Chemical Structure : PTP1B and TCPTP degrader X1
CAS No.:
PTP1B and TCPTP degrader X1
货号: PC-28558Not For Human Use, Lab Use Only.
PTP1B and TCPTP degrader X1 is a potent, selective CRBN-based PROTAC dual degrader of PTP1B/TCPTP with DC50 of 8.9 nM and 6.2 nM respectively in HEK293 cells.
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纯度 & COA & 质检文件 纯度:
>98% (HPLC)
生物&药学活性
PTP1B and TCPTP degrader X1 is a potent, selective CRBN-based PROTAC dual degrader of PTP1B/TCPTP with DC50 of 8.9 nM and 6.2 nM respectively in HEK293 cells.
X1 induces complete degradation of both proteins in multiple human and mouse cell lines.
X1 induces PTP1B/TCPTP degradation via depending on ubiquitination, proteasome activity, and binding to PTP1B/TCPTP and E3 ligase CRBN.
X1 enhances IFNγ-induced STAT1 phosphorylation and nuclear translocation.
X1 enhances JAK/STAT and TCR signaling and activation of immune cells that are essential for anti-tumor immunity.
X1 is efficacious in promoting CAR-T tumor killing effects.
X1 showed anticancer efficacy in MC38 syngeneic tumor model either alone or in combination with anti-PD-1 therapy.
物理化学性质&存储条件
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分子量
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1313.16
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分子式
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C62H69BrF2N9O14P
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外观性状
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Solid
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CAS No.
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储存条件
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- 固体粉末
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-20°C 12 个月; 4°C 6 个月
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- 配置液
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-80°C 6 个月; -20°C 6 个月
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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((4-((2S)-3-(((2S)-6-(3-bromo-4-methylbenzamido)-1-(4-(3-((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)amino)-3-oxopropyl)piperazin-1-yl)-1-oxohexan-2-yl)amino)-2-((S)-2-(2-(4-hydroxy-3-methoxyphenyl)acetamido)-3-phenylpropanamido)-3-oxopropyl)phenyl)difluoromethyl)phosphonic acid
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参考文献
1. Zihan Qu, et al. J Med Chem. 2026 Oct 8;69(19):22336-22354.
