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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-PARP-TDI-012804
TDI-012804

Chemical Structure : TDI-012804

CAS No.: 3120102-92-0

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TDI-012804 (TDI 012804, TDI012804)

货号: 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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5 mg ￥5980 In stock
10 mg ￥8980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

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.

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