GLPBio

FTI 276 TFA

Catalog No.: GC36085Purity:>98.00%
COASDSData Sheet

FTI-276 es un inhibidor de la transferasa de farnesilo de proteína (PFT) con IC50s de 0,9 nM y 0,5 nM para Plasmodium falciparum y humano, respectivamente.

Los productos son exclusivamente para uso en investigación. No aptos para uso humano. No vendemos a pacientes.

FTI 276 TFA
Cas No.: 1217471-51-6
5mgIn Stock
$176.00
1
10mgIn Stock
$292.00
1
25mgIn Stock
$584.00
1
50mgIn Stock
$944.00
1
100mgIn Stock
$1,520.00
1
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Descripción (Description)

FTI 276 TFA is a protein farnesyl transferase (PFT) inhibitor with an IC50 value of 1nM [1]. FTI 276 TFA can block Ras oncogenic signaling and prevent constitutive activation of the MAPK cascade [2]. FTI 276 TFA has been widely used to inhibit tumor growth in the primary mouse lung tumor model [3].

In vitro, FTI 276 TFA treatment (50μM) for 24 hours significantly reduced the extracellular MMP-1 level in 143B cells and inhibited the invasion of 143B cells[4].

In vivo, FTI 276 TFA treatment via daily intraperitoneal injection at a dose of 70mg/kg for 80 days significantly inhibited the growth of A549 xenograft tumors (express K-Ras mutations) in mice[5]. Intravenous infusion of 307μg/kg/day dose of FTI 276 TFA for 3 weeks significantly reduced myocardial fibrosis and improved cardiac remodeling in spontaneously hypertensive rats [6]. Continuous intraperitoneal injection of 50mg/kg/day dose of FTI 276 TFA for 36 consecutive days significantly inhibited tumor growth in the Calu-1 xenograft mouse model[7].

References:
[1] Chakrabarti D, Da Silva T, Barger J, et al. Protein Farnesyltransferase and Protein Prenylation inPlasmodium falciparum[J]. Journal of Biological Chemistry, 2002, 277(44): 42066-42073.
[2] Lerner E C, Qian Y, Blaskovich M A, et al. Ras CAAX peptidomimetic FTI-277 selectively blocks oncogenic Ras signaling by inducing cytoplasmic accumulation of inactive Ras-Raf complexes[J]. Journal of Biological Chemistry, 1995, 270(45): 26802-26806.
[3] Lantry L E, Zhang Z, Crist K A, et al. Chemopreventive efficacy of promising farnesyltransferase inhibitors[J]. Experimental lung research, 2000, 26(8): 773-790.
[4] Garamszegi N, Garamszegi S P, Scully S P. Matrix metalloproteinase‐1 contribution to sarcoma cell invasion[J]. Journal of cellular and molecular medicine, 2012, 16(6): 1331-1341.
[5] Sun J, Qian Y, Hamilton A D, et al. Both farnesyltransferase and geranylgeranyltransferase I inhibitors are required for inhibition of oncogenic K-Ras prenylation but each alone is sufficient to suppress human tumor growth in nude mouse xenografts[J]. Oncogene, 1998, 16(11): 1467-1473.
[6] Li X, Han J, Li L, et al. Effect of farnesyltransferase inhibition on cardiac remodeling in spontaneously hypertensive rats[J]. International journal of cardiology, 2013, 168(4): 3340-3347.
[7] Sun J, Qian Y, Hamilton A D, et al. Ras CAAX peptidomimetic FTI 276 selectively blocks tumor growth in nude mice of a human lung carcinoma with K-Ras mutation and p53 deletion[J]. Cancer research, 1995, 55(19): 4243-4247.

Protocolo (Protocol)

Cell experiment [1]:

Cell lines

143B cells

Preparation Method

143B cells were cultivated in DMEM medium supplemented with 10% heat-inactivated fetal bovine serum (FBS) at 37°C in an incubator with 5% CO2. After trypsinization, cells were quenched in DMEM with 5% bovine serum albumin then incubated overnight in p100 plates at 37°C to achieve a 70% confluence before serum starvation. Different concentrations of FTI 276 TFA (0, 2.5, 5, 15, and 50μM) were used in serum-free DMEM for 24h. Following exposure, cells were washed with PBS and harvested on ice for analysis.

Reaction Conditions

0, 2.5, 5, 15, and 50μM; 24h

Applications

FTI 276 TFA treatment significantly reduced the extracellular MMP-1 protein levels in 143B cells in a dose-dependent manner.
Animal experiment [2]:

Animal models

Female nude mice

Preparation Method

Female nude mice (8 weeks old) were maintained in a controlled environment at 22±3°C and 60% relative humidity under a 12h light/dark cycle, and were given free access to standard rodent nutrition and water. Calu-1 cells were harvested, resuspended in PBS, and injected s.c. into the right and left flanks of mice (107 cells/flank). On day 32, after s.c. implantation of tumors, animals were dosed i.p. with 0.2ml once daily for 36 days. Control mice received a saline vehicle whereas treated mice received injections of FTI 276 TFA (50mg/kg). The tumor volumes were determined by measuring the length (1) and width (w) and calculating the volume (V = lw2/2).

Dosage form

50mg/kg/day for 36 days; i.p.

Applications

FTI 276 TFA treatment significantly inhibited tumor growth in the Calu-1 xenograft mouse model.

References:
[1] Garamszegi N, Garamszegi S P, Scully S P. Matrix metalloproteinase‐1 contribution to sarcoma cell invasion[J]. Journal of cellular and molecular medicine, 2012, 16(6): 1331-1341.
[2] Sun J, Qian Y, Hamilton A D, et al. Ras CAAX peptidomimetic FTI 276 selectively blocks tumor growth in nude mice of a human lung carcinoma with K-Ras mutation and p53 deletion[J]. Cancer research, 1995, 55(19): 4243-4247.

Documentos del producto (Product Documents)

Purity:>98.00%Appearance:A solid
COASDSData Sheet

Propiedades químicas (Chemical Properties)

N.º CAS
1217471-51-6
SMILES
O=C(O)[C@@H](NC(C1=CC=C(NC[C@@H](N)CS)C=C1C2=CC=CC=C2)=O)CCSC.O=C(O)C(F)(F)F
Fórmula molecular
C23H28F3N3O5S2
Peso molecular
547.61
Solubilidad
Soluble in DMSO
Almacenamiento
Store at -20°C
Consejos generales
Seleccione un disolvente adecuado según los datos de solubilidad del producto. Una vez preparada, divida la solución madre en alícuotas para evitar ciclos repetidos de congelación y descongelación.
Utilice las soluciones madre en un plazo de 6 meses si se conservan a -80°C, o de 1 mes si se conservan a -20°C.
Para mejorar la solubilidad, caliente el tubo a 37°C y soníquelo durante un periodo adecuado.
Condiciones de envío
Las muestras de evaluación se envían con acumuladores de frío. Los demás tamaños se envían a temperatura ambiente o, previa solicitud, con acumuladores de frío.

Calculadoras (Calculators)Molaridad / Dilución / Peso molecular / Conversión de unidades / Formulación in vivo / Solubilidad

g/mol

Reviews

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