bs-60228C

DATASHEET

Formulation Powder

Storage: Store in dry, dark place at -20C for 1 year.

Product Information:

Molecular Weight: 334.3

Formula: C16 H13 F3 N4 O

CAS Number: 1637739-82-2

InChi Key: IJCMHHSFXFMZAI-UHFFFAOYSA-N

InChi: InChI=1S/C16H13F3N4O/c1-8-12-13(9-3-5-10(6-4-9)16(17,18)19)11(7-20)14(21)24-15(12)23(2)22-8/h3-6,13H,21H2,1-2H3

Smiles: CC1=NN(C)C2OC(N)=C(C#N)C(C1=2)C1C=CC(=CC=1)C(F)(F)F

Purity: 98.0

Solubility: DMSO up to 50 mM

Appearance: Solid Power.

Shelf Life: 1.0 years

Description:

BQU57 is a potent and selective GTPase Ral Inhibitor. It showed selectivity for Ral relative to the GTPases Ras and RhoA and inhibited tumour xenograft growth to a similar extent to the depletion of Ral using RNA interference. It inhibited the binding of Ral to its effector RALBP1, as well as inhibiting Ral-mediated cell spreading of murine embryonic fibroblasts and anchorage-independent growth of human cancer cell lines. The binding of the BQU57 to RalB was confirmed by isothermal titration calorimetry, surface plasmon resonance and 1H-15N transverse relaxation-optimized spectroscopy (TROSY) NMR spectroscopy. The Ras-like GTPases RalA and RalB are important drivers of tumour growth and metastasis. BQU57 that blocks Ral function would be valuable as research tools and for cancer therapeutics.