ACXT-3102 (SW V-49) | Ferroptosis inducer, xCT inhibitor

Chemical Structure : ACXT-3102

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ACXT-3102 (SW V-49, ACXT3102)

货号: PC-28285Not For Human Use, Lab Use Only.

ACXT-3102 (SW V-49) is a cancer-specific drug conjugate and ferroptosis inducer consisting of a pro-apoptotic sigma-2 ligand as a delivery moiety (SV119), linked to an inhibitor of the cystine antiporter xCT (des-methyl Erastin, dm-Erastin), exhibits potent, targeted therapeutic for pancreatic cancer cells.

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生物&药学活性

ACXT-3102 (SW V-49) is a cancer-specific drug conjugate and ferroptosis inducer consisting of a pro-apoptotic sigma-2 ligand as a delivery moiety (SV119), linked to an inhibitor of the cystine antiporter xCT/SLC7A11 (des-methyl Erastin, dm-Erastin), exhibits potent, targeted therapeutic for pancreatic cancer cells.
SW V-49 overcomes the chemotherapeutic plateau of dm-Erastin via enhanced drug uptake
shows potent cytotoxic response effect against PANC-1 cells with IC50 of 4.1 uM, 17-fold more effective than an equimolar mix of SV119 and dm-Erastin.
SW V-49 inhibits cell viability of multiple human pancreatic cancer organoid cultures with IC50 of 1.84 uM.
SW V-49 reduces tumor growth and improves survival in syngeneic and patient-derived xenograft models of pancreatic cancer.
SW V-49 competes for the sigma-2 receptor with known sigma-2 binders and activates cargo-specific signaling pathways.

物理化学性质&存储条件

分子量	914.14
分子式	C53H67N7O7
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(1R,3r,5S)-9-(6-((4-(2-(4-((3-(2-ethoxyphenyl)-4-oxo-3,4-dihydroquinazolin-2-yl)methyl)piperazin-1-yl)-2-oxoethoxy)benzyl)amino)hexyl)-9-azabicyclo[3.3.1]nonan-3-yl (2-methoxy-5-methylphenyl)carbamate

参考文献

1. Kerri A Ohman, et al. Oncotarget. 2016 Jun 7;7(23):33529-41.

2. Brashears CB, et al. Clin Cancer Res. 2022 Aug 15;28(16):3573-3589.

ACXT-3102 (SW V-49, ACXT3102)

生物&药学活性

物理化学性质&存储条件

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ACXT-3102 (SW V-49, ACXT3102)

生物&药学活性

物理化学性质&存储条件

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