Biological Activity
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.
Compound Libraries
Deltarasin is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 713.14 |
| Formula | C40H37N5O.3HCl |
| Storage | Store at -20°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 1440898-82-7 |
| PubChem ID | 91826089 |
| InChI Key | NCIOVAYUMQEQEU-VKZSUDIWSA-N |
| Smiles | C12=CC=CC=C1N=C(C4=CC=C(OC[C@H]([C@H]8CCNCC8)N5C(C7=CC=CC=C7)=NC6=C5C=CC=C6)C=C4)N2CC3=CC=CC=C3.Cl.Cl.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 71.31 | 100 | |
| water | 71.31 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 713.14. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.4 mL | 7.01 mL | 14.02 mL |
| 5 mM | 0.28 mL | 1.4 mL | 2.8 mL |
| 10 mM | 0.14 mL | 0.7 mL | 1.4 mL |
| 50 mM | 0.03 mL | 0.14 mL | 0.28 mL |
Molarity Calculator
Reconstitution Calculator
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Product Datasheets
References
References are publications that support the products' biological activity.
Zimmermann et al (2013) Small molecule inhibition of the KRAS-PDEδ interaction impairs oncogenic KRAS signalling. Nature 497 638 PMID: 23698361
Zimmermann et al (2014) Structure guided design and kinetic analysis of highly potent benzimidazole inhibitors targeting the PDEδ prenyl binding site. J.Med.Chem. 57 5435 PMID: 24884780
Keywords: Deltarasin, supplier, high, affinity, PDEdelta, PDED, PDEδ, PDE6D, phosphodiesterases, KRAS, inhibitors, inhibits, GTPase, Phosphodiesterases, G, Proteins, (Small), GTPase, Tocris Bioscience
