For research use only. Not for therapeutic Use.
RBC8 is a novel small molecule inhibitor of Ral GTPase; has IC50 of 3.5 μM in H2122 cell and 3.4 μM in H358 cell.
IC50 value:
Target: Ral GTPase inhibitor
RBC8 or BQU57 treatment showed no further inhibition of colony formation after Ral knockdown. RBC8 and BQU57 showed favorable properties that define good drug candidates. To test the effect of Ral inhibitors on xenograft tumor growth, nude mice were inoculated subcutaneously with H2122 human lung cancer cells and treated intraperitoneally with 50 mg/kg/d of RBC8 for 21 days (except weekends). RBC8 inhibited tumor growth to a similar extent as dual knockdown of RalA and RalB.
| Catalog Number | I003325 |
| CAS Number | 361185-42-4 |
| Synonyms | 6-amino-4-(2,5-dimethoxyphenyl)-3-naphthalen-2-yl-2,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile |
| Molecular Formula | C25H20N4O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C25H20N4O3/c1-30-17-9-10-20(31-2)18(12-17)21-19(13-26)24(27)32-25-22(21)23(28-29-25)16-8-7-14-5-3-4-6-15(14)11-16/h3-12,21H,27H2,1-2H3,(H,28,29) |
| InChIKey | CLMQBVUFKIKYLU-UHFFFAOYSA-N |
| SMILES | COC1=CC(=C(C=C1)OC)C2C(=C(OC3=NNC(=C23)C4=CC5=CC=CC=C5C=C4)N)C#N |
| Reference | [1]. Yan C, et al. Discovery and characterization of small molecules that target the GTPase Ral. Nature. 2014 Nov 20;515(7527):443-7. |
