RBC8

Names

[ Name ]:
RBC8

[Synonym ]:
6-amino-4-(2,5-dimethoxyphenyl)-3-(naphthalen-2-yl)-1,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile
6-amino-4-(2,5-dimethoxyphenyl)-1,4-dihydro-3-(2-naphthalenyl)-pyrano[2,3-c]pyrazole-5-carbonitrile

Biological Activity

[Description]:

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 inhibitorRBC8 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.

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Ras

Research Areas >> Cancer

[References]

[1]. Yan C, et al. Discovery and characterization of small molecules that target the GTPase Ral. Nature. 2014 Nov 20;515(7527):443-7.

[Related Small Molecules]

ARS-853 | ARS-1620 | NSC 23766 | ML 141 | Salirasib | Pan-RAS-IN-1 | Rhosin hydrochloride | CASIN | EHT 1864 | EHop-016 | 1A-116 | CCG 1423 | K-Ras(G12C) inhibitor 12 | ZCL 278 | Y16

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₅H₂₀N₄O₃

[ Molecular Weight ]:
424.45100

[ Exact Mass ]:
424.15400

[ PSA ]:
106.18000

[ LogP ]:
5.16558

[ Appearance of Characters ]:
light yellow solid

[ Storage condition ]:
-20℃

Safety Information

[ RIDADR ]:
NONH for all modes of transport

Related Compounds

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