Chemical Structure : SD-2301
CAS No.:
3054116-24-1
SD-2301
(SD2301)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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1366.51
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Formula
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C64H80N13O15PS2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(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
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References
1. Zhou J, et al. Nature. 2025 Jul;643(8071):519-528.
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