PSIRC3 | BTK PROTAC | Probechem Biochemicals

Chemical Structure : PSIRC3

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PSIRC3 (PSIRC-3)

货号: PC-28765Not For Human Use, Lab Use Only.

PSIRC3 is a potent, selective, poseltinib-based covalent PROTAC degrader for Bruton's tyrosine kinase (BTK) with DC50 of 0.75 nM and Dmax of 85% in BTK-HiBiT Ramos cells.

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生物&药学活性

PSIRC3 is a potent, selective, poseltinib-based covalent PROTAC degrader for Bruton's tyrosine kinase (BTK) with DC50 of 0.75 nM and Dmax of 85% in BTK-HiBiT Ramos cells.
PSIRC3 shows high binding affinity for WT BTK with IC50 of 81.6 nM, while has no affinity for C481S BTK, inhibits WT BTK with IC50 of 36.2 nM.
PSIRC3 shows robust degradation activity in BTK-nLuc Ramos cells with DC50 of 1.5 nM.
PSIRC3 induces potent BTK degradation in wild-type TMD8 cells but has no degradation potency in C481S-BTK TMD8 cells.
PSIRC3 induces a potent, dose-dependent, and rapid ternary complex signal, with an EC50 of 9.6 nM and Amax of 2216 at 60 min in ternary complex formation assay.
PSIRC3 (15 mg/kg, i.v.) shows BTK degradation in peripheral blood mononuclear cells (PBMCs) and splenocytes from mice and high selectivity in proteomics.

物理化学性质&存储条件

分子量	783.89
分子式	C43H45N9O6
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	N-(3-((2-((4-(4-(2-(4-(4-((2,6-dioxopiperidin-3-yl)amino)phenyl)piperidin-1-yl)acetyl)piperazin-1-yl)phenyl)amino)furo[3,2-d]pyrimidin-4-yl)oxy)phenyl)acrylamide

参考文献

1. Cheng R, et al. Nat Commun. 2026 Oct 7;17(1):11429.

PSIRC3 (PSIRC-3)

生物&药学活性

物理化学性质&存储条件

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PSIRC3 (PSIRC-3)

生物&药学活性

物理化学性质&存储条件

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