BTK-PROTAC C13

Chemical Structure : BTK-PROTAC C13

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货号: 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

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

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.

物理化学性质&存储条件

分子量	749.88
分子式	C43H43N9O4
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-[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

参考文献

1. Zhang J, et al. J Med Chem. 2022 Jul 14;65(13):9096-9125.

BTK-PROTAC C13

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BTK-PROTAC C13

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