Drug Details

General Information of the Drug (ID: DR6220)
Name
S-farnesylthiosalicylic acid
Synonyms
Salirasib; 162520-00-5; Farnesylthiosalicylic acid; S-Farnesylthiosalicylic acid; Farnesyl Thiosalicylic Acid; UNII-MZH0OM550M; MZH0OM550M; CHEMBL23293; 2-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trienyl]sulfanylbenzoic acid; 2-((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trienylthio)benzoic acid; 2-[[(2E,6E)-3,7,11-Trimethyl-2,6,10-dodecatrien-1-yl]thio]benzoic Acid; Benzoic acid, 2-[[(2E,6E)-3,7,11-trimethyl-2,6,10-dodecatrien-1-yl]thio]-; 2-(((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)thio)benzoic acid; Salirasib [USAN:INN]; Farnesylthiosalicyclic acid; Salirasib; FTS; S-trans,trans-farnesylthiosalicylic acid; Salirasib (INN/USAN); Lopac-F-8175; Lopac0_000517; MLS006010835; GTPL6281; Salirasib, >=98% (HPLC); AMY39921; BCP27978; EX-A1170; ONO-7056; trans,trans-Farnesylthiobenzoic acid; ZINC1650377; 2030AH; BDBM50034278; KD-032; MFCD00467723; NSC685986; NSC755771; s7684; 2-(((2E,6E)-3,7,11-Trimethyl-2,6,10-dodecatrienyl)sulfanyl)benzoic acid; AKOS024458453; Benzoic acid, 2-(((2E,6E)-3,7,11-trimethyl-2,6,10-dodecatrienyl)thio)-; CCG-204607; CS-0681; DB12681; NSC-685986; NSC-755771; NCGC00015448-01; NCGC00015448-02; NCGC00015448-03; NCGC00015448-11; NCGC00093912-01; NCGC00093912-02; AS-73028; HY-14754; SMR004701762; EU-0100517; D08995; F 8175; W-5109; Farnesylthiosalicylic acid, >98% (HPLC), solid; SR-01000075885; J-009946; SR-01000075885-1; Q27088685; 2-[(3,7,11-Trimethyl-2,6,10-dodecatrienyl)thio]benzoic acid; 2-((2E,6E)-3,7,11-Trimethyl-dodeca-2,6,10-trienylsulfanyl)-benzoic acid; 2-{[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl]sulfanyl}benzoic acid; 166445-40-5
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Molecular Type
Small molecule
Disease Lung cancer [ICD-11: 2C25] Phase 2 [1]
Structure
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2D MOL

