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首页-抗体药物偶连体和PROTACs-PROTAC-Cyclin D1 degrader MS28
Cyclin D1 degrader MS28

Chemical Structure : Cyclin D1 degrader MS28

CAS No.: 2229974-73-4

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Cyclin D1 degrader MS28 (XY028-133)

货号: PC-26498Not For Human Use, Lab Use Only.

Cyclin D1 degrader MS28 (XY028-133) is a potent, selective and first-in-class PROTAC degrader of cyclin D1 through recruiting the CDK4/6-cyclin D1 complex to VHL E3 ligase, effectively degrades cyclin D1 in Calu-1 cells with DC50 of 950 nM and Dmax of 90% (8 h).

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5 mg ￥1980 In stock
10 mg ￥3280 In stock
25 mg ￥5480 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Cyclin D1 degrader MS28 (XY028-133) is a potent, selective and first-in-class PROTAC degrader of cyclin D1 through recruiting the CDK4/6-cyclin D1 complex to VHL E3 ligase, effectively degrades cyclin D1 in Calu-1 cells with DC50 of 950 nM and Dmax of 90% (8 h).
MS28 displays modest degradation effects on CDK4/6 with DC50 > 10 μM and Dmax < 50% at the 8 h time point。
MS28 at 0.3 μM reduces the CDK6 protein level close to 50%, while it has no effect on CDK4.
MS28 preferentially degrades Cyclin D1 over CDK4/6.
MS28 degrades cyclin D1 by recruiting the CDK6-cyclin D1 complex to VHL, degrades cyclin D1 in a VHL-, CDK6- and UPS-dependent manner.
MS28 does not degrade cyclin D2 or other major cyclins and CDKs, such as cyclin B1 and CDK2.
MS28 effectively suppressed the proliferation of Calu-1 cells with GI50 of 1.0 uM, significantly reduced the mRNA levels of E2F target genes at 8 h of treatment in Calu-1 cells.
MS28 phenocopied the effect of CCND1 KO in Calu-1 cells, inhibited the clonogenicity of Calu-1 cells.

物理化学性质&存储条件

分子量 1002.25
分子式 C53H67N11O7S
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

(2S,4R)-1-((S)-2-(7-(4-(6-((6-Acetyl-8-cyclopentyl-5-methyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl)amino)pyridin-3-yl)piperazin-1-yl)-7-oxoheptanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide

参考文献

1. JIN, Jian, et al. Patent. US2017/065027.

2. Yan Xiong, et al. J Am Chem Soc. 2022 Dec 14;144(49):22622-22632.

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