A947 | SMARCA2 PROTAC | Probechem Biochemicals

Chemical Structure : A947

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A947 (A-947)

货号: PC-49454Not For Human Use, Lab Use Only.

A-947 (A947) is a potent and selective PROTAC targeting SMARCA2, potently degrades SMARCA2 in SW1573 cells with DC50 value of 39 pM, maximal degradation of 96% at 10 nM.

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生物&药学活性

A-947 (A947) is a potent and selective PROTAC targeting SMARCA2, potently degrades SMARCA2 in SW1573 cells with DC50 value of 39 pM, maximal degradation of 96% at 10 nM.
A947 is designed by binding the bromodomains of SMARCA2/4 and PBRM1 to a VHL-targeting moiety, shows binding affinity to the SMARCA2 and SMARCA4 bromodomains with Kd of 93 and 65 nM, respectively.
A947 displays an 28-fold higher concentration needed to achieve a DC50 on SMARCA4 (1.1 nM), with a maximal degradation of SMARCA4 (92%) being achieved at concentrations approaching 100 nM.
A947 also exhibits similar selectivity on SMARCA2 degradation over PBRM1.
Inhibitors of the ubiquitin activating enzyme (MLN-7243) and proteasome inhibitor (MG-132) could block A947-mediated degradation of SMARCA2.
A947 is equally efficient in degrading both the murine and rat orthologs of SMARCA2.
A947 inhibits growth of a panel of SMARCA4-mutant NSCLC cells (mean IC50=7 nM), SMARCA4WT cells is significantly less sensitive to A947 (IC50=86 nM).
A-947 (40 mg/kg, i.v.) exhibits tumor growth inhibition in the SMARCA4wt Calu-6 xenograft model, also shows synergistic effect when combined with MCL1 inhibitor (AMG-176 and S63845).

物理化学性质&存储条件

分子量	1121.416
分子式	C61H76N12O7S
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-((2R)-2-(3-(4-((4-((1r,3r)-3-((4-(3-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)pyridin-2-yl)oxy)cyclobutoxy)piperidin-1-yl)methyl)piperidin-1-yl)isoxazol-5-yl)-3-methylbutanoyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide

参考文献

1. Cantley J, et al. Nat Commun. 2022 Nov 10;13(1):6814.

A947 (A-947)

生物&药学活性

物理化学性质&存储条件

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A947 (A-947)

生物&药学活性

物理化学性质&存储条件

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