Size | Price | Stock | Qty |
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2mg |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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Purity: ≥98%
FTI 277 HCl (FTI-277; FTI277), the HCl salt of FTI 277, is a peptide mimetic of the COOH-terminal Cys-Val-Ile-Met of K-Ras4B which is a novel, potent and selective farnesyltransferase (FTase) inhibitor with antiviral activity. It inhibits FTase with an IC50 of 500 pM. It shows >100-fold selectivity for FTase over the closely related GGTase I. FTI-277 is a highly potent Ras CAAX peptidomimetic which antagonizes both H- and K-Ras oncogenic signaling.FTI-277 inhibits the processing of both oncogenic and normal Ras. FTI-277 was extremely potent (IC50 = 100 nM) at inhibiting H-Ras, but not the geranylgeranylated Rap1A processing in whole cells.
ln Vitro |
HeLa 3A, a kind of radioresistant cell that expresses the 24-kDa isoform, showed a substantial decrease in survival after 48 hours of treatment with FTI-277 (20 microM), while control cells (HeLa PINA) showed no significant change in survival. FTI-277's radiosensitizing action is followed by a decrease in G(2)/M-phase arrest in both cell types as well as an increase in postmitotic cell death in HeLa 3A cells [1]. In a dose- and time-dependent manner, PC-3 cells treated with GGTI-298 and FTI-277 were unable to migrate or invade [3].
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ln Vivo |
When compared to vehicle alone, FTI-277 therapy inhibited elevated PTP-1B and PTEN protein expression in burned mice. On the other hand, in sham-burned animals, FTI-277 had no discernible effect on PTP-1B or PTEN protein expression [2].
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Animal Protocol |
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References |
[1]. Cohen-Jonathan E, et al. The farnesyltransferase inhibitor FTI-277 suppresses the 24-kDa FGF2-induced radioresistance in HeLa cells expressing wild-type RAS. Radiat Res. 1999 Oct;152(4):404-11.
[2]. 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. [3]. Virtanen SS, et al. Inhibition of GGTase-I and FTase disrupts cytoskeletal organization of human PC-3 prostate cancer cells. Cell Biol Int. 2010 Aug;34(8):815-26. [4]. Bordier BB, et al. A prenylation inhibitor prevents production of infectious hepatitis delta virus particles. J Virol. 2002 Oct;76(20):10465-72. |
Molecular Formula |
C22H30CLN3O3S2
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Molecular Weight |
484.07
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CAS # |
180977-34-8
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Related CAS # |
FTI-277;170006-73-2
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SMILES |
CSCC[C@@H](C(OC)=O)NC(C1=CC=C(NC[C@@H](N)CS)C=C1C2=CC=CC=C2)=O.[H]Cl
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InChi Key |
PIAFFJUUNXEDEW-PXPMWPIZSA-N
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InChi Code |
InChI=1S/C22H29N3O3S2.ClH/c1-28-22(27)20(10-11-30-2)25-21(26)18-9-8-17(24-13-16(23)14-29)12-19(18)15-6-4-3-5-7-15;/h3-9,12,16,20,24,29H,10-11,13-14,23H2,1-2H3,(H,25,26);1H/t16-,20+;/m1./s1
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Chemical Name |
methyl (5-(((R)-2-amino-3-mercaptopropyl)amino)-[1,1-biphenyl]-2-carbonyl)-L-methioninate hydrochloride
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.16 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.16 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.16 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 33.33 mg/mL (68.85 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.0658 mL | 10.3291 mL | 20.6582 mL | |
5 mM | 0.4132 mL | 2.0658 mL | 4.1316 mL | |
10 mM | 0.2066 mL | 1.0329 mL | 2.0658 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.