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SML4296

LXG6403

≥98% (HPLC), powder, LOX inhibitor

Synonym(s):

N-[4-[[4-(2-amino-4-methyl-thiazol-5-yl)thiazol-2-yl]amino]phenyl]acetamide

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About This Item

Empirical Formula (Hill Notation):
C15H15N5OS2
CAS Number:
315705-04-5
Molecular Weight:
345.44
Assay:
≥98% (HPLC)
Form:
powder
Storage condition:
desiccated, protect from light
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Quality Segment

100

assay

≥98% (HPLC)

form

powder

storage condition

desiccated, protect from light

color

white to dark brown

solubility

DMSO: 2 mg/mL

storage temp.

-10 to -25°C

General description

LXG6403 is an orally available, cell penetrant, highly potent and well tolerated Lysyl oxidase (LOX) competitive and irreversible inhibitor (IC50 = 1.3 µM) that sensitizing solid tumors to chemotherapy.

Application

LXG6403 may be used to study the effects of LOX inhibition in 3D collagen I-embedded triple-negative breast cancer (TNBC) cell lines and patient-derived xenograft (PDX) organoids.

Biochem/physiol Actions

LXG6403 exhibits ~3.5-fold specificity for LOX compared to LOXL2 while not inhibiting LOXL1. LXG6403 reduces solid tumors stiffens through rearrangement of tumor extracellular matrix (EMC), collagen content and crosslinking leading to better drug penetration. It appears that LXG6403 sensitizes tumors to chemotherapy through induction of ROS and DNA damage, and inhibition of FAK signaling followed by G1 arrest and apoptosis.

Disclaimer

Hygroscopic Store with dessicant

Storage Class

11 - Combustible Solids

flash_point_f

Not applicable

flash_point_c

Not applicable

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