製品番号: HY-13917

PND-1186

(別名: VS-4718; SR-2516)

16 Cited Publications

カスタマーレビュー

Based on 16 publication(s) in Google Scholar

PND-1186 (VS-4718) is a potent, highly-specific and reversible inhibitor of FAK with an IC₅₀ of 1.5 nM. PND-1186 selectively promotes tumor cell apoptosis.

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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

純度: 99.88%
CAS 番号: 1061353-68-1
分子式: C₂₅H₂₆F₃N₅O₃
分子量:501.50

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

PND-1186 構造式

CAS 番号: 1061353-68-1

容量

価格（税別）

在庫状況

数量

Amount: USD 0.00

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
- 臨床実験
化学情報
Publications (16)
溶剤 & 溶解度
- 体外
- 体内
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

PND-1186 (VS-4718) is a potent, highly-specific and reversible inhibitor of FAK with an IC₅₀ of 1.5 nM. PND-1186 selectively promotes tumor cell apoptosis^[1].

IC₅₀ & Target

IC50: 1.5 nM (FAK)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
786-0	IC₅₀	>50 μM Compound: VS-4718; PND1186	Antiproliferative activity against human 786-O cells assessed as reduction in cell viability Antiproliferative activity against human 786-O cells assessed as reduction in cell viability	[PMID: 32784087]
BXPC-3	IC₅₀	0.93 μM Compound: VS-4718; PND1186	Antiproliferative activity against human BXPC-3 cells assessed as reduction in cell viability Antiproliferative activity against human BXPC-3 cells assessed as reduction in cell viability	[PMID: 32784087]
DU-145	IC₅₀	0.62 μM Compound: VS-4718; PND1186	Antiproliferative activity against human DU-145 cells assessed as reduction in cell viability Antiproliferative activity against human DU-145 cells assessed as reduction in cell viability	[PMID: 32784087]
MDA-MB-231	IC₅₀	0.029 μM Compound: VS-4718; PND1186	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability	[PMID: 32784087]
NCI-H1975	IC₅₀	0.34 μM Compound: VS-4718; PND1186	Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability	[PMID: 32784087]
RD	IC₅₀	1.22 μM Compound: 3; VS-4718, PND-1186	Cytotoxicity against human RD cells incubated for 96 hrs by DIMSCAN method Cytotoxicity against human RD cells incubated for 96 hrs by DIMSCAN method	[PMID: 33058670]

体外実験

PND-1186 has an IC₅₀ of ~100 nM in breast carcinoma cells as determined by anti-phospho-specific immunoblotting to FAK Tyr-397^[1].
In murine 4T1 breast carcinoma cells, FAK is important in promoting an invasive and metastatic cell phenotype. Increasing concentrations of PND-1186 (0.1 to 1.0 μM) added to 4T1 cells inhibits FAK Tyr-397 phosphorylation (pY397) and results in elevated levels of total FAK protein within 1 h^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:

4T1 breast carcinoma cells
Concentration:

0.1, 0.2, 0.4, 0.6 and 1.0 µM
Incubation Time:

1 hour
Result:

Inhibited FAK Tyr-397 phosphorylation (pY397) and resulted in elevated levels of total FAK protein.

体内実験

PND-1186 (30 mg/kg or 100 mg/kg; subcutaneously; injected subcutaneously in the neck region) inhibits 4T1 subcutaneous tumor growth by induction of apoptosis^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

BALB/c mice^[1]
Dosage:

30 mg/kg or 100 mg/kg
Administration:

Injected (100 µL) subcutaneously in the neck region; every 12 h (twice-daily, b.i.d.) for 5 days.
Result:

100 mg/kg treatment significantly reduced final 4T1 tumor weight 2-fold whereas 30 mg/kg treatment slightly reduced final tumor weight but was not significantly different compared to control.

