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ADT-1004

Chemical Structure : ADT-1004

CAS No.: 1945941-72-9

ADT-1004 (ADT1004)

货号: PC-23212Not For Human Use, Lab Use Only.

ADT-1004 is an orally bioavailable prodrug of ADT-007, potent, selective pan-RAS inhibitor, selectively inhibits PDAC cells with mutant KRAS, does not impact the growth of tumors from RAS WT PDAC cells.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

ADT-1004 is an orally bioavailable prodrug of ADT-007, potent, selective pan-RAS inhibitor, selectively inhibits PDAC cells with mutant KRAS, does not impact the growth of tumors from RAS WT PDAC cells.
ADT-1004 is designed to improve the water solubility and metabolic stability of ADT-007.
ADT-1004 inhibited ERK phosphorylation in PDAC tumors.
ADT-1004 blocked tumor growth and ERK phosphorylation in PDX PDAC models with KRAS G12D , KRAS G12V , KRAS G12C , or KRAS G13Q mutations.
ADT-1004 treatment increased CD4 + and CD8 + T cells in the TME consistent with exhaustion and increased MHCII + M1 macrophage and dendritic cells
ADT-1004 demonstrated superior efficacy over sotorasib and adagrasib in tumor models involving human PDAC cells resistant to these KRAS G12C inhibitors.

物理化学性质&存储条件

分子量 589.66
分子式 C33H36FN3O6
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

(Z)-4-((5-fluoro-3-(2-((furan-2-ylmethyl)amino)-2-oxoethyl)-2-methyl-1H-inden-1-ylidene)methyl)-2,6-dimethoxyphenyl (1-methylpiperidin-4-yl)carbamate

参考文献

1. Reddy Bandi DS, et al. bioRxiv [Preprint]. 2024 Oct 8:2024.10.04.616725.

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