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532626 Ral Activation Inhibitor, BQU57 - CAS 1637739-82-2 - Calbiochem

A cell-permeable compound that specifically, reversibly, and stoichiometrically (1:1) binds to the GDP-bound Ral A/B in an allosteric manner (Kd = 7.7 µM) and blocks its activation.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 6-Amino-1,3-dimethyl-4-(4-(trifluoromethyl)phenyl)-1,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile, Ral Inhibitor, RalA Activation Inhibitor, RalB Activation Inhibitor

Primary Target: Ral-GDP
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532626
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Overview

Key Spec Table

CAS #Empirical Formula
1637739-82-2C₁₆H₁₃F₃N₄O

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      		 Glass bottle 25 mg
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      Description
      OverviewA cell-permeable dihydropyranopyrazole compound that binds and locks RalA/B in the inactive GDP-bound form by targeting an allosteric site close to the guanine nucleotide-binding pocket (Kd = 7.7 µM binding study by ITC using RalB) in a 1:1 stoichiometric ratio, while exhibiting little affinity toward free or GTP-bound Ral. Shown to inhibit anchorage-independent growth of human lung cancer cell lines H358 & H2122 in vitro (IC50 = 1.3 & 2.0 µM, respectively, in 2-4 wks by soft agar colony formation assays) by reducing cellular level of ATP-bound, active RalA/B (by >90% with 10 µM BQU57 treatment for 3 h; assessed by by RALBP1-agarose pull-down). BQU57 is bioavailable in mice via intraperitoneal injection (Plasma T1/2 = 1.5 h, AUC0-5 h = 28.6 µg·h/mL post single 50 mg/kg i.p. dosage) with overall tissue distribution, including brain (µg drug/g tissue = 4.1/liver, 2.4/kidney, 2.1/heart, 1.8/lung, 1.4/brain, 1.2/H2122 tumor; 3 h post single 50 mg/kg i.p. dosage). Shown to selectively downregulate leves of active RalA/B, but not Ras or RhoA, in H2122-derived tumor in mice in a dose-dependent manner (64% and 86% reduction of ATP-bound RalA and RalB, respectively, 3 h post single 50 mg/kg i.p. dosage) and effectively suppress H2122 tumor expansion when administered via daily i.p. dosing (by 70% 22 d post H2122 inoculation with 21 daily 50 mg/kg/d i.p. dosages) in vivo.

      Please note that the molecular weight for this compound is batch-specific due to variable water content.
      Catalogue Number532626
      Brand Family Calbiochem®
      Synonyms6-Amino-1,3-dimethyl-4-(4-(trifluoromethyl)phenyl)-1,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile, Ral Inhibitor, RalA Activation Inhibitor, RalB Activation Inhibitor
      References
      ReferencesYan, C., et al. 2014. Nature. 515, 443.
      Product Information
      CAS number1637739-82-2
      FormBeige solid
      Hill FormulaC₁₆H₁₃F₃N₄O
      Chemical formulaC₁₆H₁₃F₃N₄O
      ReversibleY
      Quality LevelMQ100
      Biological Information
      Primary TargetRal-GDP
      Purity≥97% by HPLC
      Physicochemical Information
      Cell permeableY
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Global Trade Item Number
      Catalogue Number GTIN
      5.32626.0001 04055977281811