AU-15330 | SWI/SNF ATPase PROTAC | Probechem Biochemicals

Chemical Structure : AU-15330

CAS No.: 2380274-50-8

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AU-15330 (AU15330)

货号: PC-72798Not For Human Use, Lab Use Only.

AU-15330 (AU15330) is a highly specific and VHL-dependent PROTAC degrader of SWI/SNF ATPase components (SMARCA2, SMARCA4 and PBRM1), shows preferential cytotoxicity in enhancer-binding transcription factor-addicted cancers at low nanomolar concentrations.

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5 mg	￥2480	In stock
10 mg	￥3980	In stock
25 mg	￥5880	In stock
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100 mg		Get quote

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生物&药学活性

AU-15330 (AU15330) is a highly specific and VHL-dependent PROTAC degrader of SWI/SNF ATPase components (SMARCA2, SMARCA4 and PBRM1), shows preferential cytotoxicity in enhancer-binding transcription factor-addicted cancers at low nanomolar concentrations.
The PROTAC degrader, AU-15330, comprising a bait moiety that binds the bromodomain in SMARCA2 and SMARCA4 and a ligand moiety for the von Hippel–Lindau (VHL) ubiquitin ligase.
Treatment of several cell lines with AU-15330 led to time and dose-dependent degradation of SMARCA2, SMARCA4 and PBRM1, exhibited preferential cytotoxicity in enhancer-binding transcription factor-driven cancers.
AR and FOXA1-driven prostate cancer cells to be preferentially sensitive to AU-15330 (IC50<100 nM).
AU-15330 inhibits tumour growth in preclinical models of CRPC and synergizes with enzalutamide.
Inactivation of SWI/SNF ATPase induces a rapid, near-complete and targeted loss of chromatin accessibility at the core-enhancer circuitry of AR, FOXA1, MYC and ERG, thereby attenuating their cancer-promoting transcriptional programs and tempering the enhancer-wired supra-physiologic expression of driver oncogenes.

物理化学性质&存储条件

分子量	755.939
分子式	C39H49N9O5S
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	(2S,4R)-1-((S)-2-(2-(4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)acetamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide

参考文献

1. Lanbo Xiao, et al. Nature. 2022 Jan;601(7893):434-439.

AU-15330 (AU15330)

生物&药学活性

物理化学性质&存储条件

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AU-15330 (AU15330)

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