Art. -Nr.: HY-12289

Defactinib

(Synonyms: VS-6063; PF-04554878)

59 Cited Publications

Kundenbewertung

Based on 59 publication(s) in Google Scholar

Defactinib (VS-6063; PF-04554878) is a novel FAK inhibitor with potential antiangiogenic and antineoplastic activities.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.74%
CAS. Nr.: 1073154-85-4
Formel: C₂₀H₂₁F₃N₈O₃S
Molecular Weight:510.49

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Defactinib Chemical Structure

CAS. Nr.: 1073154-85-4

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (59)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Defactinib (VS-6063; PF-04554878) is a novel FAK inhibitor with potential antiangiogenic and antineoplastic activities.

IC₅₀ & Target

FAK^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A375P	GI₅₀	5.94 μM Compound: VS-6063; PF-04554878	Antiproliferative activity against human A375P cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human A375P cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay	[PMID: 34324343]
A549	IC₅₀	4.09 μM Compound: 7	Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 34091209]
BXPC-3	IC₅₀	3.25 μM Compound: 7	Antiproliferative activity against human BxPC-3 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human BxPC-3 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 34091209]
HCT-116	GI₅₀	9.13 μM Compound: VS-6063; PF-04554878	Antiproliferative activity against human HCT-116 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human HCT-116 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay	[PMID: 34324343]
HCT-116	IC₅₀	2.65 μM Compound: 5; VS-6063	Antiproliferative activity against human HCT116 cells overexpressing FAK assessed as reduction in cell viability after 72 hrs by MTS assay Antiproliferative activity against human HCT116 cells overexpressing FAK assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 31129452]
HCT-15	IC₅₀	4.36 μM Compound: 7	Antiproliferative activity against human HCT-15 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human HCT-15 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 34091209]
HEK293	IC₅₀	4.07 μM Compound: 7	Antiproliferative activity against human HEK293 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human HEK293 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 34091209]
HepG2	IC₅₀	3.69 μM Compound: 7	Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 34091209]
HUVEC	IC₅₀	3.24 μM Compound: 7	Antiproliferative activity against human HUVEC cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human HUVEC cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 34091209]
L02	IC₅₀	4.66 μM Compound: 7	Antiproliferative activity against human L02 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human L02 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 34091209]
MCF-10A	IC₅₀	18.42 μM Compound: 5; VS-6063	Cytotoxicity against human MCF10A cells assessed as reduction in cell viability after 72 hrs by MTS assay Cytotoxicity against human MCF10A cells assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 31129452]
MCF7	IC₅₀	5.81 μM Compound: 7	Antiproliferative activity against human MCF-7 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human MCF-7 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 34091209]
MCF7	IC₅₀	8.97 μM Compound: 5; VS-6063	Antiproliferative activity against human MCF7 cells overexpressing FAK assessed as reduction in cell viability after 72 hrs by MTS assay Antiproliferative activity against human MCF7 cells overexpressing FAK assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 31129452]
MDA-MB-231	GI₅₀	11.45 μM Compound: VS-6063; PF-04554878	Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay	[PMID: 34324343]
MDA-MB-231	IC₅₀	3.75 μM Compound: 7	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 34091209]
PANC-1	IC₅₀	3.48 μM Compound: 7	Antiproliferative activity against human PANC-1 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human PANC-1 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 34091209]
PC-3	IC₅₀	>20 μM Compound: 5; VS-6063	Antiproliferative activity against human PC3 cells overexpressing FAK assessed as reduction in cell viability after 72 hrs by MTS assay Antiproliferative activity against human PC3 cells overexpressing FAK assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 31129452]
U-87MG ATCC	IC₅₀	10.21 μM Compound: 5; VS-6063	Antiproliferative activity against human U87MG cells overexpressing FAK assessed as reduction in cell viability after 72 hrs by MTS assay Antiproliferative activity against human U87MG cells overexpressing FAK assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 31129452]

In Vitro

Defactinib (VS-6063) inhibits FAK phosphorylation at the Tyr397 site in a time- and dose-dependent manner. RPPA data shows that Defactinib reduces levels of AKT and YB-1 in taxane-resistant cell lines. The expression of pFAK (Tyr397) is statistically significantly inhibited by Defactinib in a dose-dependent manner in all cell lines. Defactinib inhibits pFAK (Tyr397) expression within 3 hours, with a gradual return of expression by 48 hours^[1].

