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
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M.Wt
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1149.39
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Formula
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C61H75F3N10O7S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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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
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References
1. Xin Yu, et al. bioRxiv. 2024 Mar 29:2024.03.25.586133.
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