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  2. Effects Info
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Drug Details
01. General Information
Name Sunitinib
PubChem CID 5329102
Molecular Weight 398.5g/mol
Synonyms

Sunitinib, 557795-19-4, Sutent, SU11248, SU-11248, sunitinibum, Su-011248, Sunitinib Base, 342641-94-5, (Z)-N-(2-(Diethylamino)ethyl)-5-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide, N-[2-(diethylamino)ethyl]-5-{[(3Z)-5-fluoro-2-oxo-2,3-dihydro-1H-indol-3-ylidene]methyl}-2,4-dimethyl-1H-pyrrole-3-carboxamide, Sunitinib (INN), Sunitinib [INN], NSC-750690, SU 11248, UNII-V99T50803M, CHEBI:38940, HSDB 7932, N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide, CHEMBL535, N-(2-(Diethylamino)ethyl)-5-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide, NSC-736511, V99T50803M, SU011248, NSC750690, Sunitinib, Free base, NSC 736511, NSC 750690, 1H-Pyrrole-3-carboxamide, N-(2-(diethylamino)ethyl)-5-((Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl)-2,4-dimethyl-, n-(2-(diethylamino)ethyl)-5-((z)-(5-fluoro-1,2-dihydro-2-oxo-3h-indol-3-ylidene)methyl)-2,4-dimethyl-1h-pyrrole-3-carboxamide, N-(2-(DIETHYLAMINO)ETHYL)-5-((Z)-(5-FLUORO-2-OXO-1,2-DIHYDRO-3H-INDOL-3-YLIDENE)METHYL)-2,4-DIMETHYL-1H-PYRROLE-3-CARBOXAMIDE, Sunitinib (free base), Sunitinib [INN:BAN], NCGC00164631-01, MFCD09260778, C22H27FN4O2, (Z)-Sunitinib, 1H-Pyrrole-3-carboxamide, N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-, 5-(5-fluoro-2-oxo-1,2-dihydro-indol-(3Z)-ylidenemethyl]-2,4-dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylamino-ethyl)-amide, 5-[5-fluoro-2-oxo-1,2-dihydro-indol-(3Z)-ylidenemethyl]-2,4-dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylamino-ethyl)-amide, Sutent (free base), KS-5022, SUNITINIB [MI], 1126641-10-8, SUNITINIB [VANDF], SCHEMBL8081, SUNITINIB [WHO-DD], SUNITINIB [EMA EPAR], BDBM4814, GTPL5713, Sutent, Sunitinib, SU11248, DTXCID9021134, CHEBI:91430, EX-A553, L01XE04, WINHZLLDWRZWRT-ATVHPVEESA-N, BCPP000057, K00588a, (E)-N-[2-(Diethylamono)ethyl]-5-[(5-fluoro-2-oxo-1,2-dihydro-3H-indole-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide, N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide, HY-10255A, NSC800937, s7781, AKOS015908193, AKOS025312424, CCG-268638, CS-1670, DB01268, NSC-800937, NCGC00164631-02, NCGC00164631-04, 5-(5-fluoro-2-oxo-1,2-dihydroindolylidenemethyl)-2,4-dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, BD164426, 1,2,4,5-tetramethylpyrrole-3-carboxamide, AM20090630, FT-0651493, FT-0659515, NS00004661, D08552, EN300-323230, AB01273976-01, AB01273976-02, AB01273976_04, A822143, A830806, Q417542, SR-00000000005, SR-00000000005-2, Q27163278, Z2568722545, 1H-Pyrrole-3-carboxamide,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-, 5-[5-fluoro-2-oxo-1,2-dihydro-indol-(3Z)-ylidenemethyl]-2,4-dimethyl-1H-pyrrole-3-carboxylic acid(2-diethylamino-ethyl)-amide, N-(2-(Diethylamino)ethyl)-5-((Z)-(5-fluoro-1 pound not2-dihydro-2-oxo-3H-indol-3-ylidene)methyl)-2 pound not4-dimethyl-1H-pyrrole-3-carboxamide, N-[2-(diethylamino)ethyl]-5-[(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide, N-[2-(diethylamino)ethyl]-5-[(5-fluoro-2-oxo-2,3-dihydro-1H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide, N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carbo

Drug Type Small molecule
Formula C₂₂H₂₇FN₄O₂
SMILES CCN(CC)CCNC(=O)C1=C(NC(=C1C)C=C2C3=C(C=CC(=C3)F)NC2=O)C
InChI 1S/C22H27FN4O2/c1-5-27(6-2)10-9-24-22(29)20-13(3)19(25-14(20)4)12-17-16-11-15(23)7-8-18(16)26-21(17)28/h7-8,11-12,25H,5-6,9-10H2,1-4H3,(H,24,29)(H,26,28)/b17-12-
InChIKey WINHZLLDWRZWRT-ATVHPVEESA-N
CAS Number 557795-19-4
ChEMBL ID CHEMBL535
ChEBI ID CHEBI:38940
TTD ID D0R0MW
Drug Bank ID DB01268
KEGG ID D08552
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 2D-img
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2D MOL 3D MOL
02. Combinatorial Therapeutic Effect(s)
Synergistic Effect
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Enhancing Drug Efficacy
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Combination Pair ID: 365
Pair Name Pterostilbene, Sunitinib
Partner Name Pterostilbene
Disease Info [ICD-11: 2B72] Gastric cancer Investigative
Biological Phenomena Induction-->Oxidative Stress
Gene Regulation Down-regulation Expression PDZD8 hsa118987
In Vitro Model TMK-1 Gastric adenocarcinoma Homo sapiens (Human) CVCL_4384
MKN74 Gastric tubular adenocarcinoma Homo sapiens (Human) CVCL_2791
In Vivo Model Subcutaneous tumor models were established by inoculating cancer cells (MKN74: 5×10⁶ per mouse, TMK-1: 1×107 per mouse) into the scapular subcutaneous tissues of nude mice on Day 0.
