Chemical Structure : TDI-012804
CAS No.:
TDI-012804
(TDI 012804)
Catalog No.: PC-24241Not For Human Use, Lab Use Only.
TDI-012804 is a potent and selective Tankyrase 2 (TNKS2) inhibitor with IC50 of 3.46 nM in in vitro PARylation assays, has 25-fold selectivity over TNKS1, suppresses WNT signaling in TNKS depleted cells.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
TDI-012804 is a potent and selective Tankyrase 2 (TNKS2) inhibitor with IC50 of 3.46 nM in in vitro PARylation assays, has 25-fold selectivity over TNKS1, suppresses WNT signaling in TNKS depleted cells.
TDI-012804 is potent (EC50 <100nM) and shows TNKS2-selectivity against in TNKS1 isogenic DLD1 cells using an integrated TOP-Flash reporter.
TDI-012804 shows no inhibition of related PARP family enzymes (PARP1, PARP2, and PARP3).
Mutation of L1136 to tyrosine (L1136Y) significantly reduces the potency of TDI-012804 against TNKS2 but has no effect on the activity of XAV939.
TDI-012804 increases AXIN1 protein in TNKS1KO and TNKS1KO/TNKS2WT cells, but not in TNKS1WT or TNKS1KO/TNKS2L1136Y cells.
TDI-012804 is selectively toxic to Tnks1KO AKP-G12D and AKP-G13D organoids, compared to Tnks1WT lines.
Physicochemical Properties
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M.Wt
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506.56
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Formula
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C30H26N4O4
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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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N-(2-(4-(2-hydroxypropan-2-yl)phenyl)-4-oxo-3,4-dihydroquinazolin-7-yl)-4-methoxy-6-phenylnicotinamide
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References
1. Zimmerman J, et al. bioRxiv [Preprint]. 2025 Mar 7:2025.03.04.641305.
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