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FTI-277 hydrochloride

Catalog No. T2700 CAS 180977-34-8

Synonyms: FTI 277 HCl

FTI-277 hydrochloride (FTI 277 HCl) is an effective and specific farnesyltransferase (FTase) inhibitor (IC50: 500 pM); this selectivity is about 100-fold than the closely related GGTase I.

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FTI-277 hydrochloride Chemical Structure

FTI-277 hydrochloride, CAS 180977-34-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 48.00
2 mg	In stock	$ 67.00
5 mg	In stock	$ 97.00
10 mg	In stock	$ 185.00
25 mg	In stock	$ 337.00
50 mg	In stock	$ 565.00
100 mg	In stock	$ 793.00
1 mL * 10 mM (in DMSO)	In stock	$ 113.00

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Purity: 98.19%

Purity: 97.57%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	FTI-277 hydrochloride (FTI 277 HCl) is an effective and specific farnesyltransferase (FTase) inhibitor (IC50: 500 pM); this selectivity is about 100-fold than the closely related GGTase I.
Targets&IC50	FTase:500 pM
In vitro	In mouse models infected with Hepatitis B Virus (HBV) and Hepatitis D Virus (HDV), FTI-277 administered intraperitoneally at a dosage of 50 mg/kg/day effectively clears Hepatitis D viremia.
In vivo	In drug-resistant myeloma cells, FTI-277 inhibits cell growth and induces apoptosis. It mitigates the toxicity induced by methamphetamine in SH-SY5Y cells through effects on cell degeneration, activation, the c-Jun N-terminal kinase cascade, and the Ras activation process. FTI-277 inhibits Ras processing (IC50: 100 nM) without affecting the overall cellular prenylation of Rap1A. Additionally, FTI-277 increases post-irradiation apoptosis and enhances the radiation sensitivity of H-ras transformed rat embryo cells.
Kinase Assay	FTase and GGTase I Activity Assay: FTase and GGTase I activities from 60,000×g supernatants of human Burkitt lymphoma (Daudi) cells are assayed. Inhibition studies are performed by determining the ability of Ras CAAX peptidomimetics to inhibit the transfer of [3H]farnesyl and [3H]geranylgeranyl from [3H]farnesylpyrophosphate and [3H]geranylgeranylpyrophosphate to H-Ras-CVLS and H-Ras-CVLL, respectively.
Cell Research	Cells are seeded at 8000–14 000 cells/well in 96-well plates. To establish a dose–response to FTI-277, cells are incubated for 96 h in two-fold serial dilutions ranging from 3.75 times 10-7 M to 1 times 10-5 M. Following continuous drug exposure, 50 μL MTT dye is added. The insoluble formazan complex is solubilized with DMSO and absorbance measured at 540 nm. IC50s and 95% confidence intervals are calculated by regression analysis of the linear portion of the dose–response curve. (Only for Reference)

Synonyms	FTI 277 HCl
Molecular Weight	484.07
Formula	C22H30ClN3O3S2
CAS No.	180977-34-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 12 mg/mL (24.8 mM)

H2O: 14 mg/mL (28.9 mM)

DMSO: 89 mg/mL (183.9 mM)

References and Literature

1. Lerner EC, et al. J Biol Chem. 1995, 270(45), 26802-26806. 2. Bernhard EJ, et al. Cancer Res. 1996, 56(8), 1727-1730. 3. Bolick SC, et al. Leukemia. 2003, 17(2), 451-457 4. Pirompul N, et al. Neurosci Lett. 2013, 545, 138-143. 5. Bordier BB, et al. J Clin Invest. 2003, 112(3), 407-414. 6. Nakazawa H, et al. Role of protein farnesylation in burn-induced metabolic derangements and insulin resistance in mouse skeletal muscle. PLoS One. 2015 Jan 16;10(1):e0116633. 7. Sun Q, Xiong K, Yuan Y, et al. Inhibiting fungal echinocandin resistance by small-molecule disruption of geranylgeranyltransferase type I activity[J]. Antimicrobial Agents and Chemotherapy. 2020, 64(2).

Citations

1. Sun Q, Xiong K, Yuan Y, et al Inhibiting fungal echinocandin resistance by small-molecule disruption of geranylgeranyltransferase type I activity. Antimicrobial Agents and Chemotherapy. 2020, 64(2).

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Immunology/Inflammation Compound Library Kinase Inhibitor Library Highly Selective Inhibitor Library Membrane Protein-targeted Compound Library GPCR Compound Library Anti-Cancer Active Compound Library Anti-Liver Cancer Compound Library Anti-Pancreatic Cancer Compound Library MAPK Inhibitor Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

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Keywords

FTI-277 hydrochloride 180977-34-8 Apoptosis GPCR/G Protein MAPK Metabolism Ras Transferase Inhibitor Farnesyl Transferase FTI 277 Ftase FTI-277 Hydrochloride FTI 277 Hydrochloride inhibit FTI277 Hydrochloride FTI-277 FTI277 hydrochloride FTI 277 hydrochloride FTI277 FTI 277 HCl inhibitor

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