TQ-3959 | BTK PROTAC | Probechem Biochemicals

Chemical Structure : TQ-3959

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TQ-3959 (TQ3959)

货号: PC-25199Not For Human Use, Lab Use Only.

TQ-3959 is a potent, selective and orally bioavailable BTK PROTAC degrader with DC50 of 0.4 nM in OCI-Ly10 cell line using an HTRF assay, Dmax=97.7%.

规格	价格	库存	数量
25 mg		Get quote
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

TQ-3959 is a potent, selective and orally bioavailable BTK PROTAC degrader with DC50 of 0.4 nM in OCI-Ly10 cell line using an HTRF assay, Dmax=97.7%.
TQ-3959 exhibited a 512-fold selectivity for EGFR
TQ-3959 demonstrated robust antiproliferative activity against both of BTK WT and BTK C481S DLBCL cell lines with IC50 values ranging from 0.08 to 1.0 nM (BTKC481S TMD-8 cell, IC50=0.6 nM).
showed significantly reduced activity in normal cell lines HEK293 and HUVEC (IC50 > 1000 nM)
TQ-3959 (7.5, 15, and 30 mg/kg, oral gavage) exhibited antitumor efficacy in TMD-8 xenograft mouse models.

物理化学性质&存储条件

分子量	761.89
分子式	C40H47N11O5
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	3-((4-(1-(1-(3-(2,6-Dioxopiperidin-3-yl)benzo[d]isoxazol-6-yl)azetidin-3-yl)piperidin-4-yl)phenyl)amino)-5-((R)-3-(3-methyl-2-oxoimidazolidin-1-yl)piperidin-1-yl)pyrazine-2-carboxamide

参考文献

1. Jing Ren, et al. J Med Chem. 2025 Jul 29. doi: 10.1021/acs.jmedchem.5c00956.

TQ-3959 (TQ3959)

生物&药学活性

物理化学性质&存储条件

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TQ-3959 (TQ3959)

生物&药学活性

物理化学性质&存储条件

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