Chemical Structure : BTK-PROTAC C13
CAS No.:
2801715-13-7
BTK-PROTAC C13
Catalog No.: PC-22720Not For Human Use, Lab Use Only.
BTK-PROTAC C13 is a highly potent, selective and orally bioavailable BTK PROTAC degrader with DC50 of 5.8 nM in Mino cells, Dmax=96%, degrades C481 and T316-mutated BTK proteins
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
BTK-PROTAC C13 is a highly potent, selective and orally bioavailable BTK PROTAC degrader with DC50 of 5.8 nM in Mino cells, Dmax=96%, degrades C481 and T316-mutated BTK proteins
BTK-PROTAC C13 effectively decreased BTK protein levels within 2 h and achieved 91% BTK degradation after 8 h of treatment.
BTK-PROTAC C13 is highly potent and effective in inhibiting cell growth in OCI-ly10 and achieved IC50 ranges of 5-150 nM.
BTK-PROTAC C13 (100 mg/kg) effectively reduced BTK protein levels after 6 h in the blood monocytes of mice.
BTK-PROTAC C13 functions through the ubiquitin–proteasome system (UPS).
BTK-PROTAC C13 does not affect proteins in BCR signaling pathway (LYN, NFATC1, NFKBIE, and CD72), as well as the substrates of IMiD, including IKZF1 and ZFP9.
BTK-PROTAC C13 (10 mg/kg, 30 mg/kg, bid) displays antitumor effects and BTK degradation OCI-ly10 xenograft tumors.
Physicochemical Properties
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M.Wt
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749.88
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Formula
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C43H43N9O4
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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-[5-[3-[4-[4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl][1,4′-bipiperidin]-1′-yl]-1-propyn-1-yl]-1,3-dihydro-1-oxo-2H-isoindol-2-yl]-2,6-piperidinedione
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References
1. Zhang J, et al. J Med Chem. 2022 Jul 14;65(13):9096-9125.
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