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

In Vivo

Defactinib (VS-6063) doses of 25 mg/kg twice a day or greater statistically significantly inhibits pFAK (Tyr397) at 3 hours, with return of expression noted by 24 hours. Therefore, administration of Defactinib at 25 mg/kg twice a day is selected as the dosing schedule for subsequent therapy experiments. For therapy experiments, female nude mice bearing HeyA8 tumors in the peritoneal cavity are randomly divided into 4 groups (n=10 per group): 1) vehicle orally twice daily and phosphate-buffered saline intraperitoneally weekly (control); 2) Defactinib 25 mg/kg orally twice daily; 3) PTX intraperitoneally weekly; and 4) both VDefactinib 25 mg/kg orally twice daily and PTX intraperitoneally weekly. There is an 87.4% reduction in tumor weight by PTX monotherapy in the HeyA8 model, and combination therapy resulted in the greatest tumor weight reduction, with a 97.9% reduction (P=0.05 compared with PTX). In the SKOV3ip1 model, a 92.7% tumor weight reduction is observed in the combination group compared with PTX (P<0.001)^[1].

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

Clinical Trial

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

Chemical Information

CAS. Nr. 1073154-85-4
Appearance Solid
Molecular Weight 510.49
Formel C₂₀H₂₁F₃N₈O₃S
Color White to off-white
SMILES

O=C(NC)C1=CC=C(NC2=NC=C(C(F)(F)F)C(NCC3=NC=CN=C3N(C)S(=O)(C)=O)=N2)C=C1
Synonyms

VS-6063; PF-04554878
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (59)

All ELISAIn Vivo ImagingIn Vivo Efficacy StudyWBHistological Imaging/Staining

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Journal Impact Factor

Cancer Cell

2026 May 21:S1535-6108(26)00220-5. PMID: 42167227
Science

The target landscape of clinical kinase drugs. [Abstract]

2017 Dec 1;358(6367):eaan4368. PMID: 29191878
Cancer Commun (Lond)

Galectin 3-binding protein (LGALS3BP) depletion attenuates hepatic fibrosis by reducing transforming growth factor-β1 (TGF-β1) availability and inhibits hepatocarcinogenesis. [Abstract]

2024 Oct;44(10):1106-1129. PMID: 39073023

Defactinib purchased from MedChemExpress. Usage Cited in: Cancer Commun (Lond). 2024 Oct;44(10):1106-1129. [Abstract]

ELISA measurement of active TGF-β1 in the culture medium of Hepa-1c1c7 cells upon rLGALS3BP ± Defactinib (1 μM, 1 h) treatment.
Bioact Mater

Nanoporous titanium implant surface promotes osteogenesis by suppressing osteoclastogenesis via integrin β1/FAKpY397/MAPK pathway. [Abstract]

2021 Jul 1:8:109-123. PMID: 34541390
Bioact Mater

Matrix stiffness modulates tip cell formation through the p-PXN-Rac1-YAP signaling axis. [Abstract]

2021 Jun 1:7:364-376. PMID: 34466738
Cancer Res

Netrin-1 Promotes Pancreatic Tumorigenesis and Innervation through NEO1. [Abstract]

2025 Dec 31. PMID: 41474982
Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Nat Commun

Biomimetic organo-hydrogels reveal the adipose tissue local mechanical anisotropy regulates ovarian cancer invasion. [Abstract]

2025 Sep 29;16(1):8541. PMID: 41022685
Nat Commun

Hydrogel dressing integrating FAK inhibition and ROS scavenging for mechano-chemical treatment of atopic dermatitis. [Abstract]

2023 Apr 29;14(1):2478. PMID: 37120459
Nat Commun

N-glycosylation-defective splice variants of neuropilin-1 promote metastasis by activating endosomal signals. [Abstract]

2019 Aug 16;10(1):3708. PMID: 31420553
ACS Nano

Porous Silicon Nanocarriers Boost the Immunomodulation of Mitochondria-Targeted Bovine Serum Albumins on Macrophage Polarization. [Abstract]

2023 Jan 4;17(2):1036-1053. PMID: 36598186
J Exp Clin Cancer Res

HGF-mediated elevation of ETV1 facilitates hepatocellular carcinoma metastasis through upregulating PTK2 and c-MET. [Abstract]

2022 Sep 16;41(1):275. PMID: 36109787

Defactinib purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2022 Sep 16;41(1):275. [Abstract]

The representative BLI images in the liver were shown 9 weeks after implantation with indicated cells. Defactinib was orally administered at a dose of 25 mg/kg twice a day.

Defactinib purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2022 Sep 16;41(1):275. [Abstract]

The bioluminescent signals were used to show the growth rate of liver tumors. Defactinib was orally administered at a dose of 25 mg/kg twice a day.

