DW0254 | PDE6D-RAS inhibitor | Probechem Biochemicals

Chemical Structure : DW0254

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DW0254 (DW-0254)

货号: PC-73367Not For Human Use, Lab Use Only.

DW0254 (DW-0254) is a small molecules capable of inhibiting RAS-related C3 botulinum toxin substrate (RAC) small GTPase activation in ALL cell lines, directly binds to the hydrophobic pocket of PDE6D (Kd=436 nM, ITC), a RAS chaperone protein.

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生物&药学活性

DW0254 (DW-0254) is a small molecules capable of inhibiting RAS-related C3 botulinum toxin substrate (RAC) small GTPase activation in ALL cell lines, directly binds to the hydrophobic pocket of PDE6D (Kd=436 nM, ITC), a RAS chaperone protein.
DW0254 demonstrated dose-dependent RAC inhibition, arrest of proliferation and induced apoptosis in human leukemic cell lines (RS4;11 IC50=1.5-1.8 uM), also showed promising anti-leukemic activity in RAS-mutated cells (CCRF-CEM NRAS G12D, IC50=3.3-4.2 uM).
DW0254 disrupted the interaction between PDE6D and RAS, disturbing RAS subcellular localization.
DW0254 demonstrated anti-leukemic activity, decreased tumor progression in a murine xenograft model.

物理化学性质&存储条件

分子量	416.525
分子式	C25H28N4O2
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	3-(5-(2-(1H-indol-3-yl)ethyl)-1,3,4-oxadiazol-2-yl)-N-(4-ethylbenzyl)-N-methylpropanamide

参考文献

1. Sara Canovas Nunes, et al. Blood Cancer J. 2022 Apr 14;12(4):64.

DW0254 (DW-0254)

生物&药学活性

物理化学性质&存储条件

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DW0254 (DW-0254)

生物&药学活性

物理化学性质&存储条件

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