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Purity: ≥98%
PND-1186 (also known as SR2156, PND1186 or VS4718) is a novel, potent, reversible and selective FAK (focal adhesion kinase) inhibitor with potential anticancer activities. It inhibits FAK with an IC50 of 1.5 nM. PND-1186 shows potent anti-proliferative activity in vitro with an IC50 of ~100 nM in breast carcinoma cells, and high in vivo antitumor efficacy against ovarian carcinoma tumors.
| ln Vitro |
PND-1186's IC50 in breast cancer cells was found to be less than 100 nM using anti-phospho-specific immunoblotting against FAK Tyr-397[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 decreased final 4T1 tumor weight 2-fold whereas 30 mg/kg treatment slightly decreased 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 |
C25H26F3N5O3
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| Molecular Weight |
501.5
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| CAS # |
1061353-68-1
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| Related CAS # |
PND-1186 hydrochloride;1356154-94-3
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| SMILES |
O=C(NC)C1=CC=CC=C1NC2=CC(NC3=C(OC)C=C(N4CCOCC4)C=C3)=NC=C2C(F)(F)F
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| InChi Key |
IGUBBWJDMLCRIK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H26F3N5O3/c1-29-24(34)17-5-3-4-6-19(17)31-21-14-23(30-15-18(21)25(26,27)28)32-20-8-7-16(13-22(20)35-2)33-9-11-36-12-10-33/h3-8,13-15H,9-12H2,1-2H3,(H,29,34)(H2,30,31,32)
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| Chemical Name |
2-((2-((2-methoxy-4-morpholinophenyl)amino)-5-(trifluoromethyl)pyridin-4-yl)amino)-N-methylbenzamide.
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| Synonyms |
SR-2156; VS-4718; PND-1186; PND 1186; PND1186; SR 2516; SR2516; VS4718; VS 4718.
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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) |
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| Solubility (In Vivo) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9940 mL | 9.9701 mL | 19.9402 mL | |
| 5 mM | 0.3988 mL | 1.9940 mL | 3.9880 mL | |
| 10 mM | 0.1994 mL | 0.9970 mL | 1.9940 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.
PND-1186 inhibitory effects differ from Dasatinib (Src inhibition). Cancer Biol Ther. 2010 May; 9(10): 764–777. |
PND-1186 inhibits ovarian carcinoma tumor growth. Cancer Biol Ther. 2010 May; 9(10): 764–777.Cancer Biol Ther.2010 May 15;9(10):764-77. |
Selective 4T1 cell apoptosis in suspension at low PND-1186 levels.Cancer Biol Ther.2010 May 15;9(10):764-77. |
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