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Chemical Structure : 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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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.
| M.Wt | 749.88 | |
| Formula | C43H43N9O4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Zhang J, et al. J Med Chem. 2022 Jul 14;65(13):9096-9125.
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