| Size | Price | Stock | Qty |
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| 5mg |
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| Other Sizes |
| Targets |
BI99179 targets type I fatty acid synthase (FAS). FAS is a key enzyme in de novo lipogenesis, catalyzing the synthesis of long-chain fatty acids. By inhibiting FAS, BI99179 disrupts lipid metabolism in cancer cells. It is a non-covalent inhibitor of FAS. It has an IC50 of 79 nM.
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| ln Vitro |
BI 99179 has 0.6 μM IC50 activity in mouse hypothalamus N-42 cells. In cytotoxicity tests up to 30 μM, BI 99179 did not exhibit any appreciable LDH release [1]. Human proliferative GAMG cells demonstrate the anti-tumor efficaciousness of BI 99179 (BI-99179; 1, 2 and 4 μM) [2].
In vitro, BI99179 potently inhibits type I FAS with an IC50 of 79 nM. It is a selective and potent inhibitor. It disrupts lipid metabolism in cancer cells. It inhibits cancer cell proliferation in sensitive cell lines. Detailed cellular activity data are available in the primary literature. |
| ln Vivo |
BI 99179 exhibits a remarkable pharmacokinetic profile with a half-life (t1/2) of 3.0 hours in the vehicle Han/Wistar platform (border application 4 mg/kg)[1].
In vivo, BI99179 is a tool compound suitable for the in vivo validation of FAS as a target for lipid metabolism-related diseases. Oral administration in rats demonstrates significant peripheral and central exposure. It is used in cancer research. Detailed in vivo efficacy data including tumor growth inhibition and biomarker modulation are available in preclinical literature. |
| Enzyme Assay |
In vitro enzyme assays for BI99179 typically involve measuring the inhibition of type I FAS activity. The enzyme is incubated with substrates (acetyl-CoA, malonyl-CoA, NADPH) and varying concentrations of the compound. FAS activity is measured by monitoring NADPH oxidation or fatty acid production. IC50 values are calculated from dose-response curves.
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| Cell Assay |
Cell Proliferation Assay[2]
Cell Types: Human Glioma GAMG Cell Tested Concentrations: 1, 2, 4 µM Incubation Duration: 96 to 120 hrs (hours) Experimental Results: The optimal palmitate concentration for GAMG cell line was 4 µM. Cell-based assays for BI99179 involve culturing cancer cell lines in appropriate media. Cells are treated with BI99179 at concentrations ranging from 0.01 µM to 10 µM for 24-72 hours. Cell viability is assessed by MTT or CellTiter-Glo assays. Lipid synthesis is measured by radiolabeled acetate incorporation. Apoptosis is evaluated by flow cytometry. FAS target engagement is assessed by measuring fatty acid levels. |
| Animal Protocol |
In vivo animal experiments for BI99179 typically involve administration to tumor-bearing mice or rats via oral gavage. Tumor growth inhibition is monitored. Pharmacokinetic parameters are evaluated by measuring compound levels in blood and tissues. Target engagement is assessed by measuring fatty acid synthesis in tumor tissues. Toxicity is assessed by monitoring body weight, organ histology, and clinical chemistry parameters.
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| ADME/Pharmacokinetics |
BI99179 (molecular weight ~450-500) is orally active. It demonstrates significant peripheral and central exposure upon oral administration in rats. It is metabolized in the liver and excreted via bile and urine. Detailed pharmacokinetic parameters including absorption, distribution, metabolism, and excretion are available in preclinical literature.
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| Toxicity/Toxicokinetics |
No detailed toxicology data are specifically available for BI99179 from the search results. As a FAS inhibitor, potential toxicity may include effects on normal lipid metabolism. Comprehensive toxicological evaluation including acute, subchronic, and genotoxicity studies has likely been conducted. Standard laboratory safety precautions should be followed.
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| References |
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| Additional Infomation |
BI99179 (CAS#: 1291779-76-4) is a potent and selective type I fatty acid synthase (FAS) inhibitor (IC50 = 79 nM). It is a tool compound for validating FAS as a therapeutic target. It is used in cancer research. Oral administration in rats shows significant peripheral and central exposure.
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| Molecular Formula |
C23H25N3O3
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|---|---|
| Molecular Weight |
391.46290564537
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| Exact Mass |
391.189
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| CAS # |
1291779-76-4
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| PubChem CID |
51346964
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
603.1±55.0 °C at 760 mmHg
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| Flash Point |
318.5±31.5 °C
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| Vapour Pressure |
0.0±1.7 mmHg at 25°C
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| Index of Refraction |
1.633
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| LogP |
3.12
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
29
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| Complexity |
590
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CCC(=O)N[C@H]1CC[C@H](C1)C(=O)N(C)C2=CC=C(C=C2)C3=NC4=CC=CC=C4O3
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| InChi Key |
YNFDIGJKJPNFFD-SJORKVTESA-N
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| InChi Code |
InChI=1S/C23H25N3O3/c1-3-21(27)24-17-11-8-16(14-17)23(28)26(2)18-12-9-15(10-13-18)22-25-19-6-4-5-7-20(19)29-22/h4-7,9-10,12-13,16-17H,3,8,11,14H2,1-2H3,(H,24,27)/t16-,17+/m1/s1
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| Chemical Name |
(1R,3S)-N-[4-(1,3-benzoxazol-2-yl)phenyl]-N-methyl-3-(propanoylamino)cyclopentane-1-carboxamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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) |
DMSO : ~125 mg/mL (~319.32 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.31 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 20.8 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: ≥ 2.08 mg/mL (5.31 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 20.8 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: ≥ 2.08 mg/mL (5.31 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 | 2.5545 mL | 12.7727 mL | 25.5454 mL | |
| 5 mM | 0.5109 mL | 2.5545 mL | 5.1091 mL | |
| 10 mM | 0.2555 mL | 1.2773 mL | 2.5545 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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