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首页-抗体药物偶连体和PROTACs-PROTAC-XL01126
XL01126

Chemical Structure : XL01126

CAS No.: 3011029-58-3

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XL01126 (XL 01126)

货号: PC-49282Not For Human Use, Lab Use Only.

XL01126 (XL 01126) is a fast and potent degrader of LRRK2 in multiple cell lines with DC50 values of 15-72 nM, Dmax values ranging from 82 to 90%, and degradation half-lives spanning from 0.6 to 2.4 h.

规格 价格 库存 数量
2 mg ￥4580 In stock
5 mg ￥7580 In stock
10 mg ￥11800 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

XL01126 (XL 01126) is a fast and potent degrader of LRRK2 in multiple cell lines with DC50 values of 15-72 nM, Dmax values ranging from 82 to 90%, and degradation half-lives spanning from 0.6 to 2.4 h.
XL01126 exhibits high cell permeability and forms a positively cooperative ternary complex with VHL and LRRK2 (α = 5.7), which compensates for a substantial loss of binary binding affinities to VHL and LRRK2.
XL01126 is orally bioavailable (F = 15%) and can penetrate the blood-brain barrier after either oral or parenteral dosing in mice.
XL01126 is a suitable degrader probe to study the noncatalytic and scaffolding functions of LRRK2 in vitro and in vivo.

物理化学性质&存储条件

分子量 1019.694
分子式 C50H64ClFN10O6S2
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

(2R,4R)-1-((R)-3-((((1r,4R)-4-((4-(4-((5-chloro-4-(methylamino)pyrimidin-2-yl)amino)-3-methoxybenzoyl)piperazin-1-yl)methyl)cyclohexyl)methyl)thio)-2-(1-fluorocyclopropane-1-carboxamido)-3-methylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide

参考文献

1. Liu X, et al. J Am Chem Soc. 2022 Aug 25. doi: 10.1021/jacs.2c05499.

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