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首页-抗体药物偶连体和PROTACs-PROTAC-YTHDC1 PROTAC XY-2
YTHDC1 PROTAC XY-2

Chemical Structure : YTHDC1 PROTAC XY-2

CAS No.:

YTHDC1 PROTAC XY-2

货号: PC-27441Not For Human Use, Lab Use Only.

YTHDC1 PROTAC XY-2 is a selective, efficient PROTAC degrader of N6-Methyladenosine (m6A) reader YTHDC1 with DC50 of 11.42 nM in MOLM13 and 13.59 nM in Kasumi-1 cells respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

YTHDC1 PROTAC XY-2 is a selective, efficient PROTAC degrader of N6-Methyladenosine (m6A) reader YTHDC1 with DC50 of 11.42 nM in MOLM13 and 13.59 nM in Kasumi-1 cells respectively.
XY-2 does not cause appreciable changes in the protein levels of YTHDC2 or YTHDF2.
XY-2 induces potent degradation of YTHDC1 at nanomolar concentrations in multiple AML cell lines.
XY-2 promotes celebron- and proteasome-dependent degradation of YTHDC1, without altering YTHDC1 mRNA expression.
XY-2 markedly suppressed proliferation, colony formation, migration and invasion, while inducing robust apoptosis in AML cells.
XY-2 exhibits potent antiproliferative activity in chronic myeloid leukemia K562 cells with IC50 of 125.2 nM.
XY-2 (2.5 or 5 mg/kg, intraperitoneally, once daily) exerts significant antitumor activity in AML xenograft tumor models.

物理化学性质&存储条件

分子量 658.12
分子式 C32H32ClN9O5
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-((2-chloro-6-(methylamino)-9H-purin-9-yl)methyl)-N-(5-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)pentyl)benzamide

参考文献

1. Zhongpao Xie, et al. Development of the First YTHDC1 Degrader with Improved Antileukemia Activity. JACS Au. 2026 Jun 10;6(7):3778-3789.

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