BQU57

Research use only, not for human use.

BQU57 shows selective inhibition for Ral relative to Ras or Rho and inhibit xenograft tumor growth.

BQU57 is a GTPase Ral inhibitor. The Ras-like GTPases RalA and RalB are important drivers of tumour growth and metastasis. Chemicals that block Ral function would be valuable as research tools and for cancer therapeutics. The binding of the RBC8 derivative BQU57 to RalB was confirmed by isothermal titration calorimetry, surface plasmon resonance and (1)H-(15)N transverse relaxation-optimized spectroscopy (TROSY) NMR spectroscopy. RBC8 and BQU57 show selectivity for Ral relative to the GTPases Ras and RhoA and inhibit tumour xenograft growth to a similar extent to the depletion of Ral using RNA interference. The utility of structure-based discovery for the development of therapeutics for Ral-dependent cancers.

BQU57; BQU 57; BQU-57

Angiogenesis

CDK

Ral

Cancer

——

1637739-82-2

334.3

C16H13F3N4O

98%

DMSO : ≥ 36 mg/mL; 107.69 mM

Cc1nn(c2c1C(C(=C(O2)N)C#N)c1ccc(cc1)C(F)(F)F)C

6-amino-1,3-dimethyl-4-(4-(trifluoromethyl)phenyl)-1,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile

(-20℃)

With Ice Pack

≥ 2 years