| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| Targets |
IC50: 250 nM (FT) and 520 nM (GGT)[1]
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| ln Vitro |
Human cancer cells that are KRAS-dependent but not mutant KRAS-dependent undergo apoptosis when exposed to FGTI-2734 mesylate (1-30 μM; 72 hours) [1]. The inhibition of HDJ2, RAP1A, KRAS, NRAS, and protein prenylation is achieved by FGTI-2734 mesylate (3-30 μM; 72 hours). In RAS-transformed mouse NIH3T3 cells as well as mutated KRAS human cancer cells, FGTI-2734 mesylate inhibits KRAS membrane localization [1].
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| ln Vivo |
Mesylate FGTI-2734 (ip; 100 mg/kg/day for 18 to 25 days) only inhibits the growth of tumors that are dependent on KRAS; it has no effect on tumors that are independent of KRAS[1].
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| Cell Assay |
Apoptosis Analysis[1]
Cell Types: MiaPaCa2, L3.6pl, Calu6 cells Tested Tested Concentrations: 1, 3, 10, 30 μM Incubation Duration: 72 hrs (hours) Experimental Results: Induced apoptosis in mutant KRAS-dependent human cancer cell lines Western Blot Analysis[1] Cell Types: KRAS, HRAS, and NRAS-transformed NIH3T3 cells Tested Tested Concentrations: 3, 10, 30 μM Incubation Duration: 72 hrs (hours) Experimental Results: Inhibited both protein prenylation of HDJ2, RAP1A, KRAS and NRAS. |
| Animal Protocol |
Animal/Disease Models: Male SCID-bg mice following injection of MiaPaCa2, L3.6pl, Calu6, A549, H460 and DLD1 cancer cells[1]
Doses: 100 mg/kg Route of Administration: Intraperitoneally; daily; for 18 to 25 days Experimental Results: Inhibited tumor growth in mutant KRAS-dependent tumors. |
| References |
[1]. Kazi A, et al. Dual farnesyl and geranylgeranyl transferase inhibitor thwarts mutant KRAS-driven patient-derived pancreatic tumors. Clin Cancer Res. 2019 Jun 21.
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| Molecular Formula |
C27H35FN6O5S2
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|---|---|
| Molecular Weight |
606.73
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| CAS # |
2702297-24-1
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| Related CAS # |
FGTI-2734;1247018-19-4
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| SMILES |
S(O)(=O)(=O)C.N(C1C=CC(C#N)=CC=1F)(CCN(CC1CCCCC1)S(C1N=CC=CC=1)(=O)=O)CC1=CN=CN1C
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| Solubility (In Vitro) |
DMSO: 75 mg/mL (123.61 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3 mg/mL (4.94 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 30.0 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: ≥ 3 mg/mL (4.94 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 30.0 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: ≥ 3 mg/mL (4.94 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6482 mL | 8.2409 mL | 16.4818 mL | |
| 5 mM | 0.3296 mL | 1.6482 mL | 3.2964 mL | |
| 10 mM | 0.1648 mL | 0.8241 mL | 1.6482 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.
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