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Defactinib

CAS No.
1073154-85-4
Chemical Name:
Defactinib
Synonyms
VS6063;VS-6063;VS 6063;CS-1796;Defactinib;Defactinib (VS-6063;Defactinib free base;VS-6063; PF-04554878;PF-04554878 Defactinib;Defactinib(PF-04554878)
CBNumber:
CB82716190
Molecular Formula:
C20H21F3N8O3S
Molecular Weight:
510.49
MDL Number:
MOL File:
1073154-85-4.mol
Last updated:2023-06-30 15:45:59

Defactinib Properties

Density 1.495±0.06 g/cm3(Predicted)
storage temp. -20°C (des.)
solubility Soluble in DMSO (up to at least 25mg/ml)
pka 15.16±0.46(Predicted)
form solid
color White
Stability Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
FDA UNII 53O87HA2QU
NCI Drug Dictionary defactinib

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
NFPA 704
0
2 0

Defactinib price More Price(23)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 17737 Defactinib ≥98% 1073154-85-4 1mg $37 2024-03-01 Buy
Cayman Chemical 17737 Defactinib ≥98% 1073154-85-4 5mg $116 2024-03-01 Buy
Cayman Chemical 17737 Defactinib ≥98% 1073154-85-4 10mg $213 2024-03-01 Buy
Cayman Chemical 17737 Defactinib ≥98% 1073154-85-4 25mg $353 2024-03-01 Buy
Usbiological 474093 Defactinib 1073154-85-4 100mg $1380 2021-12-16 Buy
Product number Packaging Price Buy
17737 1mg $37 Buy
17737 5mg $116 Buy
17737 10mg $213 Buy
17737 25mg $353 Buy
474093 100mg $1380 Buy

Defactinib Chemical Properties,Uses,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

Global( 116)Suppliers
Supplier Tel Email Country ProdList Advantage
ATK CHEMICAL COMPANY LIMITED
+undefined-21-51877795 ivan@atkchemical.com China 32951 60
Hubei Jusheng Technology Co.,Ltd.
18871490254 linda@hubeijusheng.com CHINA 28172 58
BOC Sciences
+1-631-485-4226 inquiry@bocsci.com United States 19553 58
career henan chemical co
+86-0371-86658258 +8613203830695 factory@coreychem.com China 29815 58
TargetMol Chemicals Inc.
+1-781-999-5354 +1-00000000000 marketing@targetmol.com United States 32063 58
HANGZHOU CLAP TECHNOLOGY CO.,LTD
86-571-88216897,88216896 13588875226 sales@hzclap.com CHINA 6312 58
Zhejiang J&C Biological Technology Co.,Limited
+1-2135480471 +1-2135480471 sales@sarms4muscle.com China 10473 58
InvivoChem
+1-708-310-1919 +1-13798911105 sales@invivochem.cn United States 6391 58
LEAP CHEM CO., LTD.
+86-852-30606658 market18@leapchem.com China 24727 58
Coresyn Pharmatech Co., Ltd.
+86-571-86626709 +86-18157142896 cbc@coresyn.com China 9984 58

View Lastest Price from Defactinib manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Defactinib pictures 2020-02-02 Defactinib
1073154-85-4
US $1.00 / KG 1KG 97% 200kg Career Henan Chemical Co
  • Defactinib pictures
  • Defactinib
    1073154-85-4
  • US $1.00 / KG
  • 97%
  • Career Henan Chemical Co

Defactinib Spectrum

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