ChemicalBook > CAS DataBase List > Defactinib

Defactinib

Product Name
Defactinib
CAS No.
1073154-85-4
Chemical Name
Defactinib
Synonyms
VS6063;VS-6063;VS 6063;CS-1796;Defactinib;Defactinib (VS-6063;VS-6063; PF-04554878;Defactinib free base;PF-04554878 Defactinib;Defactinib(PF-04554878)
CBNumber
CB82716190
Molecular Formula
C20H21F3N8O3S
Formula Weight
510.49
MOL File
1073154-85-4.mol
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Defactinib Property

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.
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
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N-Bromosuccinimide Price

Cayman Chemical
Product number
17737
Product name
Defactinib
Purity
≥98%
Packaging
1mg
Price
$37
Updated
2024/03/01
Cayman Chemical
Product number
17737
Product name
Defactinib
Purity
≥98%
Packaging
5mg
Price
$116
Updated
2024/03/01
Cayman Chemical
Product number
17737
Product name
Defactinib
Purity
≥98%
Packaging
10mg
Price
$213
Updated
2024/03/01
Cayman Chemical
Product number
17737
Product name
Defactinib
Purity
≥98%
Packaging
25mg
Price
$353
Updated
2024/03/01
Usbiological
Product number
474093
Product name
Defactinib
Packaging
100mg
Price
$1380
Updated
2021/12/16
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Defactinib Chemical Properties,Usage,Production

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.

Uses

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

Defactinib Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from Defactinib manufacturers

Career Henan Chemical Co
Product
Defactinib 1073154-85-4
Price
US $1.00/KG
Min. Order
1KG
Purity
97%
Supply Ability
200kg
Release date
2020-02-01

1073154-85-4, DefactinibRelated Search:


  • Defactinib
  • VS 6063
  • VS6063
  • VS-6063
  • Defactinib(PF-04554878)
  • N-methyl-4-(4-((3-(N-methylmethan-3-ylsulfonamido)pyrazin-2-yl)methylamino)-5-(trifluoromethyl)pyrimidin-2-ylamino)benzamide
  • N-Methyl-4-[[4-[[[3-[methyl(methylsulfonyl)amino]-2-pyrazinyl]methyl]amino]-5-(trifluoromethyl)-2-pyrimidinyl]amino]benzamide
  • N-METHYL-4-(4-((3-(N-METHYLMETHYL SULFON
  • N-methyl-4-[[4-[[3-[methyl(methylsulfonyl)amino]pyrazin-2-yl]methylamino]-5-(trifluoromethyl)pyrimidin-2-yl]amino]benzamide
  • Defactinib (VS-6063
  • N-methyl-4-(4-((3-(N-methylmethylsulfonamido)pyrazin-2-yl)methylamino)-5-(trifluoromethyl)pyrimidin-2-ylamino)benzamide
  • VS-6063; PF-04554878
  • PF-04554878 Defactinib
  • N-methyl-4-((4-(((3-(N-methylmethylsulfonamido)pyrazin-2-yl)methyl)amino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)benzamide Defactinib(PF-04554878)(VS-6063)
  • VS-6063; VS6063; VS 6063; PF04554878; PF-04554878; PF 04554878
  • CS-1796
  • Benzamide, N-methyl-4-[[4-[[[3-[methyl(methylsulfonyl)amino]-2-pyrazinyl]methyl]amino]-5-(trifluoromethyl)-2-pyrimidinyl]amino]-
  • Defactinib free base
  • 1073154-85-4
  • C20H21F3N8O3S
  • Inhibitors
  • API