Farnesyl thiosalicylic acid amide (Synonyms: FTS amide; Salirasib amide)

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Farnesyl thiosalicylic acid amide (FTS-A) is an orally active derivative of farnesyl thiosalicylic acid (HY-14754). Farnesyl thiosalicylic acid amide reduces Ras-GTP levels and inhibits cell growth with IC₅₀s of 20 and 10 μM for Panc-1 and U87 cells, respectively. Farnesyl thiosalicylic acid amide can be used for the research of cancer.

For research use only. We do not sell to patients.

Farnesyl thiosalicylic acid amide Chemical Structure

CAS No. : 1092521-74-8

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K-Ras H-Ras N-Ras Ras

Biological Activity
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References
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Description

Cellular Effect

Cell Line	Type	Value	Description	References
BXPC-3	EC₅₀	> 20 μM Compound: FTSA	Cytotoxicity against human BxPC3 cells after 48 hrs by fluorescence assay Cytotoxicity against human BxPC3 cells after 48 hrs by fluorescence assay	[PMID: 24852279]
MIA PaCa-2	EC₅₀	> 20 μM Compound: FTSA	Cytotoxicity against human MIAPaCa2 cells harboring K-Ras mutant oncogene after 48 hrs by fluorescence assay Cytotoxicity against human MIAPaCa2 cells harboring K-Ras mutant oncogene after 48 hrs by fluorescence assay	[PMID: 24852279]
PANC-1	IC₅₀	20 μM Compound: FTS-A	Cytotoxicity against human PANC1 cells after 5 to 7 days Cytotoxicity against human PANC1 cells after 5 to 7 days	[PMID: 19072665]
U-87MG ATCC	IC₅₀	10 μM Compound: FTS-A	Cytotoxicity against human U87 cells after 5 to 7 days Cytotoxicity against human U87 cells after 5 to 7 days	[PMID: 19072665]

In Vitro

Farnesyl thiosalicylic acid amide (50 μM, 24 h) decreases the levels of total Ras-GTP and K-Ras-GTP in Panc-1 and U87 cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:	U87 cells
Concentration:	50 μM
Incubation Time:	24 h
Result:	Reduced the level of N-Ras-GTP, phospho-ERK and phospho-AKT.

In Vivo

Farnesyl thiosalicylic acid amide (100 mg/kg, i.g., once time) inhibits tumor growth in Panc-1 nude mouse model^[1].
Farnesyl thiosalicylic acid amide (100 mg/kg, p.o., twice a day, 14 days) inhibits tumor growth in U87 nude mouse model^[1].

Pharmacokinetic Analysis in Panc-1 Nude Mouse Model^[1]

Route	Dose (mg/kg)	half-life (min)	T_max (h)	C_max (ng/mL)	AUC_0-inf (min*ng/mL)
i.g.	100	314	110	371	108783

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

357.55

Formula

C₂₂H₃₁NOS

CAS No.

1092521-74-8

SMILES

C/C(C)=C/CC/C(C)=C/CC/C(C)=C/CSC1=C(C=CC=C1)C(N)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Goldberg L, et al. New derivatives of farnesylthiosalicylic acid (salirasib) for cancer treatment: farnesylthiosalicylamide inhibits tumor growth in nude mice models. J Med Chem. 2009 Jan 8;52(1):197-205. [Content Brief]

Farnesyl thiosalicylic acid amide Related Classifications

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Farnesyl thiosalicylic acid amide1092521-74-8FTS amide Salirasib amideRasPanc-1U87cancerRas-GTPorally activeInhibitorinhibitorinhibit

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