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Chemical Structure| 162520-00-5 Chemical Structure| 162520-00-5

Structure of Salirasib
CAS No.: 162520-00-5

Chemical Structure| 162520-00-5

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Salirasib is an inhibitor of prenylated protein methyltransferase (PPMTase) with Ki of 2.6 μM and can inhibit the methylation of Ras.

Synonyms: S-Farnesylthiosalicylic acid; Farnesyl Thiosalicylic Acid; FTS

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Product Details of Salirasib

CAS No. :162520-00-5
Formula : C22H30O2S
M.W : 358.54
SMILES Code : O=C(O)C1=CC=CC=C1SC/C=C(C)/CC/C=C(C)/CC/C=C(C)/C
Synonyms :
S-Farnesylthiosalicylic acid; Farnesyl Thiosalicylic Acid; FTS
MDL No. :MFCD00467723
InChI Key :WUILNKCFCLNXOK-CFBAGHHKSA-N
Pubchem ID :5469318

Safety of Salirasib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
4T1-luc2 0, 2, 4, 6, 8, 10, 25, 50, 70 µM 48 h Evaluate the anti-proliferative effect of FTS-IR783 on 4T1-luc2 cells, results showed that FTS-IR783 is more effective than FTS. Acta Pharmacol Sin. 2022 Jul;43(7):1843-1856.
MDA-MB-231 0, 2, 4, 6, 8, 10, 25, 50, 70 µM 48 h Evaluate the anti-proliferative effect of FTS-IR783 on MDA-MB-231 cells, results showed that FTS-IR783 is more effective than FTS. Acta Pharmacol Sin. 2022 Jul;43(7):1843-1856.
Panc-1 cells 50 µM 24 h To evaluate the inhibitory effect of Salirasib on the invasion of Panc-1 cells, the results showed that FTS inhibited the invasion of Panc-1 cells, but its efficacy was lower than that of 15 mM rasfonin. Cell Death Dis. 2014 May 22;5(5):e1241.
Panc-1 cells 50 µM 24 h To evaluate the inhibitory effect of Salirasib on the migration of Panc-1 cells, the results showed that FTS significantly reduced the migratory activity of Panc-1 cells. Cell Death Dis. 2014 May 22;5(5):e1241.
Panc-1 cells 50 µM 24 h To evaluate the inhibitory effect of Salirasib on the proliferation of Panc-1 cells, the results showed that FTS inhibited the proliferation of Panc-1 cells slightly more strongly than rasfonin during the first 24 h. Cell Death Dis. 2014 May 22;5(5):e1241.
Hep3B 150 μM 24 h Salirasib induced a time and dose dependent growth inhibition through inhibition of proliferation and partially through induction of apoptosis Mol Cancer. 2010 Sep 22;9:256.
Huh7 150 μM 24 h Salirasib induced a time and dose dependent growth inhibition through inhibition of proliferation and partially through induction of apoptosis Mol Cancer. 2010 Sep 22;9:256.
HepG2 150 μM 24 h Salirasib induced a time and dose dependent growth inhibition through inhibition of proliferation and partially through induction of apoptosis Mol Cancer. 2010 Sep 22;9:256.
NRK-49F cells 20 μM 48 h To test the inhibitory effect of AN-FTS on TGF-β1-induced activation of NRK-49F cells, the results showed that AN-FTS significantly inhibited the expression of fibrotic genes and reduced the protein levels of α-SMA, Col1a1, and fibronectin. Int J Nanomedicine. 2021 Sep 21;16:6441-6453.
HCT116 cells 100 µM 24-48 h To assess the effect of Salirasib on HCT116 cell proliferation and apoptosis, results showed that Salirasib had no significant effect on cell proliferation and apoptosis within 24-48 h. Sci Rep. 2021 May 13;11(1):10302.
HEK293T cells 1-100 µM 16 h To assess the effect of Salirasib on cell viability, results showed that Salirasib had no significant effect on cell viability at concentrations ranging from 1 to 100 µM. Sci Rep. 2021 May 13;11(1):10302.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Balb/c mice 4T1-luc2 tumor model Intraperitoneal injection 15 mg/kg, 30 mg/kg Once daily for 14 days Evaluate the anti-tumor effect of FTS-IR783 in the 4T1-luc2 tumor model, results showed that FTS-IR783 is more effective than FTS. Acta Pharmacol Sin. 2022 Jul;43(7):1843-1856.
CD1 nude mice Panc-1 cell xenograft model Intraperitoneal injection 15 mg/kg Once daily for 20 days To evaluate the inhibitory effect of Salirasib on tumor growth in the Panc-1 cell xenograft model, the results showed that FTS demonstrated no significant antitumor efficacy in the Panc-1 xenograft model. Cell Death Dis. 2014 May 22;5(5):e1241.
Nude mice Subcutaneous xenograft model Intraperitoneal injection 10 mg/kg Daily for 12 days Salirasib significantly inhibited tumor growth from day 5 onwards, and after 12 days, the mean tumor weight was reduced by 56% Mol Cancer. 2010 Sep 22;9:256.
C57BL/6J mice Unilateral ureteral obstruction (UUO)-induced renal fibrosis model Intravenous injection 20 mg/kg Once daily for 7 days To evaluate the therapeutic effect of AN-FTS on UUO-induced renal fibrosis, the results showed that AN-FTS significantly improved renal function, alleviated renal injury, inflammation, and fibrosis, and inhibited the renal epithelial-mesenchymal transition process by suppressing the Ras/Raf1/p38 MAPK signaling pathway. Int J Nanomedicine. 2021 Sep 21;16:6441-6453.
Mice Aβ1–42-induced Alzheimer's disease model Intraperitoneal injection 3 mg/kg Once daily for 14 days FTS reduced the expression of proinflammatory factors and microglial activation in Aβ1–42 mice through the inhibition of Gal-3, improving cognitive function. CNS Neurosci Ther. 2024 Nov;30(11):e70127

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00867230 Myelodysplastic Syndrome|Leuke... More >>mia Less << PHASE1 COMPLETED 2025-02-09 U.T.M.D. Anderson Cancer Cente... More >>r, Houston, Texas, 77030, United States Less <<
NCT00531401 Carcinoma, Non-Small-Cell Lung PHASE2 COMPLETED 2025-11-09 Memorial Sloan Kettering Cance... More >>r Center, New York, New York, 10017, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.79mL

0.56mL

0.28mL

13.95mL

2.79mL

1.39mL

27.89mL

5.58mL

2.79mL

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