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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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Defactinib Suppliers

Target molecule Corp.
Tel
857-239-0968
Fax
857-239-8801
Email
service1@targetmol.com
Country
United States
ProdList
2559
Advantage
60
Musechem
Tel
+1-800-259-7612
Fax
+1-800-259-7612
Email
info@musechem.com
Country
United States
ProdList
4660
Advantage
60
TargetMol Chemicals Inc.
Tel
+1-781-999-5354 +1-00000000000
Email
marketing@targetmol.com
Country
United States
ProdList
32161
Advantage
58
InvivoChem
Tel
+1-708-310-1919 +1-13798911105
Fax
708-557-7486
Email
sales@invivochem.cn
Country
United States
ProdList
6391
Advantage
58
Cckinase, Inc.
Tel
+1 (732)236-3202
Email
sales@cckinase.com
Country
United States
ProdList
2738
Advantage
58
BOC Sciences
Tel
+1-631-485-4226
Fax
1-631-614-7828
Email
inquiry@bocsci.com
Country
United States
ProdList
19553
Advantage
58
Aladdin Scientific
Tel
+1-+1(833)-552-7181
Email
sales@aladdinsci.com
Country
United States
ProdList
57505
Advantage
58
Aceschem Inc.
Tel
+1-817863-6948 +1-(817)863-6948
Email
sales@aceschem.com
Country
United States
ProdList
19632
Advantage
58
ApexBio Technology
Tel
--
Fax
--
Email
sales@apexbt.com
Country
United States
ProdList
6251
Advantage
58
BOC Sciences
Tel
16314854226
Email
info@bocsci.com
Country
United States
ProdList
9923
Advantage
65
Focus Biomolecules
Tel
--
Fax
--
Email
sales@focusbiomolecules.com
Country
United States
ProdList
1284
Advantage
58
Cayman Chemical Company
Tel
--
Fax
--
Email
cayman@caymanchem.com
Country
United States
ProdList
6213
Advantage
81
Axon Medchem LLC
Tel
--
Fax
--
Email
info@axonmedchem.com
Country
United States
ProdList
763
Advantage
58
ChemieTek
Tel
--
Fax
--
Email
info@chemietek.com
Country
United States
ProdList
219
Advantage
50
LKT Laboratories, Inc.
Tel
--
Fax
--
Email
info@lktlabs.com
Country
United States
ProdList
2164
Advantage
64
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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