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Deltarasin

Cat. No. M3394
Deltarasin Structure
Size Price Availability Quantity
5mg USD 144  USD160 In stock
10mg USD 234  USD260 In stock
50mg USD 738  USD820 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

Deltarasin inhibits the interaction of RAS with PDEδ with KD of 41 nM. Deltarasin selectively binds to the prenyl-binding pocket of PDEδ with nanomolar affinity (IC50 = 41 nM, binding to PDEδ in cell). Deltarasin was tested as an inhibitor in mice that had previously received injections of human tumor cells with KRAS mutations. Deltarasin was effective as an inhibitor in sharply reducing tumor growth in comparison to a placebo.

Protocol
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models Mice bearing Panc-Tu-I xenografts
Formulation Lipovenoes 10% PLR and 5% DMSO
Dosages 10 mg/kg bid
Administration i.p.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 603.75
Formula C40H37N5O
CAS Number 1440898-61-2
Purity >98%
Solubility DMSO
Storage at -20°C
References

Structure guided design and kinetic analysis of highly potent benzimidazole inhibitors targeting the PDEδ prenyl binding site.
Zimmermann G, et al. J Med Chem. 2014 Jun 26;57(12):5435-48. PMID: 24884780.

Small molecule inhibition of the KRAS-PDEδ interaction impairs oncogenic KRAS signalling.
Zimmermann G, et al. Nature. 2013 May 30;497(7451):638-42. PMID: 23698361.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Deltarasin supplier, PDE, inhibitors

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