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Deltarasin

Chemical Structure : Deltarasin

CAS No.: 1440898-61-2

Deltarasin

货号: PC-22366Not For Human Use, Lab Use Only.

Deltarasin is potent, specfic inhibitor of KRAS-PDEδ (PDE6D) interaction, bind to the prenyl-binding pocket of PDEδ with KD of 38 nM, inhibits oncogenic RAS signalling.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Deltarasin is potent, specfic inhibitor of KRAS-PDEδ (PDE6D) interaction, bind to the prenyl-binding pocket of PDEδ with KD of 38 nM, inhibits oncogenic RAS signalling.
Deltarasin interferes with the binding of KRAS to PDEδ in cells and resulting delocalization of KRAS.
Deltarasin potently suppresses proliferation and MAPK-signalling in oncogenic KRAS-dependent PDAC cells.
Deltarasin (10 mg/kg QD, 15 mg/ kg QD and 10 mg/kg BID) impairs dose-dependent in vivo growth of xenografted pancreatic carcinoma in nude mice.

物理化学性质&存储条件

分子量 603.77
分子式 C40H37N5O
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)-1-Benzyl-2-(4-(2-(2-phenyl-1H-benzo[d]imidazol-1-yl)-2-(piperidin-4-yl)ethoxy)phenyl)-1H-benzo[d]imidazole

参考文献

1. Leung ELH, et al. Cell Death Dis. 2018 Feb 13;9(2):216.

2. Agalioti T, et al. Nat Commun. 2017 May 16;8:15205.

3. Papke B, et al. Nat Commun. 2016 Apr 20;7:11360.

4. Zimmermann G, et al. Nature. 2013 May 30;497(7451):638-42.

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