FTI 277 HClFTase inhibitor CAS# 180977-34-8 |
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Quality Control & MSDS
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Chemical structure
3D structure
| Cas No. | 180977-34-8 | SDF | Download SDF |
| PubChem ID | 88309922 | Appearance | Powder |
| Formula | C22H30ClN3O3S2 | M.Wt | 484.07 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : 100 mg/mL (206.58 mM; Need ultrasonic) H2O : 50 mg/mL (103.29 mM; Need ultrasonic) | ||
| Chemical Name | methyl (2S)-2-[[4-[[(2R)-2-amino-3-sulfanylpropyl]amino]-2-phenylbenzoyl]amino]-4-methylsulfanylbutanoate;hydrochloride | ||
| SMILES | COC(=O)C(CCSC)NC(=O)C1=C(C=C(C=C1)NCC(CS)N)C2=CC=CC=C2.Cl | ||
| Standard InChIKey | PIAFFJUUNXEDEW-PXPMWPIZSA-N | ||
| Standard InChI | 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 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
FTI 277 HCl Dilution Calculator
FTI 277 HCl Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.0658 mL | 10.3291 mL | 20.6582 mL | 41.3163 mL | 51.6454 mL |
| 5 mM | 0.4132 mL | 2.0658 mL | 4.1316 mL | 8.2633 mL | 10.3291 mL |
| 10 mM | 0.2066 mL | 1.0329 mL | 2.0658 mL | 4.1316 mL | 5.1645 mL |
| 50 mM | 0.0413 mL | 0.2066 mL | 0.4132 mL | 0.8263 mL | 1.0329 mL |
| 100 mM | 0.0207 mL | 0.1033 mL | 0.2066 mL | 0.4132 mL | 0.5165 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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FTI-277 is a highly potent and selective FTase inhibitor. At concentration as low as 10 nM, FTI-277 inhibits H-Ras processing and the processing is blocked by more than 95% at 3 μM. [1]
Ras proteins are plasma membrane-associated GTPases. It acts as relay switches transducing biological information from extracellular signals to the nucleus. Farnesyltransferase (FTase) is an enzyme that catalyzed the Ras farnesylation, a lipid posttranslational modification that is required for Ras-induced malignant transformation. [1]
FTI-277, the methyl ester derivative of FTI-276, is extremely potent (ICGraphic = 100 nM) at inhibiting H-Ras, but not the geranylgeranylated Rap1A processing in whole cells. FTI-277 is a farnesylation-specific inhibitor which inhibits the processing of both oncogenic and normal Ras. [1]
In mice that hydrodynamically transfected to produce Hepatitis delta virus (HDV) viremia, FTI-277 treatment is effective in inhibiting viremia. [2]
References:
1. Bordier BB, Ohkanda J, Liu P et al. In vivo antiviral efficacy of prenylation inhibitors against hepatitis delta virus. J Clin Invest. 2003 Aug;112(3):407-14.
2. Lerner EC, Qian Y, Blaskovich MA 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 Nov 10;270(45):26802-6. PubMed PMID: 7592920.
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