Chemical Structure : TQ-3959
CAS No.:
2926610-43-5
TQ-3959
(TQ3959)
Catalog No.: 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%.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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761.89
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Formula
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C40H47N11O5
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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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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
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References
1. Jing Ren, et al. J Med Chem. 2025 Jul 29. doi: 10.1021/acs.jmedchem.5c00956.
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