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.
Synonym
LXG6403; LXG-6403; LXG 6403;
IUPAC/Chemical Name
N-[4-[[4-(2-Amino-4-methylthiazol-5-yl)thiazol-2-yl]amino]phenyl]acetamide
InChi Key
DCUSBOBFLJMFTB-UHFFFAOYSA-N
InChi Code
InChI=1S/C15H15N5OS2/c1-8-13(23-14(16)17-8)12-7-22-15(20-12)19-11-5-3-10(4-6-11)18-9(2)21/h3-7H,1-2H3,(H2,16,17)(H,18,21)(H,19,20)
SMILES Code
CC(NC1=CC=C(NC2=NC(C3=C(C)N=C(N)S3)=CS2)C=C1)=O
Appearance
To be determined
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as a non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark, and at 0 -4 °C for short term (days to weeks) or -20 °C for long term(months to years).
Solubility
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
Stock Solution Storage
0 - 4 °C for short term (days to weeks), or -20 °C for long term (months).
China
