A small molecule that binds to the farnesyl-binding pocket of PDEδ (Kd = 41 nM) in cells thus inhibiting its interaction with KRAS and disrupting RAS signaling; reduces proliferation and increases cell death of Panc-Tu-I tumor cells at 5 μM in a human pancreatic ductal adenocarcinoma cell model; reduces tumor growth at a dose of 10 mg/kg in nude mice xenografted with pancreatic carcinoma

Deltarasin (hydrochloride) – 10 mg

Brand:
Cayman
CAS:
1440898-82-7
Storage:
-20
UN-No:
Non-Hazardous - /

KRAS is an oncogene product that acts as a GTPase tethered to cell membranes to assist in various cell signaling pathways. The prenyl-binding protein PDEδ regulates the correct localization and signaling of farnesylated KRAS by facilitating its diffusion to the cytoplasm. Deltarasin is a small molecule that binds to the farnesyl-binding pocket of PDEδ (Kd = 41 nM) in cells thus inhibiting its interaction with KRAS and disrupting RAS signaling.{25383} Treatment of human pancreatic ductal adenocarcinoma cell models with 5 μM deltarasin has been reported to prevent KRAS plasma membrane localization and subsequent solubilization by PDEδ, resulting in reduced proliferation and increased cell death of Panc-Tu-I tumor cells.{25383} Furthermore, in nude mice bearing pancreatic carcinoma xenografts, deltarasin has been shown to reduce tumor growth at a dose of 10 mg/kg.{25383}  

 

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SKU: 9001536 - 10 mg Category:

Description

A small molecule that binds to the farnesyl-binding pocket of PDEδ (Kd = 41 nM) in cells thus inhibiting its interaction with KRAS and disrupting RAS signaling; reduces proliferation and increases cell death of Panc-Tu-I tumor cells at 5 μM in a human pancreatic ductal adenocarcinoma cell model; reduces tumor growth at a dose of 10 mg/kg in nude mice xenografted with pancreatic carcinoma

Formal name: 2-[4-[(2S)-2-(2-phenyl-1H-benzimidazol-1-yl)-2-(4-piperidinyl)ethoxy]phenyl]-1-(phenylmethyl)-1H-benzimidazole, hydrochloride

Synonyms: 

Molecular weight: 691.3

CAS: 1440898-82-7

Purity: ≥98%

Formulation: A crystalline solid

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