Defactinib purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2022 Sep 16;41(1):275. [Abstract]

The number of metastatic lesions in the lung tissues. Defactinib was orally administered at a dose of 25 mg/kg twice a day for 9 weeks.

Defactinib purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2022 Sep 16;41(1):275. [Abstract]

The Overall survival of diferent groups of HCC nude mice. Defactinib was orally administered at a dose of 25 mg/kg twice a day.

Defactinib purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2022 Sep 16;41(1):275. [Abstract]

Representative images of H&E staining of lung samples (indicated by arrowheads) from each group. Defactinib was orally administered at a dose of 25 mg/kg twice a day for 9 weeks.
J Exp Clin Cancer Res

Hippo component YAP promotes focal adhesion and tumour aggressiveness via transcriptionally activating THBS1/FAK signalling in breast cancer. [Abstract]

2018 Jul 28;37(1):175. PMID: 30055645

Defactinib purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Jul 28;37(1):175. [Abstract]

Western blot verified the inhibition of FAK Y397 phosphorylation via Defactinib in MCF7-YAP-S127A and MDA-MB-231 cells.
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
Mol Biomed

Epithelial membrane protein 1 drives hepatic stellate cell activation via the TLN1/FAK cascade in MASLD donor liver transplantation. [Abstract]

2025 Nov 24;6(1):116. PMID: 41284206
Cell Death Dis

Serglycin induces osteoclastogenesis and promotes tumor growth in giant cell tumor of bone. [Abstract]

2021 Sep 23;12(10):868. PMID: 34556636
Phytomedicine

Demethylzeylasteral attenuates hepatic stellate cell activation and liver fibrosis by inhibiting AGAP2 mediated signaling. [Abstract]

2022 Oct:105:154349. PMID: 35905567
Cell Death Discov

Non-enzymatic function of QSOX2 directly regulates the JUNB-ITGB4 axis and enhanced resistance to osimertinib in EGFR-mutation lung adenocarcinoma. [Abstract]

2026 Apr 1;12(1):215. PMID: 41922310
J Orthop Translat

Defactinib attenuates osteoarthritis by inhibiting positive feedback loop between H-type vessels and MSCs in subchondral bone. [Abstract]

2020 May 19:24:12-22. PMID: 32518750
J Transl Med

Increased expression of OPN contributes to idiopathic pulmonary fibrosis and indicates a poor prognosis. [Abstract]

2023 Sep 19;21(1):640. PMID: 37726818
Oncogene

Cooperation between SIX1 and DHX9 transcriptionally regulates integrin-focal adhesion signaling mediated metastasis and sunitinib resistance in KIRC. [Abstract]

2024 Sep;43(39):2951-2969. PMID: 39174859
Oncogene

Stromal nicotinamide N-methyltransferase orchestrates the crosstalk between fibroblasts and tumour cells in oral squamous cell carcinoma: evidence from patient-derived assembled organoids. [Abstract]

2023 Apr;42(15):1166-1180. PMID: 36823377
EMBO J

Ephrin A1 functions as a ligand of EGFR to promote EMT and metastasis in gastric cancer. [Abstract]

2025 Mar;44(5):1464-1487. PMID: 39838173
Cell Mol Gastroenterol Hepatol

MFAP4 Deficiency Attenuates Liver Fibrosis by Regulating Hepatic Stellate Cell Fate through Inhibition of the FAK/PI3K/NFκB Signaling Pathway. [Abstract]

2025;19(10):101548. PMID: 40449846
Cell Mol Gastroenterol Hepatol

Fibrinogen/AKT/Microfilament Axis Promotes Colitis by Enhancing Vascular Permeability. [Abstract]

2021;11(3):683-696. PMID: 33075564
ACS Appl Mater Interfaces

Matrix Stiffness of GelMA Hydrogels Regulates Lymphatic Endothelial Cells toward Enhanced Lymphangiogenesis. [Abstract]

2024 Oct 16;16(41):55130-55141. PMID: 39352138
Anal Chem

TROP2 Promotes Tumor Cell Migration through Downregulation of DSG2 Revealed by Super-Resolution Fluorescence Imaging. [Abstract]

2026 Jan 27;98(3):1901-1914. PMID: 41531208
Sci Data

High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]

2024 Sep 19;11(1):1024. PMID: 39300112
Atherosclerosis

Loss of ADAMTS5 promotes vascular calcification via versican/integrin β1/FAK signal. [Abstract]

