| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| ln Vitro |
PND-1186 possesses an IC50 of approximately 100 nM in breast cancer cells as shown by FAK Tyr-397 anti-phospho-specific immunoblotting[1]. FAK has a crucial role in generating an invasive and metastatic cell phenotype in murine 4T1 breast cancer cells. When PND-1186 is introduced to 4T1 cells at increasing concentrations (0.1 to 1.0 µM), FAK Tyr-397 phosphorylation (pY397) is inhibited, and within an hour, total FAK protein levels are raised[1].
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| ln Vivo |
PND-1186 suppresses the growth of 4T1 subcutaneous tumors by inducing apoptosis when injected subcutaneously in the neck region (30 mg/kg or 100 mg/kg)[1].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: 4T1 breast carcinoma cells Tested Concentrations: 0.1, 0.2, 0.4, 0.6 and 1.0 µM Incubation Duration: 1 hour Experimental Results: Inhibited FAK Tyr-397 phosphorylation (pY397) and resulted in elevated levels of total FAK protein. |
| Animal Protocol |
Animal/Disease Models: balb/c (Bagg ALBino) mouse:[1]
Doses: 30 mg/kg or 100 mg/kg Route of Administration: Injected (100 µL) subcutaneously (sc) in the neck region; every 12 h (twice-daily, bid) for 5 days . Experimental Results: 100 mg/kg treatment Dramatically diminished final 4T1 tumor weight 2-fold whereas 30 mg/kg treatment slightly diminished final tumor weight but was not Dramatically different compared to control. |
| References |
[1]. Tanjoni I, et al. PND-1186 FAK inhibitor selectively promotes tumor cell apoptosis in three-dimensional environments. Cancer Biol Ther. 2010 May 15;9(10):764-77.
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| Molecular Formula |
C25H27CLF3N5O3
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|---|---|
| Molecular Weight |
537.96
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| CAS # |
1356154-94-3
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| Related CAS # |
PND-1186;1061353-68-1
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| SMILES |
Cl.FC(C1=CN=C(C=C1NC1C=CC=CC=1C(NC)=O)NC1C=CC(=CC=1OC)N1CCOCC1)(F)F
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| Solubility (In Vitro) |
DMSO : 200 mg/mL (371.77 mM)
H2O : 20 mg/mL (37.18 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (9.29 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 50.0 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: ≥ 5 mg/mL (9.29 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 50.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8589 mL | 9.2944 mL | 18.5887 mL | |
| 5 mM | 0.3718 mL | 1.8589 mL | 3.7177 mL | |
| 10 mM | 0.1859 mL | 0.9294 mL | 1.8589 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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