Result PDZD8 may be a newly discovered off-target for SUN, and that the combined use of PTE with SUN significantly promotes antitumor activity in gastric cancer cell lines. The combined use of SUN and PTE might be a new molecular-targeted therapy for gastric cancer.
Combination Pair ID: 883
Pair Name Gambogic Acid, Sunitinib
Partner Name Gambogic Acid
Disease Info [ICD-11: 2C90.0] Renal cell carcinoma Investigative
Biological Phenomena Inhibition-->Angiogenesis
Gene Regulation Down-regulation Expression BCL2 hsa596
Up-regulation Expression CDKN1A hsa1026
Down-regulation Expression VEGFA hsa7422
In Vitro Model 786-O Renal cell carcinoma Homo sapiens (Human) CVCL_1051
Caki-1 Clear cell renal cell carcinoma Homo sapiens (Human) CVCL_0234
In Vivo Model Caki-1 cells (2×10⁶) in 100 ul RPMI-1640 and 100 ul of matrigel were used to inject subcutaneously into each mouse (5-week-old male athymic BALB/c nu/nu mice).
Result Our results show that the joint use of GA and SU can provide greater antitumor efficacy compared to either drug alone and thus may offer a new treatment strategy for renal cell carcinoma.
Combination Pair ID: 47
Pair Name Dihydroberberine, Sunitinib
Partner Name Dihydroberberine
Disease Info [ICD-11: 2C25] Lung cancer Investigative
Biological Phenomena Induction-->Proliferation
Gene Regulation Up-regulation Expression CCNB1 hsa891
Up-regulation Expression CCND1 hsa595
Down-regulation Expression CCNE1 hsa898
Up-regulation Expression CDK1 hsa983
Down-regulation Expression COX2 hsa4513
Down-regulation Expression IKBKE hsa9641
Down-regulation Expression IL1B hsa3553
Down-regulation Phosphorylation MAPK14 hsa1432
Down-regulation Phosphorylation MAPK8 hsa5599
Down-regulation Phosphorylation NFKB1 hsa4790
In Vitro Model A-549 Lung adenocarcinoma Homo sapiens (Human) CVCL_0023
NCI-H460 Lung large cell carcinoma Homo sapiens (Human) CVCL_0459
NCI-H1299 Lung large cell carcinoma Homo sapiens (Human) CVCL_0060
In Vivo Model Four to six‐week‐old non‐obese diabetic severe combined immunodeficiency (NOD/SCID) mice were injected subcutaneously into the right flank with 4×10⁶ NCI‐H460 cells suspended in sterile physiological saline.
Result DCS induced the expression of cell cycle signal molecules that are known to be affected by JNK and p38. The change of cell cycle, in turn, led to down-regulation of JNK and p38, and further reduced IL-1 secretion. Collectively, these findings highlight potential molecular mechanisms of DCS chemotherapeutic activity and suggest that DCS is an efficacious strategy in NSCLC therapy.
03. Reference
No. Title Href
1 Sunitinib and Pterostilbene Combination Treatment Exerts Antitumor Effects in Gastric Cancer via Suppression of PDZD8. Int J Mol Sci. 2022 Apr 4;23(7):4002. doi: 10.3390/ijms23074002. Click
2 Targeting renal cell carcinoma with gambogic acid in combination with sunitinib in vitro and in vivo. Asian Pac J Cancer Prev. 2012;13(12):6463-8. doi: 10.7314/apjcp.2012.13.12.6463. Click
3 Dihydroberberine exhibits synergistic effects with sunitinib on NSCLC NCI-H460 cells by repressing MAP kinase pathways and inflammatory mediators. J Cell Mol Med. 2017 Oct;21(10):2573-2585. doi: 10.1111/jcmm.13178. Click
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