SD-2301 | STAT3 PROTAC | Probechem Biochemicals

Chemical Structure : SD-2301

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SD-2301 (SD2301)

货号: PC-27259Not For Human Use, Lab Use Only.

SD-2301 is a highly potent, selective, and efficacious STAT3 PROTAC degrader with DC50 of 4 nM, Dmax of >95% in HiBiT assays using HeLa cell line.

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生物&药学活性

SD-2301 is a highly potent, selective, and efficacious STAT3 PROTAC degrader with DC50 of 4 nM, Dmax of >95% in HiBiT assays using HeLa cell line.
SD-2301 is >100 times more potent than SD-36 and SD-91 and 6 times more potent than KT-333 in inducing STAT3 degradation in cells.
SD-2301 is highly selective for inducing STAT3 degradation over other STAT members.
SD-2301 inhibits cell growth with IC50 of 5-11 nM in the SU-DHL-1 and SUP-M2 lymphoma cell lines.
The potent STAT3 degradation by SD-2301 depends upon its binding to STAT3 and VHL-1 and is also neddylation- and proteasome-dependent.
SD-2301 (20 mg/kg, i.v.) effectively reduces the levels of STAT3 proteinin SUP-M2 Xenograft mouse tissue, has no significant reduction of all other STAT proteins.
SD-2301 (10 and 30 mg/kg weekly for 4 weeks, i.v. injection) achieved rapid and complete tumor regression antitumor efficacy in the SU-DHL-1 and SUP-M2 xenograft mouse models.

物理化学性质&存储条件

分子量	1366.51
分子式	C64H80N13O15PS2
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	(2-(((5S,8S,10aR)-8-(((S)-5-Amino-1-((4-(ethylsulfonyl)benzyl)amino)-1,5-dioxopentan-2-yl)carbamoyl)-3-(5-(1-((S)-1-((2S,4R)-4-hydroxy-2-(((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)-1H-1,2,3-triazol-4-yl)pentanoyl)-6-oxodecahydropyrrolo[1,2-a][1,5]diazocin-5-yl)carbamoyl)-1H-indole-5-carbonyl)phosphonic Acid

参考文献

1. Zhou J, et al. Nature. 2025 Jul;643(8071):519-528.

SD-2301 (SD2301)

生物&药学活性

物理化学性质&存储条件

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SD-2301 (SD2301)

生物&药学活性

物理化学性质&存储条件

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