531057 | ETV1 Inhibitor, BRD32048 - Calbiochem

531057
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      概要

      Replacement Information

      主要スペック表

      Empirical Formula
      C₁₆H₂₂N₆O

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      5.31057.0001
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          ガラスビン 25 mg
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          Description
          OverviewA cell-permeable triazine compound that directly and reversibly binds to ETS family transcription factor ETV1 (KD = 17.1 µM) and reduces its transcriptional activity, independent of its binding to DNA. Selectively inhibits p300-dependent ETV1 acetylation at K33 and K116 and thereby promotes its degradation (~50 µM). Inhibits the invasion capacity of ETV1-dependent cell lines and primary melanocytes expressing NRASG12D, but not in primary melanocytes expressing NRAS. Does not affect PC3 cell line that is not dependent on ETV1 for invasion. Also it has no effect on the invasion of cancer cells expressing mutated ETV1 (K33R/K116R).

          Please note that the molecular weight for this compound is batch-specific due to variable water content.
          Catalogue Number531057
          Brand Family Calbiochem®
          SynonymsN-(4-Methoxyphenyl)-6-(1-piperidinylmethyl)-1,3,5-triazine-2,4-diamine, ER81 Inhibitor, ETV1-mediated Transcription Inhibitor, Transcription Inhibitor ETV1 Inhibitor
          References
          ReferencesPop, M.S., et al. 2014. Mol. Cancer Ther. 13, 1492.
          Product Information
          FormOff-white powder
          Hill FormulaC₁₆H₂₂N₆O
          Chemical formulaC₁₆H₂₂N₆O
          ReversibleY
          Applications
          Biological Information
          Primary TargetETS family transcription factor ETV1
          Purity≥95% 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 6 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          (M)SDS

          タイトル

          英語版製品安全データシート((M)SDS) 

          参考資料

          参考資料の概要
          Pop, M.S., et al. 2014. Mol. Cancer Ther. 13, 1492.
          データシート

          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.

          Revision29-August-2014 JSW
          SynonymsN-(4-Methoxyphenyl)-6-(1-piperidinylmethyl)-1,3,5-triazine-2,4-diamine, ER81 Inhibitor, ETV1-mediated Transcription Inhibitor, Transcription Inhibitor ETV1 Inhibitor
          DescriptionA cell-permeable triazine compound that targets the ETS family transcription factor ETV1, but not TBX21, RELA, RUNX1, RFWD2, or P/CAF, via affinity interaction (KD = kd/ka = 5.853 x 10-2 s-1/4.128 x 103 M-1s-1= 14.2 µM) and selectively suppresses ETV1-, but not MITF-, dependent reporter transcription activity in 501mel melanoma cells (2.57-fold vs 4-fold of mock level in 24 h, respectively, with or without 10 µM BRD32048) without affecting ETV1 DNA-binding activity. Shown to inhibit ETV1-dependent invasion by downregulating p300-, but not P/CAF-, mediated ETV1 lysine acetylation (K-Ac) in LNCaP & 501mel cultures (50 µM for 16 h) that are known to harbor ETV1 chromosomal rearrangement (translocation) and amplification, respectively, resulting in enhanced ETV1 degradation, while ETV1 K-Ac is not detectable in PC3 (lacking ETV1 rearrangement) & SK-MEL-28 (wild-type ETV1) cells and no invasion inhibition by BRD32048 treatment is seen in these cultures. Likewise, BRD32048 is demonstrated to inhibit invasion of NRASG12D-expressing primary melanocytes (pmel) only when infected to express ETV1, and no inhibition is seen in the non-infected or MYC-infected cells.
          FormOff-white powder
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₁₆H₂₂N₆O
          Purity≥95% by HPLC
          SolubilityDMSO (100 mg/ml)
          Storage +2°C to +8°C
          Protect from light
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
          Toxicity Standard Handling
          ReferencesPop, M.S., et al. 2014. Mol. Cancer Ther. 13, 1492.