Cat. No.: HY-15873A

FTI 276 TFA

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FTI 276 TFA is a farnesyltransferase (FTase) inhibitor with an IC₅₀ of 0.5 nM, and it exhibits selectivity for FTase over geranylgeranyltransferase I (GGTase I). FTI 276 TFA blocks the farnesylation of H-Ras and K-Ras4B, causes inactive Ras-Raf complexes to accumulate in the cytoplasm, and inhibits constitutive MAPK activation. FTI 276 TFA reduces the number, incidence and volume of tumors, and restricts the growth of tumors expressing activated K-ras. FTI 276 TFA can be used in research related to pulmonary adenoma.

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Pureté: 98.31%
CAS No.: 1217471-51-6
Formule: C₂₃H₂₈F₃N₃O₅S₂
Masse moléculaire:547.61

Stockage:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

FTI 276 TFA Chemical Structure

CAS No.: 1217471-51-6

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

IC50: 0.9 nM (PFT, Plasmodium falciparum), 0.5 nM (PFT, human)^[1].

Voir tous les produits spécifiques à Isoform Ras :

Voir tous les produits spécifiques à Isoform p38 MAPK :

In Vitro

FTI 276 TFA potently and selectively inhibits FTase in vitro, with 100-fold greater activity against FTase than GGTase I^[1].
FTI 276 TFA inhibits farnesylation of K-Ras4B in vitro with 10-fold lower potency than it inhibits farnesylation of H-Ras^[1].
FTI 276 TFA potently inhibits Daudi cell-derived FTase with an IC₅₀ of 500 pM and shows 100-fold selectivity over Daudi cell-derived GGTase I, which it inhibits with an IC₅₀ of 50 nM^[2].

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

In Vivo

FTI 276 TFA (50 mg/kg/day; subcutaneous; constant rate; 30 days) produces significant chemotherapeutic efficacy in established NNK-induced lung adenomas in male A/J mice^[1].

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

Chemical Information

CAS No. 1217471-51-6
Appearance Solid
Masse moléculaire 547.61
Formule C₂₃H₂₈F₃N₃O₅S₂
Color White to off-white
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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (182.61 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8261 mL

9.1306 mL

18.2612 mL

5 mM

0.3652 mL

1.8261 mL

3.6522 mL

10 mM

0.1826 mL

0.9131 mL

1.8261 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.57 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.57 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.57 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (271 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. antry LE, et al. Effect of farnesyltransferase inhibitor FTI-276 on established lung adenomas from A/J mice induced by 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone. Carcinogenesis. 2000;21(1):113-116. [Content Brief]

[2]. Lerner EC, et al. Ras CAAX peptidomimetic FTI-277 selectively blocks oncogenic Ras signaling by inducing cytoplasmic accumulation of inactive Ras-Raf complexes. J Biol Chem. 1995;270(45):26802-26806. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8261 mL	9.1306 mL	18.2612 mL	45.6529 mL
	5 mM	0.3652 mL	1.8261 mL	3.6522 mL	9.1306 mL
	10 mM	0.1826 mL	0.9131 mL	1.8261 mL	4.5653 mL
	15 mM	0.1217 mL	0.6087 mL	1.2174 mL	3.0435 mL
	20 mM	0.0913 mL	0.4565 mL	0.9131 mL	2.2826 mL
	25 mM	0.0730 mL	0.3652 mL	0.7304 mL	1.8261 mL
	30 mM	0.0609 mL	0.3044 mL	0.6087 mL	1.5218 mL
	40 mM	0.0457 mL	0.2283 mL	0.4565 mL	1.1413 mL
	50 mM	0.0365 mL	0.1826 mL	0.3652 mL	0.9131 mL
	60 mM	0.0304 mL	0.1522 mL	0.3044 mL	0.7609 mL
	80 mM	0.0228 mL	0.1141 mL	0.2283 mL	0.5707 mL
	100 mM	0.0183 mL	0.0913 mL	0.1826 mL	0.4565 mL

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FTI 276 TFA

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Voir tous les produits spécifiques à Isoform Ras

Voir tous les produits spécifiques à Isoform p38 MAPK

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

FTI 276 TFA Related Classifications

HY-15873A Related Classifications