CFT7455 |
| カタログ番号GC64835 |
CFT7455 は、経口活性ジンクフィンガー転写因子 Ikaros (IKZF1)、Aiolos (IKZF3) デグレーダーです。 ＣＦＴ７４５５は、セレブロンＥ３リガーゼ（Ｋｄ０．９ｎＭ）に高い親和性で結合する抗癌剤である（ＷＯ２０２２０３２１３２Ａ１；化合物１）。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2504235-67-8
Sample solution is provided at 25 µL, 10mM.
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CFT7455 is an orally active zinc finger transcription factors Ikaros (IKZF1), Aiolos (IKZF3) degrader. CFT7455 is an anti-cancer agent that binds with high affinity to the cereblon E3 ligase (Kd of 0.9 nM) (WO2022032132A1; Compound 1)[1].
CFT7455 (Compound 1) promotes the degradation of >75% of steady state IKZF1 in multiple myeloma cells within 1.5 hours at 0.3 nM. The high binding affinity and degradation catalysis of CFT7455 enables potent cell growth inhibition in both previously untreated NCIH929 multiple myeloma cell lines (IC50 of 0.071 nM) and NCIH929 cells made resistant to both lenalidomide and pomalidomide (IC50 of 2.3 nM)[1].
In mouse xenograft tumor models, CFT7455 (Compound 1) demonstrates dose dependent efficacy from 3 μg/kg/day to 100 μg/kg/day. In several tumor xenografts tested daily dosing of CFT7455 at dose of 30 μg/kg/day to 100 μg/kg/day led to durable tumor regression[1].
[1]. David Proia, et al. Advantageous therapies for disorders mediated by ikaros or aiolos. WO2022032132A1.
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