2025 May:404:119190. PMID: 40215897
JCI Insight

Focal adhesion proteins confer smooth muscle anoikis resistance and protection against aortic aneurysm and dissection. [Abstract]

2026 Mar 24:e195291. PMID: 41874580
Mol Metab

Sema7A protects against high-fat diet-induced obesity and hepatic steatosis by regulating adipo/lipogenesis. [Abstract]

2023 Apr:70:101698. PMID: 36842496
Cancer Sci

SOX10 Regulates Melanoma Metastasis Through the IRF1-ITGA3/EphA2-FAK Pathway. [Abstract]

2025 Aug 13. PMID: 40808260
Sci Rep

Melatonin attenuates Helicobacter pylori-mediated cholangiocarcinoma-associated fibroblast activation via modulating integrin/FAK signaling pathway. [Abstract]

2025 May 6;15(1):15780. PMID: 40329017
Sci Rep

FAK and Pyk2 activity promote TNF-α and IL-1β-mediated pro-inflammatory gene expression and vascular inflammation. [Abstract]

2019 May 20;9(1):7617. PMID: 31110200
Cell Signal

The role of FAK signaling in early placental development and trophoblast lineage specification in human pregnancy. [Abstract]

2025 Oct:134:111946. PMID: 40553964
Oncol Res

Degradation of FAK-targeting by proteolytic targeting chimera technology to inhibit the metastasis of hepatocellular carcinoma. [Abstract]

2024 Mar 20;32(4):679-690. PMID: 38560575
FASEB J

Inactivation of Focal Adhesion Kinase FAK Rapidly Abrogates Keratinocyte Entry in Mitosis via Rho-Associated Kinase, Resulting in Squamous Differentiation. [Abstract]

2026 Jan 15;40(1):e71405. PMID: 41521614
Bone

PTX3 promotes osteogenic differentiation by triggering HA/CD44/FAK/AKT positive feedback loop in an inflammatory environment. [Abstract]

2022 Jan:154:116231. PMID: 34653679
Mol Carcinog

Focal adhesion kinase confers lenvatinib resistance in hepatocellular carcinoma via the regulation of lysine-deficient kinase 1. [Abstract]

2024 Jan;63(1):173-189. PMID: 37787401
Exp Cell Res

FAK-targeting PROTAC demonstrates enhanced antitumor activity against KRAS mutant non-small cell lung cancer. [Abstract]

2021 Nov 15;408(2):112868. PMID: 34648846
Front Oncol

FAK PROTAC Inhibits Ovarian Tumor Growth and Metastasis by Disrupting Kinase Dependent and Independent Pathways. [Abstract]

2022 Apr 28;12:851065. PMID: 35574330
Placenta

High expression of CX3CL1/CX3CR1 at the mother-fetus interface of preeclampsia inhibits trophoblast invasion and migration. [Abstract]

2024 Aug 21:156:30-37. PMID: 39236525
PLoS One

A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]

2024 Nov 1;19(11):e0308647. PMID: 39485774
Clin Breast Cancer

Inhibitory Impact Of Cinobufagin In Triple-Negative Breast Cancer Metastasis: Involvements Of Macrophage Reprogramming Through Upregulated MME and Inactivated FAK/STAT3 Signaling. [Abstract]

2024 Jun;24(4):e244-e257.e1. PMID: 38378361
Biochem Biophys Res Commun

Plexin D1 negatively regulates macrophage-derived foam cell migration via the focal adhesion kinase/Paxillin pathway. [Abstract]

2024 Sep 17:725:150236. PMID: 38897039
Exp Ther Med

Collagen triple helix repeat containing 1 promotes endometrial cancer cell migration by activating the focal adhesion kinase signaling pathway. [Abstract]

2020 Aug;20(2):1405-1414. PMID: 32742375
J Int Med Res

β1 integrin-mediated multicellular resistance in hepatocellular carcinoma through activation of the FAK/Akt pathway. [Abstract]

2018 Apr;46(4):1311-1325. PMID: 29332411
SSRN

2025 Dec 12.
University of Otago

2025 Oct 7.
bioRxiv

Netrin-1 promotes pancreatic tumorigenesis and innervation through NEO1. [Abstract]

2025 Jul 26:2025.07.22.666009. PMID: 40777309
bioRxiv

Desmoplakin loss leads to PKC-dependent insertion of series sarcomeres and contractile dysfunction in cardiomyocytes. [Abstract]

2025 May 19:2025.05.15.654389. PMID: 40475450
bioRxiv

2024 November 26.
Heliyon

Exosomal CTHRC1 from cancer-associated fibroblasts facilitates endometrial cancer progression via ITGB3/FAK signaling pathway. [Abstract]

