Defactinib
Defactinib (CAS 1073154-85-4) is an orally bioavailable, selective inhibitor of focal adhesion kinase (FAK), a nonreceptor tyrosine kinase implicated in multiple oncogenic signaling pathways. Elevated levels of FAK are observed in various malignancies such as breast, colon, and ovarian cancers, and its inhibition may enhance sensitivity of cancer cells to chemotherapeutic agents. In ovarian cancer cell lines (HeyA8 and HeyA8-MDR), Defactinib dose-dependently reduces phosphorylated FAK (Tyr397) levels and demonstrates synergistic anti-tumor activity when combined with Paclitaxel. In mouse tumor models, this combined regimen significantly suppresses tumor growth, indicating Defactinib's potential value in cancer therapy research.
| 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 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment:[1] | |
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Cell lines |
Taxane-sensitive (HeyA8) and taxane-resistant (HeyA8-MDR) human epithelial ovarian cancer cell lines |
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Reaction Conditions |
0 ~ 10 μM defactinib |
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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] | |
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Animal models |
Female athymic nude mice (aged 8 ~ 12 weeks) |
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Dosage form |
25 mg/kg Twice daily by oral route |
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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). |
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Note |
The technical data provided above is for reference only. |
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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. |
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Quality Control & MSDS
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Chemical structure
