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首页-抗体药物偶连体和PROTACs-PROTAC-LD5097
LD5097

Chemical Structure : LD5097

CAS No.:

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LD5097 (LD-5097)

货号: PC-25704Not For Human Use, Lab Use Only.

LD5097 is a potent, selective RIPK1 PROTAC degrader with DC50 of 0.7 nM in Jurkat cells, Dmax=96% (24h).

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

LD5097 is a potent, selective RIPK1 PROTAC degrader with DC50 of 0.7 nM in Jurkat cells, Dmax=96% (24h).
LD5097 induces dose-dependent degradation of endogenous RIPK1 after 24 h in Jurkat cells, with DC50 and Dmax values of 2.6 nM and 98%, respectively, in western blot assay.
LD5097 exhibited potent degradation of endogenous RIPK1, with DC50 values of 2.8 and 0.8 nM, respectively, in both MOLM14 and U937 cells.
LD5097 acts as a PROTAC dependent on the VHL E3 ligase and ubiquitin-proteasome system to degrade RIPK1 in the cells.
(100 nM) sensitizes Jurkat cells to TNFα-mediated apoptosis.
LD5097 (10-100 mg/kg, i.v.) induces a reduction of RIPK1 protein levels by more than 70% at both 6 and 24 h postadministration in Jurkat subcutaneous xenograft mouse model.

物理化学性质&存储条件

分子量 1382.55
分子式 C74H75F4N13O8S
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)-N-((S)-3-(4-(5-((4-(4-(4-Amino-5-(1-(2-(3-(trifluoromethoxy)phenyl)acetyl)indolin-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)piperidine-1-carbonyl)phenyl)ethynyl)pyridin-2-yl)piperazin-1-yl)-1-(4-(4-methylthiazol-5-yl)phenyl)-3-oxopropyl)-1-((S)-2-(1-fluorocyclopropane-1-carboxamido)-3,3-dimethylbutanoyl)-4-hydroxypyrrolidine-2-carboxamide

参考文献

1. Dong Lu, et al. J Med Chem. 2025 Oct 24. doi: 10.1021/acs.jmedchem.5c00773.

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