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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.

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Synonyme: 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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Übersicht

Replacement Information

Key Spec Table

CAS #Empirical Formula
1637739-82-2C₁₆H₁₃F₃N₄O

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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
      Applications
      Biological Information
      Primary TargetRal-GDP
      Purity≥97% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      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
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Bestellnummer GTIN
      5326260001 04055977281811

      Documentation

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

      Titel

      Sicherheitsdatenblatt (SDB) 

      Literatur

      Übersicht
      Yan, C., et al. 2014. Nature. 515, 443.

      Technische Informationen

      Titel
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      White Paper: Further considerations of antibody validation and usage.
      Datenblatt

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision18-March-2015 JSW
      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
      DescriptionA 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.
      FormBeige solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1637739-82-2
      Chemical formulaC₁₆H₁₃F₃N₄O
      Purity≥97% by HPLC
      SolubilityDMSO (50 mg/ml). Use only fresh DMSO for reconstitution.
      Storage Protect from light
      +2°C to +8°C
      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.
      Toxicity Standard Handling
      ReferencesYan, C., et al. 2014. Nature. 515, 443.