BQU57

  Cat. No.:  DC8202   Featured
Chemical Structure
1637739-82-2
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More than 5000 active chemicals with high quality for research!
Field of application
BQU57 is a potent and selective GTPase Ral Inhibitor.
Cas No.: 1637739-82-2
Chemical Name: BQU57
Synonyms: BQU57;6-amino-1,3-dimethyl-4-(4-(trifluoromethyl)phenyl)-1,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile;BQU-57;6-Amino-1,4-dihydro-1,3-dimethyl-4-[4-(trifluoromethyl)phenyl]-pyrano[2,3-c]pyrazole-5-carbonitrile
SMILES: NC1=C(C#N)C(C(C(C)=NN2C)=C2O1)C3=CC=C(C(F)(F)F)C=C3
Formula: C16H13F3N4O
M.Wt: 334.295833349228
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: BQU57 shows selective inhibition for Ral relative to Ras or Rho and inhibit xenograft tumor growth similar to depletion of Ral by siRNA. The IC50 for BQU57 of 2.0 μM in H2122 and 1.3 μM in H358.IC50 value: 2.0 μM (H2122 cell), 1.3 μM (H358 cell)Target: Ralin vitro: BQU57 inhibits Ral binding to its effector RalBP1, Ral-mediated cell spreading in murine fibroblasts and anchorage-independent growth of human cancer cell lines.in vivo: H2122 xenograft tumors are collected 3h after a single intraperitoneal injection BQU57 (10/20/50 mg/kg) and activation of Ral in the extracts is analyzed in RalBP1 pull-down assays. Both RalA and RalB are significantly inhibited by BQU57. By contrast, no inhibition of Ras and RhoA activity is observed.
References: [1]. Yan C, et al. Discovery and characterization of small molecules that target the GTPase Ral. Nature. 2014 Nov 20;515(7527):443-447.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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