[CAS NO. 180977-34-8] FTI-277hydrochloride
PRODUCTS SPECIFICATIONS [180977-34-8]
DESCRIPTION [180977-34-8]
Overview
| MDL | MFCD28385886 |
|---|---|
| Molecular Weight | 484.07 |
| Molecular Formula | C22H30ClN3O3S2 |
| SMILES | CSCC[C@@H](C(OC)=O)NC(C1=CC=C(NC[C@@H](N)CS)C=C1C2=CC=CC=C2)=O.[H]Cl |
2 Publications Citing Use of MCE
Summary
FTI-277 hydrochloride is an inhibitor of farnesyl transferase (FTase) ; a highly potent Ras CAAX peptidomimetic which antagonizes both H- and K-Ras oncogenic signaling . FTI-277 hydrochloride can inhibit hepatitis delta virus (HDV) infection .
In Vitro
Treatment with FTI-277 (20 microM) for 48 h prior to irradiation led to a significant decrease in survival of radioresistant cells expressing the 24-kDa isoform (HeLa 3A) but had no effect on the survival of control cells (HeLa PINA). The radiosensitizing effect of FTI-277 is accompanied by a stimulation of postmitotic cell death in HeLa 3A cells and by a reduction in G(2)/M-phase arrest in both cell types [1]. Treatment of PC-3 cells with GGTI-298 and FTI-277 inhibited migration and invasion in a time- and dose-dependent manner [3].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
FTI-277 treatment prevented increased PTP-1B and PTEN protein expression in burned mice as compared with vehicle alone. In contrast, FTI-277 did not significantly alter protein expression of PTP-1B and PTEN in sham-burned mice [2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 100 mg/mL ( 206.58 mM ; Need ultrasonic)
H 2 O : 50 mg/mL ( 103.29 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 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 |
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1.
Add each solvent one by one: PBS
Solubility: 33.33 mg/mL (68.85 mM); Clear solution; Need ultrasonic
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2.
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3.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.16 mM); Clear solution
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4.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.16 mM); Clear solution
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.