Deltarasin

SKU: orb1685659

Description

Deltarasin is a potent small molecule inhibitor that disrupts the KRAS-PDEδ interaction by binding to PDEδ with a high affinity (Kd = 38 nM). It is a valuable research tool for studying KRAS-driven cancers in both cellular and animal models, aiding in the exploration of oncogenic signaling and potential therapeutic strategies.

Research Area

Metabolism Research, Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 1440898-61-2
• MW: 603.75
• Purity: 99.06% (May vary between batches)
• Formula: C₄₀H₃₇N₅O
• SMILES: C(Oc1ccc(cc1)-c1nc2ccccc2n1Cc1ccccc1)[C@H](C1CCNCC1)n1c(nc2ccccc12)-c1ccccc1
• Target: Ras|||PDE
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:93 mg/mL (154.04 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.31 mM);DMSO:93 mg/mL (154.04 mM)

Bioactivity

• Target IC50:
  PDEδ:38 nM(Kd)
• In Vivo:
  Deltarasin (10 mg/kg i.p.) impairs dose-dependent tumor growth in nude mice bearing subcutaneous human Panc-Tu-I tumor cell xenografts . The finding may inspire novel drug discovery efforts aimed at the development of drugs targeting oncogenic RAS.
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• In Vitro:
  In liver cells, Deltarasin inhibits the interaction of RAS with PDEδ with KD of 41 nM. Inhibition of PDEδ-KRAS interaction by Deltarasin suppresses proliferation of human pancreatic ductal adenocarcinoma cells that are dependent on oncogenic KRAS.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Ras, Phosphodiesterase (PDE), phosphodiesterase, Inhibitor, PDEδ, inhibit, Deltarasin

Compound Identifiers

PubChem CID

73292904