Defactinib
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Defactinib is a selective, and orally active focal adhesion kinase (FAK) inhibitor [1].
FAK is a nonreceptor tyrosine kinase involved in many oncogenic pathways. Increased expression of FAK has been observed in a number of tumor types, including breast, colon, and ovarian cancers. It has been reported that FAK inhibition can sensitize cancer cells to chemotherapy [1].
In Taxane-sensitive (HeyA8) and Taxane-resistant (HeyA8-MDR) cell lines, Defactinib at 0 ~ 10 μM significantly inhibited pFAK (Tyr397) expression in a dose-dependent manner. In addition, simultaneous exposure to doses of Paclitaxel and Defactinib at ratios of 1:1000 for HeyA8 and 1:10 for HeyA8-MDR showed a synergistic inhibitory effect on cell growth [1].
In mice bearing HeyA8 tumors, there was a 97.9% reduction in tumor weight by the combination therapy (Defactinib: 25 mg/kg orally twice daily, Paclitaxel: 2.5 mg/kg intraperitoneally weekly), compared with an 87.4% reduction in tumor weight by Paclitaxel monotherapy. In the SKOV3ip1 model, a 92.7% tumor weight reduction was observed in the combination group (Defactinib: 25 mg/kg orally twice daily, Paclitaxel: 2 mg/kg intraperitoneally weekly) [1].
Reference:
[1]. Kang Y, Hu W, Ivan C, et al. Role of focal adhesion kinase in regulating YB-1-mediated paclitaxel resistance in ovarian cancer. Journal of the National Cancer Institute, 2013, 105(19): 1485-1495.
| Storage | Store at -20°C |
| M.Wt | 510.49 |
| Cas No. | 1073154-85-4 |
| Formula | C20H21F3N8O3S |
| Solubility | insoluble in EtOH; insoluble in H2O; ≥160.2 mg/mL in DMSO |
| Chemical Name | N-methyl-4-[[4-[[3-[methyl(methylsulfonyl)amino]pyrazin-2-yl]methylamino]-5-(trifluoromethyl)pyrimidin-2-yl]amino]benzamide |
| SDF | Download SDF |
| Canonical SMILES | CNC(=O)C1=CC=C(C=C1)NC2=NC=C(C(=N2)NCC3=NC=CN=C3N(C)S(=O)(=O)C)C(F)(F)F |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| Cell experiment:[1] | |
|
Cell lines |
Taxane-sensitive (HeyA8) and taxane-resistant (HeyA8-MDR) human epithelial ovarian cancer |
|
Reaction Conditions |
0 ~ 10 μM defactinib |
|
Applications |
In HeyA8 and HeyA8-MDR cell lines, defactinib at 0 ~ 10 μM significantly inhibited pFAK (Tyr397) expression in a dose-dependent manner. In addition, simultaneous exposure to doses of paclitaxel and defactinib at ratios of 1:1000 for HeyA8 and 1:10 for HeyA8-MDR showed a synergistic inhibitory effect on cell growth. |
| Animal experiment:[1] | |
|
Animal models |
Female athymic nude mice (aged 8 ~ 12 weeks) |
|
Dosage form |
25 mg/kg Twice daily by oral route |
|
Applications |
In mice bearing HeyA8 tumors, there was a 97.9% reduction in tumor weight by the combination therapy (defactinib: 25 mg/kg orally twice daily; paclitaxel: 2.5 mg/kg intraperitoneally weekly), compared with an 87.4% reduction in tumor weight by paclitaxel monotherapy. In the SKOV3ip1 model, a 92.7% tumor weight reduction was observed in the combination group (defactinib: 25 mg/kg orally twice daily; paclitaxel: 2 mg/kg intraperitoneally weekly). |
|
Note |
The technical data provided above is for reference only. |
|
References: 1. Kang Y, Hu W, Ivan C, et al. Role of focal adhesion kinase in regulating YB-1-mediated paclitaxel resistance in ovarian cancer. Journal of the National Cancer Institute, 2013, 105(19): 1485-1495. |
|
质量控制和MSDS
- 批次:
化学结构
