Chemical Structure : DFCI-002-06
CAS No.:
3092208-36-8
DFCI-002-06
Catalog No.: PC-26247Not For Human Use, Lab Use Only.
DFCI-002-06 is a potent, first-in-class dual HCK/BTK PROTAC degrader with DC50 values of 4.5 nM for BTK and 1.3 nM for HCK, Dmax values of >95% for BTK and 87% for HCK.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
DFCI-002-06 is a potent, first-in-class dual HCK/BTK PROTAC degrader with DC50 values of 4.5 nM for BTK and 1.3 nM for HCK, Dmax values of >95% for BTK and 87% for HCK.
DFCI-002-06 shows enzymetic IC50 of 0.52 nM and <0.495 nM for BTK and HCK respectively.
DFCI-002-06 (0.5 μM) induced significantly higher levels of apoptosis versus KIN-8194.
DFCI-002-06 induced significantly higher levels of apoptosis in malignant CD19+ lymphoplasmacytic cells compared to both Kin-8194 and zanubrutinib.
DFCI-002-06 (30 or 50 mg/kg) caused complete tumor suppression in TMD8 xenografted murine model.
Physicochemical Properties
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M.Wt
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794.92
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Formula
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C44H46N10O5
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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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5-(3-((4-((1r,4r)-4-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)cyclohexyl)piperazin-1-yl)methyl)azetidin-1-yl)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione
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References
1. Hatcher JM, et al. J Med Chem. 2026 Jan 22;69(2):1119-1134.
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