YX-2-107 | CDK6 PROTAC | Probechem Biochemicals

Chemical Structure : YX-2-107

CAS No.: 2417408-46-7

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YX-2-107 (CDK6 PROTAC degrader)

货号: PC-73342Not For Human Use, Lab Use Only.

规格	价格	库存
2 mg	￥2480	In stock
5 mg	￥3880	In stock
10 mg	￥5980	In stock
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100 mg		Get quote

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生物&药学活性

YX-2-107 is a CRBN-recruiting and specific CDK6-degrading PROTAC with IC50 of 0.69 and 4.4 nM for CDK4 and CDK6 in vitro, selectively degardes CDK6 in Ph+ BV173 ALL cells with a degradation constant of 4 nM.
YX-2-107 does not affect expression of IKZF1 and IKZF3, and does not degarde CDK4 protein.
YX-2-107 inhibits S-phase entry, cell proliferation, RB phosphorylation, and FOXM1 expression and induces the selective degradation of CDK6 in Ph+ BV173 and SUP-B15 cells.|
PROTAC YX-2-107 is bioavailable in mice and pharmacologically active in suppressing Ph+ ALL proliferation in a mouse xenograft of Ph+ ALL, comparable or superior to that of the CDK4/6 enzymatic inhibitor palbociclib.

物理化学性质&存储条件

分子量	889.971
分子式	C45H51N11O9
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-(4-((2-(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)-2-oxoethyl)amino)butyl)-2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)acetamide

参考文献

1. Marco De Dominici, et al. Blood. 2020 Apr 30;135(18):1560-1573.

YX-2-107 (CDK6 PROTAC degrader)

生物&药学活性

物理化学性质&存储条件

参考文献

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YX-2-107 (CDK6 PROTAC degrader)

生物&药学活性

物理化学性质&存储条件

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