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首页-抗体药物偶连体和PROTACs-PROTAC-CDK9 PROTAC 45
CDK9 PROTAC 45

Chemical Structure : CDK9 PROTAC 45

CAS No.: 2411021-01-5

CDK9 PROTAC 45 (CDK9 degrader compound 45)

货号: PC-21920Not For Human Use, Lab Use Only.

CDK9 PROTAC 45 is a highly potent, efficacious CDK9 PROTAC degrader, induces cell apoptosis in vitro and inhibits tumor growth in the MDA-MB-231 TNBC model.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

CDK9 PROTAC 45 is a highly potent, efficacious CDK9 PROTAC degrader, induces cell apoptosis in vitro and inhibits tumor growth in the MDA-MB-231 TNBC model.
CDK9 PROTAC 45 inhibits the growth of MDA-MB-468, MDA-MB-231, and BT-549 cells with IC50 values of 15.0, 13.6, and 3.9 nM, respectively.
CDK9 PROTAC 45 does not induce the degradation of other CDK proteins, including CDK1, CDK2, CDK4, CDK5, CDK6, and CDK7 within the concentration ranging from 100 to 500 nM in MDA-MB-231 cells.
CDK9 PROTAC 45 does not induce the degradation of GSPT1, which could induce degradation by certain CRBN-dependent PROTACs and molecule glues.
CDK9 PROTAC 45 demonstrates to specifically induce protein degradation of CDK9, rather than CDK7, resulting in the downregulation of MYC and a decrease of tumor cell proliferation in vivo.
CDK9 PROTAC 45 (2.5 or 5.0 mg/kg, i.p.) inhibits tumor growth in MDA-MB-231 CDX mice.

物理化学性质&存储条件

分子量 792.99
分子式 C43H56N10O5
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

4-(5-(2-(2,6-Dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)pentyl)-N-(4-(((5-(((S)-1-hydroxybutan-2-yl)amino)-3-isopropylpyrazolo[1,5-a]pyrimidin-7-yl)amino)methyl)phenyl)piperazine-1-carboxamide

参考文献

1. Wei D, et al. J Med Chem. 2021 Oct 14;64(19):14822-14847.

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