3D MOL

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Formula
C22H30O2S
PubChem CID
5469318
Canonical SMILES
CC(=CCCC(=CCCC(=CCSC1=CC=CC=C1C(=O)O)C)C)C
InChI
1S/C22H30O2S/c1-17(2)9-7-10-18(3)11-8-12-19(4)15-16-25-21-14-6-5-13-20(21)22(23)24/h5-6,9,11,13-15H,7-8,10,12,16H2,1-4H3,(H,23,24)/b18-11+,19-15+
InChIKey
WUILNKCFCLNXOK-CFBAGHHKSA-N
CAS Number
CAS 162520-00-5
TTD Drug ID
D00KTV
Combinatorial Therapeutic Effect(s) Validated Clinically or Experimentally
    α. A List of Natural Product(s) Able to Enhance the Efficacy of This Drug
          Vitamin D      Saccharomyces cerevisiae     Click to Show/Hide the Molecular Data of This NP
                 Achieving Therapeutic Synergy     Click to Show/Hide
                    Representative Experiment Reporting the Effect of This Combination [2]
                    Detail(s)  Combination Info  click to show the detail info of this combination
                    Molecule(s)
                    Regulation		 Down-regulation Expression CCND1  Molecule Info 
Pathway MAP
Down-regulation Expression TIMP1  Molecule Info 
Pathway MAP
                    In-vitro Model Primary hepatic stellate cells derived from rat's liver Healthy Rattus norvegicus
                    In-vivo Model Male Wistar rats (300-400 g) were used in this study.
                    Experimental
                    Result(s)		 The combined treatment may have a potential therapeutic value in the initiation of fibrotic process.
Target and Pathway
Target(s) GTPase NRas (NRAS)  Molecule Info  [3]
Serine/threonine-protein kinase mTOR (mTOR)  Molecule Info  [4]
KEGG Pathway ErbB signaling pathway Click to Show/Hide
2 HIF-1 signaling pathway
3 mTOR signaling pathway
4 PI3K-Akt signaling pathway
5 AMPK signaling pathway
6 Insulin signaling pathway
7 Thyroid hormone signaling pathway
8 Adipocytokine signaling pathway
9 Type II diabetes mellitus
10 Pathways in cancer
11 Proteoglycans in cancer
12 MicroRNAs in cancer
13 Glioma
14 Prostate cancer
15 Acute myeloid leukemia
16 Central carbon metabolism in cancer
17 Choline metabolism in cancer
Panther Pathway Hypoxia response via HIF activation Click to Show/Hide
2 Interleukin signaling pathway
Pathwhiz Pathway Intracellular Signalling Through Adenosine Receptor A2a and Adenosine Click to Show/Hide
2 Intracellular Signalling Through Adenosine Receptor A2b and Adenosine
3 Fc Epsilon Receptor I Signaling in Mast Cells
4 Insulin Signalling
5 Leucine Stimulation on Insulin Signaling
Pathway Interaction Database IL4-mediated signaling events Click to Show/Hide
2 Signaling events mediated by Hepatocyte Growth Factor Receptor (c-Met)
3 IL12-mediated signaling events
4 CDC42 signaling events
5 LKB1 signaling events
6 Regulation of Telomerase
7 mTOR signaling pathway
8 CXCR4-mediated signaling events
9 EGFR-dependent Endothelin signaling events
10 IL2 signaling events mediated by PI3K
11 IFN-gamma pathway
12 ErbB1 downstream signaling
13 ErbB2/ErbB3 signaling events
14 CXCR3-mediated signaling events
15 Class I PI3K signaling events mediated by Akt
Reactome SOS-mediated signalling Click to Show/Hide
2 Activation of RAS in B cells
3 Constitutive Signaling by Ligand-Responsive EGFR Cancer Variants
4 SHC1 events in ERBB2 signaling
5 SHC1 events in ERBB4 signaling
6 p38MAPK events
7 GRB2 events in EGFR signaling
8 SHC1 events in EGFR signaling
9 GRB2 events in ERBB2 signaling
10 Tie2 Signaling
11 EGFR Transactivation by Gastrin
12 DAP12 signaling
13 SHC-related events triggered by IGF1R
14 FCERI mediated MAPK activation
15 NCAM signaling for neurite out-growth
16 EPHB-mediated forward signaling
17 VEGFR2 mediated cell proliferation
18 CD209 (DC-SIGN) signaling
19 Constitutive Signaling by EGFRvIII
20 SHC-mediated cascade:FGFR1
21 FRS-mediated FGFR1 signaling
22 SHC-mediated cascade:FGFR2
23 FRS-mediated FGFR2 signaling
24 SHC-mediated cascade:FGFR3
25 FRS-mediated FGFR3 signaling
26 FRS-mediated FGFR4 signaling
27 SHC-mediated cascade:FGFR4
28 Regulation of RAS by GAPs
29 RAF activation
30 RAF/MAP kinase cascade
31 MAP2K and MAPK activation
32 Negative regulation of MAPK pathway
33 Insulin receptor signalling cascade
34 PIP3 activates AKT signaling
35 Macroautophagy
36 mTORC1-mediated signalling
37 HSF1-dependent transactivation
38 CD28 dependent PI3K/Akt signaling
39 VEGFR2 mediated vascular permeability
40 TP53 Regulates Metabolic Genes
41 Constitutive Signaling by AKT1 E17K in Cancer
WikiPathways Serotonin Receptor 2 and ELK-SRF/GATA4 signaling Click to Show/Hide
2 DNA Damage Response (only ATM dependent)
3 TCR Signaling Pathway
4 ErbB Signaling Pathway
5 Senescence and Autophagy in Cancer
6 TGF Beta Signaling Pathway
7 IL-2 Signaling Pathway
8 Insulin Signaling
9 EGF/EGFR Signaling Pathway
10 MAPK Cascade
11 p38 MAPK Signaling Pathway
12 G Protein Signaling Pathways
13 Signaling of Hepatocyte Growth Factor Receptor
14 Kit receptor signaling pathway
15 Extracellular vesicle-mediated signaling in recipient cells
16 IL-3 Signaling Pathway
17 Bladder Cancer
18 Signaling by ERBB4
19 Signaling by ERBB2
20 Fc epsilon receptor (FCERI) signaling
21 Neurotransmitter Receptor Binding And Downstream Transmission In The Postsynaptic Cell
22 Signaling by the B Cell Receptor (BCR)
23 RAF/MAP kinase cascade
24 Interleukin-2 signaling
25 Signaling by SCF-KIT
26 DAP12 interactions
27 Signaling by Type 1 Insulin-like Growth Factor 1 Receptor (IGF1R)
28 Gastrin-CREB signalling pathway via PKC and MAPK
29 Nanoparticle-mediated activation of receptor signaling
30 JAK/STAT
31 Aryl Hydrocarbon Receptor
32 PDGF Pathway
33 Alpha 6 Beta 4 signaling pathway
34 BDNF signaling pathway
35 Oncostatin M Signaling Pathway
36 Interleukin-11 Signaling Pathway
37 TNF alpha Signaling Pathway
38 B Cell Receptor Signaling Pathway
39 RalA downstream regulated genes
40 Prostate Cancer
41 Signaling Pathways in Glioblastoma
42 Leptin signaling pathway
43 TSH signaling pathway
44 Signaling by PDGF
45 Signaling by Insulin receptor
46 Signaling by FGFR
47 Signaling by EGFR
48 NGF signalling via TRKA from the plasma membrane
49 NCAM signaling for neurite out-growth
50 Integrin-mediated Cell Adhesion
51 Interleukin-3, 5 and GM-CSF signaling
52 Cell surface interactions at the vascular wall
53 Interferon type I signaling pathways
54 Wnt Signaling Pathway Netpath
55 Cardiac Hypertrophic Response
56 PIP3 activates AKT signaling
57 Polycystic Kidney Disease Pathway
58 TSLP Signaling Pathway
59 FSH signaling pathway
60 RANKL/RANK Signaling Pathway
61 SREBF and miR33 in cholesterol and lipid homeostasis
62 Integrated Breast Cancer Pathway
63 SREBP signalling
64 Costimulation by the CD28 family
65 Type II diabetes mellitus
66 MicroRNAs in cardiomyocyte hypertrophy
67 TOR Signaling
68 AMPK Signaling
References
Reference 1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6281).
Reference 2 Vitamin D and S-farnesylthiosalicylic acid have a synergistic effect on hepatic stellate cells proliferation. Dig Dis Sci. 2014 Oct;59(10):2462-9.
Reference 3 The Ras inhibitor farnesylthiosalicylic acid (Salirasib) disrupts the spatiotemporal localization of active Ras: a potential treatment for cancer. Methods Enzymol. 2008;439:467-89.
Reference 4 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2109).
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