
Disease Info	[ICD-11: 2C12]	Hepatocellular carcinoma		Investigative
Biological Phenomena	Induction-->Apoptosis
Gene Regulation	Down-regulation	Expression	BIRC5	hsa332
Gene Regulation	Up-regulation	Expression	CASP3	hsa836
In Vitro Model	Hep-G2	Hepatoblastoma	Homo sapiens (Human)	CVCL_0027
Result	The findings in this study offered a theoretical insight into clinical use of regorafenib and ginsenoside for treatment of liver cancer.

Pair Name	Chlorogenic acid, Regorafenib
Partner Name	Chlorogenic acid
Disease Info	[ICD-11: 2C12]	Hepatocellular carcinoma		Investigative
Biological Phenomena	Induction-->Apoptosis
Gene Regulation	Up-regulation	Expression	BAX	hsa581
	Down-regulation	Expression	BCL2	hsa596
	Down-regulation	Expression	BCL-xL	hsa598
	Up-regulation	Expression	CASP7	hsa840
In Vitro Model	PLC/PRF/5	Adult hepatocellular carcinoma	Homo sapiens (Human)	CVCL_0485
In Vitro Model	Hep-G2	Hepatoblastoma	Homo sapiens (Human)	CVCL_0027
Result	This drug combination could be considered as a safe and more effective approach in HCC therapy.

Pair Name	Silibinin, Regorafenib
Partner Name	Silibinin
Disease Info	[ICD-11: 2B91]	Colorectal cancer		Investigative
Biological Phenomena	Induction-->ROS generation
Gene Regulation	Down-regulation	Expression	AKT1	hsa207
	Down-regulation	Expression	MTOR	hsa2475
	Down-regulation	Expression	PIK3CA	hsa5290
In Vitro Model	SW48	Colon adenocarcinoma	Homo sapiens (Human)	CVCL_1724
	HCT 15	Colon adenocarcinoma	Homo sapiens (Human)	CVCL_0292
	SW480	Colon adenocarcinoma	Homo sapiens (Human)	CVCL_0546
Result	The present study suggests that silybin in combination with regorafenib is a promising strategy for treatment of metastatic colorectal patients.