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

化学情報

CAS 番号 1061353-68-1
性状 Solid
分子量 501.50
分子式 C₂₅H₂₆F₃N₅O₃
Color White to gray
SMILES

O=C(NC)C1=CC=CC=C1NC2=CC(NC3=CC=C(N4CCOCC4)C=C3OC)=NC=C2C(F)(F)F
別名

VS-4718; SR-2516
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (16)

All Cell Proliferation/Viability AssayWBRT-PCRIFIn Vivo Efficacy Study

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Journal Impact Factor

Cancer Cell

A Platform of Synthetic Lethal Gene Interaction Networks Reveals that the GNAQ Uveal Melanoma Oncogene Controls the Hippo Pathway through FAK. [Abstract]

2019 Mar 18;35(3):457-472.e5. PMID: 30773340

PND-1186 purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2019 Mar 18;35(3):457-472.e5. [Abstract]

Immunoblot showing YAP nuclear and cytoplasmic localization after 2 h VS-4718 (PND-1186) (1 μM) treatment in OMM1.3 cells, using lamin A/C and a-tubulin as nuclear and cytoplasmic markers, respectively.

PND-1186 purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2019 Mar 18;35(3):457-472.e5. [Abstract]

Immunoblot showing levels of total YAP over a time course of VS-4718 (PND-1186) treatment (1 μM; 6-36 h) in OMM1.3 cells.

PND-1186 purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2019 Mar 18;35(3):457-472.e5. [Abstract]

UM cell lines (MEL270, 92.1, OMM1.3, OMM1.5 and MEL202 with GNAQ active mutation) are sensitive to FAK inhibition in a dose-dependent manner after treatment with VS-4718 (PND-1186) (0.001-10 μM; 72 h), SKCM cells (SK-MEL-28 with BRAF mutation) served as control.

PND-1186 purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2019 Mar 18;35(3):457-472.e5. [Abstract]

VS-4718 (PND-1186) (1-10 μM; 15-360 min) inhibits FAK activation in OMM1.3 (decrease in pY397- FAK, left panel) and induces apoptosis (increased cleaved PARP, right panel).

PND-1186 purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2019 Mar 18;35(3):457-472.e5. [Abstract]

mRNA expression of CTGF and CYR61 measured by qPCR in UM cells OMM1.3 with VS-4718 (PND-1186) treatment (1μM, vehicle treatment as control, mean ± SEM, n=3).

PND-1186 purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2019 Mar 18;35(3):457-472.e5. [Abstract]

Immunofluorescent staining of endogenous YAP (green) and Hoeschst staining for nuclear DNA (blue) in OMM1.3 cells after VS-4718 (PND-1186) treatment (1μM, vehicle treatment as control).

PND-1186 purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2019 Mar 18;35(3):457-472.e5. [Abstract]

Tumor volume of MEL270 cells in vivo with or without VS-4718 (PND-1186) (100mg/kg; oral gavage; twice daily) treatment, tumor size at the end of the study were measured (mean ± SEM, n=8) (left panel), and hematoxylin and eosin (H&E)-stained sections of representative tumors from each group are shown (right panel).
Cancer Commun (Lond)

N6-methyladenosine modification of CENPF mRNA facilitates gastric cancer metastasis via regulating FAK nuclear export. [Abstract]

2023 Jun;43(6):685-705. PMID: 37256823
Nat Commun

The dysadherin/MMP9 axis modifies the extracellular matrix to accelerate colorectal cancer progression. [Abstract]

2024 Nov 30;15(1):10422. PMID: 39613801
Cell Death Differ

Functional genomic screens uncover FERMT2 as a critical regulator of YAP/TAZ-driven tumorigenicity. [Abstract]

2026 Mar 6. PMID: 41792242
J Exp Clin Cancer Res

Focal Adhesion Kinase (FAK)-Hippo/YAP transduction signaling mediates the stimulatory effects exerted by S100A8/A9-RAGE system in triple-negative breast cancer (TNBC). [Abstract]

