Deltarasin
Chemical Name: 2-[4-[(2S)-2-(2-Phenyl-1H-benzimidazol-1-yl)-2-(4-piperidinyl)ethoxy]phenyl]-1-(phenylmethyl)-1H-benzimidazole trihydrochloride
Purity: ≥99%
Biological Activity
Deltarasin is a high affinity PDEδ-KRAS interaction inhibitor (Kd = 41 nM); binds to PDEδ. Reduces proliferation and induces cell death of KRAS-dependent Panc-Tu-1 and Capan-1 pancreatic cancer cells. Attenuates tumor growth of Panc-Tu-1 xenografts in mice.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Small molecule inhibition of the KRAS-PDEδ interaction impairs oncogenic KRAS signalling.
Zimmermann et al.
Nature, 2013;497:638 -
Structure guided design and kinetic analysis of highly potent benzimidazole inhibitors targeting the PDEδ prenyl binding site.
Zimmermann et al.
J.Med.Chem., 2014;57:5435
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Citations for Deltarasin
The citations listed below are publications that use Tocris products. Selected citations for Deltarasin include:
2 Citations: Showing 1 - 2
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RNA splicing is a key mediator of tumour cell plasticity and a therapeutic vulnerability in colorectal cancer.
Authors: Malcolm G Et al.
Nat Commun 2022;13:2791
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An In Vivo Inflammatory Loop Potentiates KRAS Blockade.
Authors: Rudolf A Et al.
Biomedicines 2022;10
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