Deltarasin

Alias: Deltarasin hydrochloride; Deltarasin HCl; Deltarasin;
Cat No.:V0784 Purity: ≥98%
Deltarasin (also known as Deltarasin hydrochloride) is a novel,high affinity and potent small molecule inhibitor of KRAS-PDEδ protein-protein interaction with potential antineoplastic activity.
Deltarasin Chemical Structure CAS No.: 1440898-61-2
Product category: PDE
This product is for research use only, not for human use. We do not sell to patients.
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Other Forms of Deltarasin:

  • Deltarasin HCl
  • Deltarasin 3HCl
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Deltarasin (also known as Deltarasin hydrochloride) is a novel, high affinity and potent small molecule inhibitor of KRAS-PDEδ protein-protein interaction with potential antineoplastic activity. It inhibits KRAS-PDEδ interaction with a Kd of 38 nM for binding to purified PDEδ. The KRAS oncogene product is considered a major target in anticancer drug discovery. 5 mM of deltarasin completely inhibited PDEδ-KRAS interaction and released the insolubilized mCitrine-RHEB/KRAS6Q to the endomembrane system. This showed that deltarasin interfered with the binding of KRAS to PDEδ in cells and thereby inhibited its solubilization

Biological Activity I Assay Protocols (From Reference)
ln Vitro
Deltarasin inhibits the interaction between RAS and PDEδ in liver cells, with a Kd of 41 nM. When deltarasin inhibits the PDEδ-KRAS interaction, human pancreatic ductal adenocarcinoma cells that rely on oncogenic KRAS proliferate less[1].
ln Vivo
In nude mice with subcutaneous human Panc-Tu-I tumor cell xenografts, deltarasin (10 mg/kg, ip) reduces dose-dependent tumor growth[1].
Animal Protocol
Dissolved in 10% PLR and 5% DMSO; 10 mg/kg; Administered through i.p.
Mice bearing Panc-Tu-I xenografts
References
[1]. Zimmermann G, et al. Small molecule inhibition of the KRAS-PDEδ interaction impairs oncogenic KRAS signalling. Nature. 2013 May 30;497(7451):638-42.
[2]. Agalioti T, et al. Mutant KRAS promotes malignant pleural effusion formation. Nat Commun. 2017 May 16;8:15205. doi: 10.1038/ncomms15205
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C40H37N5O
Molecular Weight
603.75
CAS #
1440898-61-2
SMILES
C1(C2=CC=C(OC[C@@H](N3C4=CC=CC=C4N=C3C5=CC=CC=C5)C6CCNCC6)C=C2)=NC7=CC=CC=C7N1CC8=CC=CC=C8
InChi Key
NCIOVAYUMQEQEU-VKZSUDIWSA-N
InChi Code
InChI=1S/C40H37N5O.3ClH/c1-3-11-29(12-4-1)27-44-36-17-9-7-15-34(36)42-39(44)32-19-21-33(22-20-32)46-28-38(30-23-25-41-26-24-30)45-37-18-10-8-16-35(37)43-40(45)31-13-5-2-6-14-31;;;/h1-22,30,38,41H,23-28H2;3*1H/t38-;;;/m1.../s1
Chemical Name
2-[4-[(2S)-2-(2-phenyl-1H-benzimidazol-1-yl)-2-(4-piperidinyl)ethoxy]phenyl]-1-(phenylmethyl)-1H-benzimidazole, trihydrochloride
Synonyms
Deltarasin hydrochloride; Deltarasin HCl; Deltarasin;
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 100 mg/mL (165.6 mM)
Water:<1 mg/mL
Ethanol:<1 mg/L
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.6563 mL 8.2816 mL 16.5631 mL
5 mM 0.3313 mL 1.6563 mL 3.3126 mL
10 mM 0.1656 mL 0.8282 mL 1.6563 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Biological Data
  • Deltarasin

    In-cell measurements of the effect of deltarasin on the interaction of RAS with PDEδ and resulting delocalization of KRAS.Nature.2013 May 30;497(7451):638-42.
  • Deltarasin

    Inhibition of PDEδ–KRAS interaction suppresses proliferation and MAPK-signalling in oncogenic KRAS-dependent PDAC cells.Nature.2013 May 30;497(7451):638-42.
  • Deltarasin

    Deltarasin impairs dose-dependent in vivo growth of xenografted pancreatic carcinoma in nude mice.Nature.2013 May 30;497(7451):638-42.
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