2022 Jun 3;41(1):193. PMID: 35655319
Sci Adv

Inhibition of focal adhesion kinase impairs tumor formation and preserves hearing in a murine model of NF2-related schwannomatosis. [Abstract]

2026 Jan 30;12(5):eady8382. PMID: 41616055
Clin Cancer Res

High-throughput Chemical Screening Identifies Focal Adhesion Kinase and Aurora Kinase B Inhibition as a Synergistic Treatment Combination in Ewing Sarcoma. [Abstract]

2019 Jul 15;25(14):4552-4566. PMID: 30979745
EMBO Mol Med

ERK5 suppression overcomes FAK inhibitor resistance in mutant KRAS-driven non-small cell lung cancer. [Abstract]

2024 Oct;16(10):2402-2426. PMID: 39271958
Apoptosis

IGFBP2 induces podocyte apoptosis promoted by mitochondrial damage via integrin α5/FAK in diabetic kidney disease. [Abstract]

2024 May 25. PMID: 38796567
Commun Biol

Abnormal cytoskeletal remodeling but normal neuronal excitability in a mouse model of the recurrent developmental and epileptic encephalopathy-susceptibility KCNB1-p.R312H variant. [Abstract]

2024 Dec 30;7(1):1713. PMID: 39738805
Cancers (Basel)

FAK Inhibitor-Based Combinations with MEK or PKC Inhibitors Trigger Synergistic Antitumor Effects in Uveal Melanoma. [Abstract]

2023 Apr 13;15(8):2280. PMID: 37190207
Am J Physiol Renal Physiol

Focal adhesion kinase inhibition induces membrane accumulation of aquaporin-2 in renal epithelial cells by actin depolymerization and endocytosis inhibition. [Abstract]

2025 Oct 1;329(4):F465-F481. PMID: 40857140
Chembiochem

Development and characterization of selective FAK inhibitors and PROTACs with in vivo activity. [Abstract]

2023 Oct 4;24(19):e202300141. PMID: 37088717
Mol Biol Cell

Inducible FAK loss but not FAK inhibition in endothelial cells of PYK2-null mice activates p53 tumor suppressor to prevent tumor growth. [Abstract]

2025 Jun 1;36(6):ar64. PMID: 40202821
bioRxiv

2024 November 06.
bioRxiv

2020 Apr.

溶剤 & 溶解度

体外:

DMSO : 31.25 mg/mL (62.31 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.99 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.99 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 3

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: ≥ 2.5 mg/mL (4.99 mM); Clear solution

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

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COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
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OR (2659 KB)
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Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9940 mL	9.9701 mL	19.9402 mL	49.8504 mL
	5 mM	0.3988 mL	1.9940 mL	3.9880 mL	9.9701 mL
	10 mM	0.1994 mL	0.9970 mL	1.9940 mL	4.9850 mL
	15 mM	0.1329 mL	0.6647 mL	1.3293 mL	3.3234 mL
	20 mM	0.0997 mL	0.4985 mL	0.9970 mL	2.4925 mL
	25 mM	0.0798 mL	0.3988 mL	0.7976 mL	1.9940 mL
	30 mM	0.0665 mL	0.3323 mL	0.6647 mL	1.6617 mL
	40 mM	0.0499 mL	0.2493 mL	0.4985 mL	1.2463 mL
	50 mM	0.0399 mL	0.1994 mL	0.3988 mL	0.9970 mL
	60 mM	0.0332 mL	0.1662 mL	0.3323 mL	0.8308 mL

PND-1186

16 Cited Publications

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PND-1186

Apoptosis Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Bioactive Compound Library Max

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

MedChemExpress（MCE）の使用を引用している文献 PND-1186

生物活性

化学情報

Publications (16)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

PND-1186

Apoptosis Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Bioactive Compound Library Max

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

MedChemExpress（MCE）の使用を引用している文献 PND-1186

生物活性

化学情報

Publications (16)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

PND-1186 関連分類

製品番号: HY-13917