2024 Aug 6;10(16):e35727. PMID: 39229506
bioRxiv

Logic-based mechanistic machine learning on high-content images reveals how drugs differentially regulate cardiac fibroblasts. [Abstract]

2023 Oct 23:2023.03.01.530599. PMID: 36909540
Research Square Print

September 13th, 2022.
University of Zürich

2021 Dec.
Research Square Preprint

2021 Aug.
Research Square Preprint

2020 Jun.
Mater Sci Eng C Mater Biol Appl

The unique regulation of implant surface nanostructure on macrophages M1 polarization. [Abstract]

2020 Jan:106:110221. PMID: 31753358

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (97.95 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

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

1.9589 mL

9.7945 mL

19.5890 mL

5 mM

0.3918 mL

1.9589 mL

3.9178 mL

10 mM

0.1959 mL

0.9795 mL

1.9589 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: 2.5 mg/mL (4.90 mM); Suspended solution; Need ultrasonic

Protocol 2

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

Solubility: ≥ 2.08 mg/mL (4.07 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

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: 0.5% CMC-Na/saline water

Solubility: 5 mg/mL (9.79 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
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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 + +
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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

Protokoll

Animal Administration^[1]

Mice^[1]
To determine the antitumor effects of Defactinib, SKOV3ip1, SKOV3-TR, HeyA8, and HeyA8-MDR cells are injected intraperitoneally. One week after tumor cell injection, mice are randomly assigned to 4 groups of 10 mice (control, PTX alone, Defactinib alone, and PTX with Defactinib); treatment is initiated at 3-4 weeks following injection. PTX at 2 mg/kg (SKOV3ip1 and SKOV3-TR) or 2.5 mg/kg (HeyA8 and HeyA8-MDR) is given intraperitoneally weekly; Defactinib at 25 mg/kg is given orally twice every day. Control mice received HBSS intraperitoneally once a week and vehicle orally twice every day. Mice are monitored daily for adverse effects of therapy and are killed on day 35 (SKOV3ip1 or SKOV3-TR), day 28 (HeyA8 or HeyA8-MDR), or when any of the mice seemed moribund. Total body weight, tumor incidence and mass, and the number of tumor nodules are recorded. Tumors are either fixed in formalin or embedded in paraffin or snap frozen in optimal cutting temperature (OCT) compound in liquid nitrogen.

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

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COA (2659 KB)
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Handling Instructions (2659 KB)

Verweise

[1]. Kang Y, et al. Role of focal adhesion kinase in regulating YB-1-mediated resistance in ovarian cancer. J Natl Cancer Inst. 2013 Oct 2;105(19):1485-95. [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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9589 mL	9.7945 mL	19.5890 mL	48.9726 mL
	5 mM	0.3918 mL	1.9589 mL	3.9178 mL	9.7945 mL
	10 mM	0.1959 mL	0.9795 mL	1.9589 mL	4.8973 mL
	15 mM	0.1306 mL	0.6530 mL	1.3059 mL	3.2648 mL
	20 mM	0.0979 mL	0.4897 mL	0.9795 mL	2.4486 mL
	25 mM	0.0784 mL	0.3918 mL	0.7836 mL	1.9589 mL
	30 mM	0.0653 mL	0.3265 mL	0.6530 mL	1.6324 mL
	40 mM	0.0490 mL	0.2449 mL	0.4897 mL	1.2243 mL
	50 mM	0.0392 mL	0.1959 mL	0.3918 mL	0.9795 mL
	60 mM	0.0326 mL	0.1632 mL	0.3265 mL	0.8162 mL
	80 mM	0.0245 mL	0.1224 mL	0.2449 mL	0.6122 mL

Keywords

Defactinib

59 Cited Publications

100 mg Angebot einholen

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Defactinib

Anti-COVID-19 Compound Library

Cytoskeleton Compound Library

Chemical Probe Library

FDA Approved & Pharmacopeial Drug Library

Anti-Pancreatic Cancer Compound Library

Targeted Diversity Library

Rare Diseases Drug Library

Protein-protein Interaction Inhibitor Library

FDA-Approved Anticancer Drug Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Heterocyclic Compound Library

Bioactive Compound Library Max

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

FDA Kinase Inhibitor Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Drug Repurposing Compound Library

Publications Citing Use of MedChemExpress (MCE) Defactinib

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Chemical Information

Publications (59)

Lösungsmittel & Löslichkeit

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Help & FAQs

Complete Stock Solution Preparation Table

Defactinib Related Classifications

HY-12289 Related Classifications