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首页-抗体药物偶连体和PROTACs-PROTAC-dCDK9-202
dCDK9-202

Chemical Structure : dCDK9-202

CAS No.:

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dCDK9-202

货号: PC-25872Not For Human Use, Lab Use Only.

dCDK9-202 is a highly potent, selective PROTAC CDK9 degrader with DC50 of 3.5 nM and CDK9 decline (94.4%) at 25 nM in TC-71 cell line, inhibits cell growth with IC50 of 8.5 nM in TC-71 cells.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

dCDK9-202 is a highly potent, selective PROTAC CDK9 degrader with DC50 of 3.5 nM and CDK9 decline (94.4%) at 25 nM in TC-71 cell line, inhibits cell growth with IC50 of 8.5 nM in TC-71 cells.
dCDK9-202 is highly selective in the degradation of CDK9 among the CDK protein family, as well as IKZF.
dCDK9-202 depletes significantly endogenous CDK9 within 25 nM in U87 glioblastoma cells, SKUT1 uterine leiomyosarcoma cells, and RH5 rhabdomyosarcoma cells with DC50 values lower than 10 nM.
dCDK9-202 is capable of inhibiting cell proliferation and inducing apoptosis.
dCDK9-202 exhibits antiproliferative inhibition against multiple cancer cell lines (IC50=40.9 nM for T778 cell line, 79.6 nM for MDA-MB-231 cell line.
dCDK9-202 selectively proteolyzes CDK9 to impair Pol2 function and cancer-addicted transcriptome.
dCDK9-202 (10 mg/kg over a 12 day treatment) significantly inhibited xenograft growth in TC-71 xenograft model in immunocompromised mice.

物理化学性质&存储条件

分子量 803.99
分子式 C40H49N7O7S2
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

N-(5-(((5-(tert-Butyl)­oxazol-2-yl)­methyl)­thio)­thiazol-2-yl)-1-(8-(6-(2,6-dioxopiperidin-3-yl)-5,7-dioxo-3,5,6,7-tetrahydropyrrolo­[3,4-f]­isoindol-2­(1H)-yl)­octanoyl)­piperidine-4-carboxamide

参考文献

1. Ma L, et al. J Med Chem. 2025 Oct 23;68(20):21172-21186.

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