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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Phosphodiesterase (PDE)-ADT-030
ADT-030

Chemical Structure : ADT-030

CAS No.: 1945942-36-8

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ADT-030 (ADT030)

货号: PC-26071Not For Human Use, Lab Use Only.

ADT-030 is a potent, selective Phosphodiesterase 10 (PDE10) inhibitor, inhibits enzymatic activity of recombinant PDE10 using cAMP and cGMP as substrates with IC50 of 0.95 uM and 1.15 uM respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

ADT-030 is a potent, selective Phosphodiesterase 10 (PDE10) inhibitor, inhibits enzymatic activity of recombinant PDE10 using cAMP and cGMP as substrates with IC50 of 0.95 uM and 1.15 uM respectively.
ADT-030 inhibits the proliferation of a series of KRAS G12D and KRAS G12C mutant PDAC cell lines with IC50 values in the low micromolar range (1.8-4.5 uM).
ADT-030 selectively inhibits the proliferation of KRAS mutant PDAC cells, but not KRAS wild-type PDAC cell line BxPC-3.
ADT-030 inhibits the proliferation, colony formation, and motility of PDAC cell lines harboring KRASG12D and KRASG12C mutations.
ADT-030 induces apoptosis and G2/M cell cycle arrest in PDAC cells.
ADT-030 blocks PDE10 and activates PKA/PKG to reduce β-catenin levels and inhibit RAS signaling.
ADT-030 also inhibits the growth of KRASG12D and KRASG12C mutant PDAC cells resistant to allele-specific KRAS inhibitors.
ADT-030 significantly suppressed tumor growth, reduced lung and liver metastasis, and increased survival without systemic toxicity in syngeneic and patient-derived xenograft (PDX) PDAC models.

物理化学性质&存储条件

分子量 478.59
分子式 C28H34N2O5
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

(S,Z)-2-(5-methoxy-2-methyl-1-(3,4,5-trimethoxybenzylidene)-1H-inden-3-yl)-N-(1-methylpyrrolidin-3-yl)acetamide

参考文献

1. Reddy Bandi DS, et al. bioRxiv [Preprint]. 2026 Feb 13:2026.02.11.705411.

2. Patent WO2016100542 A1.

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