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LXG6403

LXG6403 Struktur
315705-04-5
CAS-Nr.
315705-04-5
Englisch Name:
LXG6403
Synonyma:
LXG6403;LXG6403 (Lysyl oxidase inhibitor);Acetamide, N-[4-[(2′-amino-4′-methyl[4,5′-bithiazol]-2-yl)amino]phenyl]-
CBNumber:
CB516565736
Summenformel:
C15H15N5OS2
Molgewicht:
345.45
MOL-Datei:
315705-04-5.mol

LXG6403 Eigenschaften

Dichte
1.453±0.06 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted)
storage temp. 
-20°C 12 Months; 4°C 6 Months
L?slichkeit
10 mM in DMSO
pka
14.605±0.70(predicted)
Aggregatzustand
powder
Farbe
white to dark brown
Aussehen
Solid

Sicherheit

LXG6403 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

LXG6403 is a potent, competitive and irreversible lysosomal oxidase (LOX) inhibitor that effectively inhibits cytosolic LOX activity in MDA-MB-231 cells, with an IC50 value of 1.3 uM. LXG6403 is 3.5 times more specific for LOX than LOXL2, while it has no inhibitory effect on LOXL1. LXG6403 has good pharmacokinetic properties and can change the structure of ECM/collagen and reduce the hardness of tumour.

Biologische Aktivit?t

LXG6403 is a highly potent, irreversible lysyl oxidase (LOX) inhibitor, inhibits cellular LOX activity efficiently in MDA-MB-231 cells with IC50 of 1.3 uM, >3-fold selective over LOXL2 and no activity against LOXL1. LXG6403 inhibits cellular LOX activity with IC50 values of 1.3 μM, 1.43 μM, 4.14 μM, and 3.0 μM in MDA-MB-231, HCC143, Hs-578-T, and HCC1937 cells.
LXG6403 enhances chemoresponse in 3D cultures of TNBC cell lines and PDX organoids.
LXG6403 diminishes collagen crosslinking/deposition and increases drug penetration in 3D culture, inhibiting FAK signaling and potentiating ROS/DNA damage axis.
LXG6403 rewires collagen architecture/signaling, overcomes doxorubicin resistance in chemoresistant TNBC PDXs in vivo.

Pharmakokinetik

LXG6403 shows favorable pharmacokinetic properties, globally changes ECM/collagen architecture, and reduces tumor stiffness. This leads to better drug penetration, inhibits FAK signaling, and induces ROS/DNA damage, G1 arrest, and apoptosis in chemoresistant triple-negative breast cancer (TNBC) cell lines, PDX organoids, and in vivo[1].

Einzelnachweise

[1] Cetin, M., Saatci, O., Rezaeian, A.-H., Rao, C. N., Beneker, C., Sreenivas, K., Taylor, H., Pederson, B., Chatzistamou, I., Buckley, B., Lessner, S., Angel, P., McInnes, C., Sahin, O. (2024). A highly potent bi-thiazole inhibitor of LOX rewires collagen architecture and enhances chemoresponse in triple-negative breast cancer. Cell Chemical Biology, 31 11, Pages 1926-1941.e11. https://doi.org/10.1016/j.chembiol.2024.06.012

LXG6403 Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


LXG6403 Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Global( 9)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
Hinova Pharma
+86-18190684138 +86-18190684138
xhchen00241@hinovapharma.com China 61 58
Shaanxi Dideu New Materials Co. Ltd
+86-18192503167 18192503167
1036@dideu.com China 9207 58
HINOVA PHARMACEUTICALS INC. 18244267397
cxinghua127@163.com China 130 58
Shanghai Lollane Biological Technology Co.,Ltd. 021-52996696,15000506266 15000506266
China 4849 55
Shanghai Chaolan Chemical Technology Center QQ:65489617 19372819560
Sales@ATKchemical.com China 9625 58
ShangHai ChuanQian Chemcial Technique Centre 15869524721
3525679403@qq.com China 4334 58
Nantong QuanYi Biotechnology Co., Ltd 0513-66337626 18051384581
sales@chemhifuture.com China 6000 58
Shanghai Aitixi Biotechnology Co., Ltd 18721763493 18721763493;
2493172863@qq.com China 995 58
Afflon Pharmaceutical (Sichuan) Co., Ltd. 17336178085
1684779048@qq.com China 2085 58

  • LXG6403
  • Acetamide, N-[4-[(2′-amino-4′-methyl[4,5′-bithiazol]-2-yl)amino]phenyl]-
  • LXG6403 (Lysyl oxidase inhibitor)
  • 315705-04-5
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