PND-1186 (VS-4718)
Catalog No.S7653 Synonyms: SR-2156
Molecular Weight(MW): 501.5
PND-1186 (VS-4718) is a reversible and selective FAK inhibitor with IC50 of 1.5 nM. Phase 1.
5 Customer Reviews
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(a) Percentage of apoptotic HepG2 and Huh7.5 cells after 48 h of treatment with DMSO (Vehicle), 0.5 μM or 1 μM PND 1186 measured by Annexin V and flow cytometry. Values are plotted as mean±SD (*P<0.05; **P<0.01; versus Vehicle, n =3). (b) Representative WB for p21 and caspase-3 in HepG2 and Huh7.5 cells after 48 h of treatment with DMSO (0), 0.5 μM or 1 μM PND 1186. β-tubulin is reported as a loading control (n=2). (c) Relative mRNA expression of EZH2 and NOTCH2 genes as measured by qRT-PCR in HepG2 and Huh7.5 cells after 48 h of treatment with DMSO (Vehicle), 0.5 μM or 1 μM PND 1186 (*P<0.05; **P<0.01; versus Vehicle, n =3).
Cell Death Differ, 2017, 24(5):889-902. PND-1186 (VS-4718) purchased from Selleck.
Cells treated with different concentrations of VS-4718 for 24 h on 3D Matrigel culture were immunostained for cleaved caspase-3 and F-actin (d), and observed using confocal microscopy. Images are representative of cells treated with 10 μM VS-4718. Arrowheads (d) indicate cleaved caspase-3 activity. Data are presented as the means±s.d. of three independent experiments. The bar graphs show the average proportion of PI-positive spheroids. *P<0.01. Scale bar, 50 μm.
Oncogene, 2017, 36(39):5522-5531. PND-1186 (VS-4718) purchased from Selleck.
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Cells were added equally to coverslips pretreated with fibronectin at 10 g/ml. Kinase inhibitors were then applied to these cells at the indicated concentrations. U0126 is a MAP kinase inhibitor, PND1186 is an FAK kinase inhibitor, saracatinib is an Src kinase inhibitor, and wortmannin is a PI3K inhibitor. Twenty-five minutes later, cells were pulsed with 2mM5-FUrd for 10 min. Cells were then instantly fixed and stained with anti-BrdU antibody to visualize newly synthesized RNA in situ. Representative images are shown. (First column) 5-FUrd staining. Magnification, ×10. (Third column) 5-FUrd staining. Magnification, ×40. (Second and fourth columns) DAPI staining.
Molecular and Cellular Biology, 2016, 36(10):1555-1568.. PND-1186 (VS-4718) purchased from Selleck.
HIEC cells were treated with FAK inhibitor (1 μM VS-4718), or DMSO for 24 h, then exposed to 5 Gy of radiation and samples were taken 6 and 24 h later. Levels of FAK, p-FAK, and γH2AX were examined using western blotting and GAPDH was used as a loading control.
Toxicol Appl Pharmacol, 2018, 360:131-140. PND-1186 (VS-4718) purchased from Selleck.
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Combined treatment of Dasatinib and PND‐1186 results in strong growth inhibition in HCC cell lines. A, Cell viability of HCC3‐4, HCC4‐4, SNU‐398, SNU‐475 cells when treated with Dasatinib, PND‐1186, or Dasatinib+PND‐1186 at ~IC50 concentration determined using crystal violet staining. Data are presented as mean ± SD; and P‐value was calculated using Mann‐Whitney U test. Each dot represents one treatment replicate. B, Expression of p‐Src, Src, p‐FAK and FAK in HCC cell lines analyzed using Western blotting. GAPDH was used as loading control. Das, Dasatinib; Veh, Vehicle
Cancer Med, 2018, doi:10.1002/cam4.1777. PND-1186 (VS-4718) purchased from Selleck.
Purity & Quality Control
Choose Selective FAK Inhibitors
Biological Activity
| Description | PND-1186 (VS-4718) is a reversible and selective FAK inhibitor with IC50 of 1.5 nM. Phase 1. | ||
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| In vitro |
In vitro, PND-1186 inhibits 4T1 breast carcinoma motility, promotes 4T1 apoptosis in suspended conditions, and decreases 4T1 soft agar colony number and size. [1] In HEY and OVCAR8 cells, VS-4718 promotes G0-G1 cell-cycle arrest followed by cell death. [2] |
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| In vivo | In mice bearing 4T1 tumors, PND-1186 (100 mg/kg s.c.) inhibits 4T1 subcutaneous tumor growth by induction of apoptosis. In mice bearing ID8 tumors, PND-1186 (0.5 mg/mL for p.o.) also causes ovarian carcinoma tumor growth inhibition. [1] |
Protocol
| Kinase Assay: |
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In vitro kinase activity: GST-FAK in vitro kinase activity is measured and compared to His-tagged FAK 411–686 using the K-LISA screening kit and poly(Glu:Tyr) (4:1) copolymer as a substrate immobilized on microtiter plates. IC50 values are determined with various concentrations of test compounds in a buffer containing 50 µM ATP and 10 mM MnCl2, 50 mM HEPES (pH 7.5), 25 mM NaCl, 0.01% BSA, and 0.1 mM Na orthovanadate for 5 min at room temperature. Serial diluted compounds are tested in triplicate. Substrate phosphorylation is measured using horseradish peroxidase-conjugated anti-pTyr antibodies with spetrophotometric color quantitation. IC50 values are determined using the Hill-Slope Model. Kinase selectivity profiling is performed by using the KinaseProfiler service. |
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Solubility (25°C)
| In vitro | DMSO | 24 mg/mL (47.85 mM) |
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| Water | Insoluble | |
| Ethanol | Insoluble | |
| In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 2% DMSO+30% PEG 300+5% Tween 80+ddH2O For best results, use promptly after mixing. |
5mg/mL |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 501.5 |
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| Formula | C25H26F3N5O3 |
| CAS No. | 1061353-68-1 |
| Storage | powder |
| in solvent | |
| Synonyms | SR-2156 |
Bio Calculators
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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Dilution Calculator
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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
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Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Molarity Calculator
Clinical Trial Information
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT02651727 | Terminated | Pancreatic Cancer | Verastem Inc. | September 2015 | Phase 1 |
| NCT02651727 | Terminated | Pancreatic Cancer | Verastem Inc. | September 2015 | Phase 1 |
| NCT01849744 | Terminated | Non Hematologic Cancers|Metastatic Cancer | Verastem Inc. | June 2013 | Phase 1 |
| NCT01849744 | Terminated | Non Hematologic Cancers|Metastatic Cancer | Verastem Inc. | June 2013 | Phase 1 |
| NCT02215629 | Withdrawn | Relapsed or Refractory Acute Myeloid Leukemia|Relapsed or Refractory B-Cell Acute Lymphoblastic Leukemia | Verastem Inc. | null | Phase 1 |
| NCT02215629 | Withdrawn | Relapsed or Refractory Acute Myeloid Leukemia|Relapsed or Refractory B-Cell Acute Lymphoblastic Leukemia | Verastem Inc. | null | Phase 1 |
Tech Support
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
Tel: +1-832-582-8158 Ext:3
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Frequently Asked Questions
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Question 1:
Whether the in vivo formulation of PND-1186 (VS-4718) using 2% DMSO+30% PEG 300+5% Tween 80+ddH2O is suitable for injection?
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Answer:
The formulation for PND-1186: 2% DMSO+30% PEG 300+5% Tween 80+ddH2O can generate a clear solution with highest contraction at 5mg/ml. It may be suitable for oral administration or injection.
