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LD4172

Chemical Structure : LD4172

CAS No.: 2782022-40-4

LD4172 (LD-4172)

Catalog No.: PC-22126Not For Human Use, Lab Use Only.

LD4172 is a first-in-class RIPK1 PROTAC degrader with DC50 values of 4-400 nM in a panel of human and mouse cancer cell lines.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

LD4172 is a first-in-class RIPK1 PROTAC degrader with DC50 values of 4-400 nM in a panel of human and mouse cancer cell lines.
LD4172 is a potent RIPK1 degrader with rapid and sustained effects in vitro.
LD4172 (1 uM) acheives >90% of RIPK1 degradation within 2 and 4 h in Jurkat and B16F10 cells, respectively.
LD4172 sensitizes B16F10 cells to TNFα-mediated apoptosis.
LD4172 induces immunogenic cell death (ICD) and enriches tumor-infiltrating lymphocytes and substantially sensitizes the tumors to anti-PD1 therapy.

Physicochemical Properties

M.Wt 1149.39
Formula C61H75F3N10O7S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N1-(3-(4-amino-5-(1-(2-(3-(trifluoromethoxy)phenyl)acetyl)indolin-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)propyl)-N12-((S)-1-((2S,4R)-4-hydroxy-2-(((R)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)dodecanediamide

References

1. Xin Yu, et al. bioRxiv. 2024 Mar 29:2024.03.25.586133.

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