Defactinib
- CAS NO.:1073154-85-4
- Empirical Formula: C20H21F3N8O3S
- Molecular Weight: 510.49
- SAFETY DATA SHEET (SDS)
- Update Date: 2023-06-30 15:45:59
What is Defactinib?
Description
Focal adhesion kinase (FAK) is a non-receptor tyrosine kinase that plays a vital role in many oncogenic pathways. Defactinib is a dose-dependent inhibitor of FAK, with maximal inhibition of FAK autophosphorylation in cells achieved at 10 μM. It is less effective against the related kinase PYK2. Defactinib restores the chemosensitivity of taxane-resistant cells to paclitaxel , although it is not cytotoxic alone. Defactinib decreases YB-1 phosphorylation and nuclear accumulation in an Akt-dependent manner. It is orally bioavailable, inhibiting FAK and augmenting paclitaxel action in suppressing the growth and number of ovarian cancer cell tumors in mice.
The Uses of Defactinib
Defactinib is a selective and orally active FAK inhibitor phase 2. Used in treating cancer patients as it decreases proliferation and increases apoptosis.
storage
Store at -20°C
References
1) Jones?et al.?(2015),?A phase I study of VS-6063, a second-generation focal adhesion kinase inhibitor, in patients with advanced solid tumors;?Invest. New Drugs?33?1100 2) Kolev?et al.?(2017),?Inhibition of FAK kinase activity preferentially targets cancer stem cells;?Oncotarget?8?51733 3) Marcucci?et al.?(2016),?Anti-Cancer Stem-like Cell Compounds in Clinical Development – An Overview and Critical Appraisal;?Front. Oncol.?6?115 4) Ring?et al.?(2015),?FAK/PYK2 inhibitors defactinib and VS-4718 enhance immune checkpoint inhibitor efficacy;?J. Immunother. Cancer?3?354 5) NCT02546531 6) Jiang?et al.?(2016),?Targeting Focal Adhesion Kinase Renders Pancreatic Cancers Responsive to Checkpoint Immunotherapy;?Nat. Med.?22?851
Properties of Defactinib
Density | 1.495±0.06 g/cm3(Predicted) |
storage temp. | -20°C (des.) |
solubility | Soluble in DMSO (up to at least 25mg/ml) |
form | solid |
pka | 15.16±0.46(Predicted) |
color | White |
Stability: | Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
Safety information for Defactinib
Computed Descriptors for Defactinib
New Products
2,2-diethoxyethanethioamide Tubulysin A (2S,4R)-4-amino-2-methyl-5-phenylpentanoic acid hydrochloride Tubulysin I Tubulysin M Diethyl Aluminium Cyanide (1.0 M in Toluene) 2,2-Difluoropropylamine hydrochloride 1-(1,1-Difluoroethyl)-2-fluorobenzene tetrahydro-4-methyl-2H-pyran Isoxazole, 3-[[[5-(difluoromethoxy)-1-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl]methyl]thio]-4,5-dihydro-5,5-dimethyl- 1,2,3,6-TETRAHYDROPYRIDINE HYDROCHLORIDE 4,4-DIFLUOROPIPERIDINE (1R,2S)-2-(3,4-Difluorophenyl)cyclopropanamine Fuel shell Imeglimin Hydrochloride IH 2-(1-(Mercaptomethyl) cyclopropyl) acetonitrile 2-[[(3aR,4S,6R,6aS)-6-Aminotetrahydro-2,2-dimethyl-4H-cyclopenta-1,3-dioxol-4-yl]oxy]ethanol ethanedioate Calcium Sodium Phosphosilicate IH 5-(piperazin-1-yl) benzofuran-2- carboxamide (+/-)-2, 6-Diamino-4,5,6,7 -tetrahydro Benzothiazole Magnesium Trisilicate Latanoprostene Bunod Lubiprostone Flame Retardant Zinc BorateRelated products of tetrahydrofuran
You may like
-
Defactinib >95% CAS 1073154-85-4View Details
1073154-85-4 -
Fuel shell 98%View Details
-
4,6-dichloro-2-propylthiopyrimidine-5-amine 145783-15-9 98%View Details
145783-15-9 -
Hydrogen Gas 98%View Details
-
590-17-0 Bromoacetonitrile 98%View Details
590-17-0 -
151767-02-1 Montelukast Sodium IP/USP 98%View Details
151767-02-1 -
Valacyclovir Hydrochloride IH 98%View Details
124832-27-5 -
2-[2-[3(S)-3[2-(7-chloro-2-quinolinyl) ethenyl] phenyl-3- hydroxyl propyl] phenyl]-2-propanol 98%View Details
142569-70-8