LXG6403 is a potent, irreversible lysyl oxidase (LOX) inhibitor with an IC₅₀ of 1.3 μM in MDA-MB-231 cells, demonstrating approximately 3.5-fold selectivity over LOXL2 and no activity against LOXL1. It effectively inhibits LOX activity across multiple triple-negative breast cancer (TNBC) cell lines, including HCC143, Hs-578-T, and HCC1937, with IC₅₀ values below 5 μM. In preclinical models, LXG6403 enhances chemosensitivity to agents such as doxorubicin, cisplatin, and paclitaxel by disrupting collagen crosslinking, thereby reducing tumor stiffness, improving drug penetration, inhibiting FAK signaling, and inducing ROS-mediated DNA damage leading to G1 arrest and apoptosis. Notably, in the TM01278 TNBC patient-derived xenograft model, LXG6403 overcame doxorubicin resistance without significant toxicity, underscoring its potential as a therapeutic agent in LOX-driven, chemoresistant cancers
MedKoo Cat#: 556390
Name: LXG6403
CAS#: 315705-04-5
Chemical Formula: C15H15N5OS2
Exact Mass: 345.0718
Molecular Weight: 345.44
Elemental Analysis: C, 52.16; H, 4.38; N, 20.27; O, 4.63; S, 18.56
The following data is based on the product molecular weight 345.44 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
