Defactinib
Based on 59 publication(s) in Google Scholar
Defactinib (VS-6063; PF-04554878) is a novel FAK inhibitor with potential antiangiogenic and antineoplastic activities.
For research use only. We do not sell to patients.
- Purity: 99.74%
- CAS No.: 1073154-85-4
- Formula: C20H21F3N8O3S
- Molecular Weight:510.49
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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Biological Activity
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Publications Citing Use of MedChemExpress (MCE) Defactinib
More- Cancer Cell. 2026 May 21:S1535-6108(26)00220-5.
- Science. 2017 Dec 1;358(6367):eaan4368. [Abstract]
- Cancer Commun (Lond). 2024 Oct;44(10):1106-1129. [Abstract]
- Bioact Mater. 2021 Jul 1:8:109-123. [Abstract]
- Bioact Mater. 2021 Jun 1:7:364-376. [Abstract]
- Cancer Res. 2025 Dec 31. [Abstract]
- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Nat Commun. 2025 Sep 29;16(1):8541. [Abstract]
- Nat Commun. 2023 Apr 29;14(1):2478. [Abstract]
- Nat Commun. 2019 Aug 16;10(1):3708. [Abstract]
- ACS Nano. 2023 Jan 4;17(2):1036-1053. [Abstract]
- J Exp Clin Cancer Res. 2022 Sep 16;41(1):275. [Abstract]
- J Exp Clin Cancer Res. 2018 Jul 28;37(1):175. [Abstract]
- Sci Adv. 2026 Jan 30;12(5):eady8382. [Abstract]
- Mol Biomed. 2025 Nov 24;6(1):116. [Abstract]
- Cell Death Dis. 2021 Sep 23;12(10):868. [Abstract]
- Phytomedicine. 2022 Oct:105:154349. [Abstract]
- Cell Death Discov. 2026 Apr 1;12(1):215. [Abstract]
- J Orthop Translat. 2020 May 19:24:12-22. [Abstract]
- J Transl Med. 2023 Sep 19;21(1):640. [Abstract]
- Oncogene. 2024 Sep;43(39):2951-2969. [Abstract]
- Oncogene. 2023 Apr;42(15):1166-1180. [Abstract]
- EMBO J. 2025 Mar;44(5):1464-1487. [Abstract]
- Cell Mol Gastroenterol Hepatol. 2025;19(10):101548. [Abstract]
- Cell Mol Gastroenterol Hepatol. 2021;11(3):683-696. [Abstract]
- ACS Appl Mater Interfaces. 2024 Oct 16;16(41):55130-55141. [Abstract]
- Anal Chem. 2026 Jan 27;98(3):1901-1914. [Abstract]
- Sci Data. 2024 Sep 19;11(1):1024. [Abstract]
- Atherosclerosis. 2025 May:404:119190. [Abstract]
- JCI Insight. 2026 Mar 24:e195291. [Abstract]
- Mol Metab. 2023 Apr:70:101698. [Abstract]
- Cancer Sci. 2025 Aug 13. [Abstract]
- Sci Rep. 2025 May 6;15(1):15780. [Abstract]
- Sci Rep. 2019 May 20;9(1):7617. [Abstract]
- Cell Signal. 2025 Oct:134:111946. [Abstract]
- Oncol Res. 2024 Mar 20;32(4):679-690. [Abstract]
- FASEB J. 2026 Jan 15;40(1):e71405. [Abstract]
- Bone. 2022 Jan:154:116231. [Abstract]
- Mol Carcinog. 2024 Jan;63(1):173-189. [Abstract]
- Exp Cell Res. 2021 Nov 15;408(2):112868. [Abstract]
- Front Oncol. 2022 Apr 28;12:851065. [Abstract]
- Placenta. 2024 Aug 21:156:30-37. [Abstract]
- PLoS One. 2024 Nov 1;19(11):e0308647. [Abstract]
- Clin Breast Cancer. 2024 Jun;24(4):e244-e257.e1. [Abstract]
- Biochem Biophys Res Commun. 2024 Sep 17:725:150236. [Abstract]
- Exp Ther Med. 2020 Aug;20(2):1405-1414. [Abstract]
- J Int Med Res. 2018 Apr;46(4):1311-1325. [Abstract]
- SSRN. 2025 Dec 12.
- University of Otago. 2025 Oct 7.
- bioRxiv. 2025 Jul 26:2025.07.22.666009. [Abstract]
- bioRxiv. 2025 May 19:2025.05.15.654389. [Abstract]
- bioRxiv. 2024 November 26.
- Heliyon.2024 Aug 6;10(16):e35727. [Abstract]
- bioRxiv. 2023 Oct 23:2023.03.01.530599. [Abstract]
- 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. 2020 Jan:106:110221. [Abstract]
Customer Validation & Images
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ELISA
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In Vivo Efficacy Study
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In Vivo Efficacy Study
Biological Activity
FAK[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A375P | GI50 |
5.94 μM
Compound: VS-6063; PF-04554878
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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
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[PMID: 34324343] |
| A549 | IC50 |
4.09 μM
Compound: 7
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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
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[PMID: 34091209] |
| BXPC-3 | IC50 |
3.25 μM
Compound: 7
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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
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[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
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[PMID: 34324343] |
| HCT-116 | IC50 |
2.65 μM
Compound: 5; VS-6063
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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
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[PMID: 31129452] |
| HCT-15 | IC50 |
4.36 μM
Compound: 7
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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
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[PMID: 34091209] |
| HEK293 | IC50 |
4.07 μM
Compound: 7
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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
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[PMID: 34091209] |
| HepG2 | IC50 |
3.69 μM
Compound: 7
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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
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[PMID: 34091209] |
| HUVEC | IC50 |
3.24 μM
Compound: 7
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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
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[PMID: 34091209] |
| L02 | IC50 |
4.66 μM
Compound: 7
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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
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[PMID: 34091209] |
| MCF-10A | IC50 |
18.42 μM
Compound: 5; VS-6063
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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
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[PMID: 31129452] |
| MCF7 | IC50 |
5.81 μM
Compound: 7
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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
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[PMID: 34091209] |
| MCF7 | IC50 |
8.97 μM
Compound: 5; VS-6063
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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
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[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
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[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
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[PMID: 34091209] |
| PANC-1 | IC50 |
3.48 μM
Compound: 7
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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
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[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
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[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] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1073154-85-4
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Appearance Solid
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Molecular Weight 510.49
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Formula C20H21F3N8O3S
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Color White to off-white
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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
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Synonyms
VS-6063; PF-04554878
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (59)
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Journal Impact Factor
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Most Recent
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Science
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.
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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
2021 Jun 1:7:364-376. PMID: 34466738 -
Cancer Res
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.
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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.
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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
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
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
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
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 -
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bioRxiv
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 -
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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 -
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Mater Sci Eng C Mater Biol Appl
2020 Jan:106:110221. PMID: 31753358
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Add each solvent one by one: 0.5% CMC-Na/saline water
Solubility: 5 mg/mL (9.79 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
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.
| 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 |
Defactinib Related Classifications
HY-12289 Related Classifications
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