Deltarasin

Catalog No.S7224 Batch:S722401

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Technical Data

Formula

C40H37N5O

Molecular Weight 603.75 CAS No. 1440898-61-2
Solubility (25°C)* In vitro DMSO 100 mg/mL (165.63 mM)
Ethanol 100 mg/mL (165.63 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Deltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with Kd of 38 nM for binding to purified PDEδ.
Targets
KRAS [1] PDEδ [1]
38 nM(Kd)
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. [1]
In vivo Deltarasin (10 mg/kg i.p.) impairs dose-dependent tumor growth in nude mice bearing subcutaneous human Panc-Tu-I tumour cell xenografts. [1]

Protocol (from reference)

Animal Study:[1]
  • Animal Models

    Mice bearing Panc-Tu-I xenografts

  • Dosages

    10 mg/kg bid

  • Administration

    i.p.

Selleck's Deltarasin has been cited by 6 publications

Detection of Ras nanoclustering-dependent homo-FRET using fluorescence anisotropy measurements [ Eur J Cell Biol, 2023, 102(2):151314] PubMed: 37058825
MEK nuclear localization promotes YAP stability via sequestering β-TrCP in KRAS mutant cancer cells. [ Cell Death Differ, 2019, 26(11):2400-2415] PubMed: 30833665
EPHA2 feedback activation limits the response to PDEδ inhibition in KRAS-dependent cancer cells. [ Acta Pharmacol Sin, 2019, 10.1038/s41401-019-0268-y] PubMed: 31316177
Myeloid-derived interleukin-1β drives oncogenic KRAS-NF-κΒ addiction in malignant pleural effusion. [ Nat Commun, 2018, 9(1):672] PubMed: 29445180
Myeloid-derived interleukin-1β drives oncogenicKRAS-NF-κΒ addiction in malignant pleural effusion [ Nature Communications, 2018, 672-2018)] PubMed: None
Inhibition of KRAS-dependent lung cancer cell growth by deltarasin: blockage of autophagy increases its cytotoxicity [ Cell Death Dis, 2018, 9(2):216] PubMed: 29440631

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.