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Merck - 5.04972.0001 - ATR Inhibitor IV - CAS 1232410-49-9 - Calbiochem

  • MFR SKU: 5.04972.0001
  • ITEM #: 13025449
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ITEM #: 13025449
This listing is for 10 mg Glass bottle

Merck - 5.04972.0001 - ATR Inhibitor IV - CAS 1232410-49-9 - Calbiochem

  • Item #: 13025449
  • MFR SKU: 5.04972.0001
  • Overview A cell-permeable phenylpyrazine derivative that acts as a potent, ATP-competitive ( K i = 13 nM; IC 50 /[ATP] = 70 nM/50 µ M and 128 nM/100 µ M), ATR-selective inhibitor with much reduced or little potency against 4 related PIKKs ( K i = 2.2, 3.9, 16, and >1 µ M, respectively, against DNA-PK, PI 3-Kγ, ATM, and mTOR) and 50 other kinases. Shown to selectively inhibit ATR-dependent H2AX Ser139 & Chk1 Ser345 phosphorylation (complete inhibition at 10 µ M in HT29 and HFL1 cultures) without affecting ATM- and DNA-PK-mediated H2AX or ATM-mediated Chk2 phosphorylation. Short-term (24 h) VE-821 treatment, either alone or in synergy with Cisplatin (Cat. No. 232120 ), results in reversible cytostatic growth arrest regardless of cellular ATM-p53 pathway activity, while cytotoxicity and Cisplatin synergism in cell death induction is reported to occur only upon long-term VE-821 exposure (≥ 72 h) in cultures with ATM-p53 pathway defects.
  • Please note that the molecular weight for this compound is batch-specific due to variable water content.
  • Catalogue Number 504972
  • Brand Family Calbiochem®
  • Synonyms VE821, 3-amino-6-(4-(methylsulfonyl)phenyl)-N-phenylpyrazine-2-carboxamide, VE-821, ATM and Rad3-Related Inhibitor IV
  • References Prevo, R., et al. 2012, Cancer Biol. Ther. 13, 1072; Pires, I.M., et al. 2012, Br. J. Cancer 107, 291; Reaper, P.M., et al. 2011, Nat. Chem. Biol. 7, 428.
  • CAS number 1232410-49-9
  • Form Yellow solid
  • Hill Formula CHNOS
  • Chemical formula CHNOS
  • Reversible Y
  • Structure formula Image
  • Quality Level MQ100
  • Primary Target ATR i $anchor_PDP_OverviewTab_Product_Biological_Info_Primary Target K i " value=" Biological Information"
  • br> Primary Target K<sub>i</sub> 13nM
  • Purity ≥ 98% by HPLC
  • Cell permeable Y
  • Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
  • Toxicity Standard Handling
  • Storage +2° C to +8° C
  • Protect from Light Protect from light
  • Do not freeze Ok to freeze
  • Special Instructions Following reconstitution, aliquot and freeze (-20° C). Stock solutions are stable for up to 3 months at -20° C.
  • Packaged under inert gas Packaged under inert gas

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