| Bioactivity | PROTAC BTK degraders-5(compound 3e) is a selective BTK degrader with a DC50 value of 7.0 nM in JeKo-1 cells. PROTAC BTK degraders-5 has no off-target effect on degrading CRBN neosubstates. PROTAC BTK degraders-5 has anti-proliferation effect on various lymphoma tumor cells and can be used in chronic lymphoid malignancies research1. |
| Invitro | PROTAC BTK Degrader-5 (Compound 3e) (1.6~1000 nM; 24 h) 诱导 JeKo-1 细胞中 BTK 的降解，DC50值为7.0 nM[1]。PROTAC BTK Degrader-5 (100 and 1000 nM) 具有代谢稳定性，其半衰期为 145 分钟[1]。PROTAC BTK Degrader-5 (100 nM;12 h) 诱导的 BTK 降解被蛋白酶体抑制剂 MG - 132 (HY-13259) (5.0 μM) 有效阻断[1]。PROTAC BTK Degrader-5 (1.6~1000 nM; 24 h)对 IKZF1 和 GSPT1 无降解作用，对 IKZF3 有一定的降解作用[1]。PROTAC BTK Degrader-5 (72 h) 对OCI-ly10、TMD8、JeKo-1、BTKC481S Ba/F3细胞具有抗增殖作用, IC50 值分别为 2.3、4.5、38.1 和 86.0 nM，效果高于 Ibrutinib (HY-10997) (IC50分别为 4.5、4.7、79.8 和 1546.0 nM)[1]。 |
| In Vivo | PROTAC BTK Degrader-5（2 mg/kg, 静脉注射, 单剂量）在小鼠体内代谢稳定[1]。 Animal Model: |
| Name | PROTAC BTK Degrader-5 |
| Formula | C52H57ClFN9O6 |
| Molar Mass | 958.52 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. 1. Song Chen, et al. Discovery of novel BTK PROTACs with improved metabolic stability via linker rigidification strategy. European Journal of Medicinal Chemistry.Volume 255, 5 July 2023, 115403. |
PROTAC BTK Degrader-5
CAS: F: C52H57ClFN9O6 W: 958.52
PROTAC BTK degraders-5(compound 3e) is a selectiveBTKdegrader with a DC50 value of 7.0 nM in JeKo-1 cells. PROTAC BTK de
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