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A-1210477

CAS No. 1668553-26-1

A-1210477( A1210477 )

Catalog No. M12546 CAS No. 1668553-26-1

A-1210477 is a potent, selective Mcl-1 inhibitor that bind to Mcl-1 (Ki=0.45 nM) to disrupt MCL-1-BIM complexes.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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5MG 50 In Stock
10MG 87 In Stock
25MG 147 In Stock
50MG 259 In Stock
100MG 403 In Stock
500MG 888 In Stock
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Biological Information

  • Product Name
    A-1210477
  • Note
    Research use only, not for human use.
  • Brief Description
    A-1210477 is a potent, selective Mcl-1 inhibitor that bind to Mcl-1 (Ki=0.45 nM) to disrupt MCL-1-BIM complexes.
  • Description
    A-1210477 is a potent, selective Mcl-1 inhibitor that bind to Mcl-1 (Ki=0.45 nM) to disrupt MCL-1-BIM complexes, shows much weaker against Bcl-2 (Ki=132 nM) and Bcl-XL (Ki>660 nM); induces the hallmarks of intrinsic apoptosis and demonstrates single agent killing of multiple myeloma and non-small cell lung cancer cell lines, synergizes with the BCL-2/BCL-XL inhibitor navitoclax to kill a variety of cancer cell lines; also enhances cobimetinib-induced apoptosis in vitro.
  • In Vitro
    A-1210477 (10?μM) reduces the amount of BIM co-immunoprecipitated with MCL-1 antibody, and triggers MCL-1 elevation in a variety of cancer cell lines, including the breast cancer cell line HCC-1806. A-1210477 inhibits MCL-1-NOXA interactions with an IC50 of approximately 1?μM, while having no effect on BCL-2-BIM or BCL-XL-BCL-XS interactions. The NSCLC cell lines H2110 and H23 are sensitive to A-1210477 with cell viability IC50<10?μM, confirming that A-1210477 can kill MCL-1-dependent cell lines.
  • In Vivo
    ——
  • Synonyms
    A1210477
  • Pathway
    Angiogenesis
  • Target
    Bcl-2
  • Recptor
    Mcl-1
  • Research Area
    Cancer
  • Indication
    ——

Chemical Information

  • CAS Number
    1668553-26-1
  • Formula Weight
    850.0366
  • Molecular Formula
    C46H55N7O7S
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: < 4.8 mg/mL
  • SMILES
    O=C(C(N1CCN2CCOCC2)=C(CCCOC3=C(C=CC=C4)C4=CC=C3)C5=C1C(C6=C(COC7=CC=C(N8CCN(S(=O)(N(C)C)=O)CC8)C=C7)N(C)N=C6C)=CC=C5)O
  • Chemical Name
    1H-Indole-2-carboxylic acid, 7-[5-[[4-[4-[(dimethylamino)sulfonyl]-1-piperazinyl]phenoxy]methyl]-1,3-dimethyl-1H-pyrazol-4-yl]-1-[2-(4-morpholinyl)ethyl]-3-[3-(1-naphthalenyloxy)propyl]-

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Leverson JD, et al. Cell Death Dis. 2015 Jan 15;6:e1590. 2. Xiao Y, et al. Mol Cancer Ther. 2015 Aug;14(8):1837-47. 3. Phillips DC, et al. Blood Cancer J. 2015 Nov 13;5:e368. 4. Karpel-Massler G, et al. Cancer Res. 2017 Jul 1;77(13):3513-3526.
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