Deltarasin
- CAS NO.:1440898-61-2
- Empirical Formula: C40H37N5O
- Molecular Weight: 603.75
- MDL number: MFCD26793865
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-10-30 18:52:02
What is Deltarasin?
The Uses of Deltarasin
Deltarasin is an inhibitior of KRAS-PDEδ which has been shown to impair oncogenic signalling.
Biological Activity
the kras oncogene product is considered a major target in anticancer drug discovery. interfering with binding of mammalian pdeδ to kras by means of small molecules provides a novel opportunity to suppress oncogenic ras signalling by altering its localization to endomembranes. deltarasin is an inhibitor of the kras-pdeδ interaction to impair oncogenic kras signalling.
in vitro
within a minute, 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 [1].
in vivo
a clear dose-dependent reduction in panc-tu-i tumour growth rate could be observed in deltarasin treated mice with respect to the vehicle-injected controls, where the growth of tumours in mice that were treated with 10mg kg/1 bid deltarasin was almost completely blocked [1].
References
[1] zimmermann g, papke b, ismail s, vartak n, chandra a, hoffmann m, hahn sa, triola g, wittinghofer a, bastiaens pi, waldmann h. small molecule inhibition of the kras-pdeδ interaction impairs oncogenic kras signalling. nature. 2013;497(7451):638-42.
Properties of Deltarasin
Boiling point: | 824.3±75.0 °C(Predicted) |
Density | 1.23±0.1 g/cm3(Predicted) |
storage temp. | Store at -20°C |
solubility | Soluble in DMSO |
form | solid |
pka | 10.35±0.10(Predicted) |
color | White |
CAS DataBase Reference | 1440898-61-2 |
Safety information for Deltarasin
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H302:Acute toxicity,oral H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation |
Precautionary Statement Codes |
P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for Deltarasin
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