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
| 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) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| NFPA 704 |
|
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 |
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
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32715 | 60 |
| Hubei Jusheng Technology Co.,Ltd. | 18871490254 | linda@hubeijusheng.com | CHINA | 28180 | 58 |
| BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19553 | 58 |
| career henan chemical co | +86-0371-86658258 15093356674; | factory@coreychem.com | China | 29826 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6313 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10523 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
| LEAP CHEM CO., LTD. | +86-852-30606658 | market18@leapchem.com | China | 24738 | 58 |
| Coresyn Pharmatech Co., Ltd. | +86-571-86626709 +86-18157142896 | cbc@coresyn.com | China | 9991 | 58 |
View Lastest Price from Defactinib manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2020-02-02 | Defactinib
1073154-85-4
|
US $1.00 / KG | 1KG | 97% | 200kg | Career Henan Chemical Co |
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- Defactinib
1073154-85-4
- US $1.00 / KG
- 97%
- Career Henan Chemical Co