TDI-012804 | TNKS2 inhibitor | Probechem Biochemicals

Chemical Structure : TDI-012804

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TDI-012804 (TDI 012804)

货号: PC-24241Not For Human Use, Lab Use Only.

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250 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	506.56
分子式	C30H26N4O4
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	N-(2-(4-(2-hydroxypropan-2-yl)phenyl)-4-oxo-3,4-dihydroquinazolin-7-yl)-4-methoxy-6-phenylnicotinamide

参考文献

1. Zimmerman J, et al. bioRxiv [Preprint]. 2025 Mar 7:2025.03.04.641305.

TDI-012804 (TDI 012804)

生物&药学活性

物理化学性质&存储条件

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TDI-012804 (TDI 012804)

生物&药学活性

物理化学性质&存储条件

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