Chemical Structure : HJM-561
CAS No.: 2570251-68-0
货号: PC-49082Not For Human Use, Lab Use Only.
HJM-561 is a potent, selective and orally bioavailable EGFR PROTAC degrader, selectively degrades the EGFR C797S-containing triple mutants Del19/T790M/C797S and L858R/T790M/C797S with DC50 values of 9.2 nM and 5.8 nM, respectively.
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
5 mg | ¥2480 | In stock | |
10 mg | ¥3980 | In stock | |
25 mg | ¥5980 | In stock | |
50 mg | Get quote | ||
100 mg | Get quote |
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HJM-561 is a potent, selective and orally bioavailable EGFR PROTAC degrader, selectively degrades the EGFR C797S-containing triple mutants Del19/T790M/C797S and L858R/T790M/C797S with DC50 values of 9.2 nM and 5.8 nM, respectively.
HJM-561 potently inhibits the proliferation of Del19/T790M/C797S and L858R/T790M/C797S Ba/F3 cells while sparing cells expressing wild-type EGFR.
HJM-561 (20-40 mpk, p.o. qd) shows robust antitumor activity in EGFR Del19/T790M/C797S-driven Ba/F3 CDX and PDX models that were resistant to osimertinib treatment.
分子量 | 864.385 | |
分子式 | C45H51ClN9O5P | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
3-(4-(4-(4-(1-(4-((5-chloro-4-((2-(dimethylphosphoryl)phenyl)amino)pyrimidin-2-yl)amino)-3-methoxyphenyl)piperidin-4-yl)piperazin-1-yl)but-1-yn-1-yl)-1-oxoisoindolin-2-yl)piperidine-2,6-dione |
1. Yong Du, et al. Mol Cancer Ther. 2022 Jul 5;21(7):1060-1066.
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