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  • AC480 (BMS-599626) (714971-09-2)
    • AC480 (BMS-599626) (714971-09-2) COFTTEK

    AC480 (BMS-599626) (714971-09-2)

    AC480, also known as BMS-599626 has been used in trials studying the treatment of Cancer, Metastases, and HER2 or EGFR Expressing Advanced Solid Malignancies…

    Not Intended for Therapeutic Use. For research use only.

    SKU 714971-09-2 Category

    AC480 (BMS-599626) (714971-09-2) Description:

    AC480, also known as BMS-599626 is an orally bioavailable inhibitor of the HER1, HER2 and HER4 tyrosine kinases (IC50 =22, 32 and 190 nM, respectively) with potential antineoplastic activity. BMS-599626 inhibits human epidermal growth factor receptors (HER) HER1, HER2 and HER4, thereby inhibiting the proliferation of tumor cells that overexpress these receptors.

    AC480 (BMS-599626) (714971-09-2) Specifications:

    Product Name AC480 (BMS-599626)
    Chemical Name BMS-599626; 714971-09-2; AC480; AC-480; BMS 599626; (S)-Morpholin-3-ylmethyl (4-((1-(3-fluorobenzyl)-1H-indazol-5-yl)amino)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl)carbamate
    Purity >98% (HPLC)
    CAS Number 714971-09-2
    Molecular Formula C27H27FN8O3
    Molecular Weight 530.564 g/mol
    Monoisotopic Mass 530.219 g/mol
    InChIKey LUJZZYWHBDHDQX-QFIPXVFZSA-N
    InChi Code InChI=1S/C27H27FN8O3/c1-17-23(34-27(37)39-15-22-14-38-8-7-29-22)13-36-25(17)26(30-16-32-36)33-21-5-6-24-19(10-21)11-31-35(24)12-18-3-2-4-20(28)9-18/h2-6,9-11,13,16,22,29H,7-8,12,14-15H2,1H3,(H,34,37)(H,30,32,33)/t22-/m0/s1
    SMILES O=C(OC[[email protected]]1NCCOC1)NC2=CN3N=CN=C(NC4=CC5=C(N(CC6=CC=CC(F)=C6)N=C5)C=C4)C3=C2C
    Form Powder
    Color N/A
    Solubility  Soluble in DMSO
    Storage Temp.  -20°C
    Shelf life >2 years if stored properly
    Handling Protect from air and moisture
    Application an orally bioavailable inhibitor

     

    Details

    RIDADR NONH for all modes of transport

    References:

    • HER receptor tyrosine kinase inhibitor, in patients with advanced solid tumors. Soria JC, Cortes J, Massard C, Armand JP, Andreis D, Ropert S, Lopez E, Catteau A, James J, Marier JF, Beliveau M, Martell RE, Baselga J.Ann Oncol. 2019 Jan 9. doi:10.1093/annonc/mdy532. [Epub ahead of print] No abstract available. PMID: 30624604
    • HER receptor tyrosine kinase inhibitor, in patients with advanced solid tumors. Soria JC, Cortes J, Massard C, Armand JP, De Andreis D, Ropert S, Lopez E, Catteau A, James J, Marier JF, Beliveau M, Martell RE, Baselga J. Ann Oncol. 2012 Feb;23(2):463-71. doi: 10.1093/annonc/mdr137. Epub 2011 May 16. PMID: 21576284
    • Gavai AV, Fink BE, Fairfax DJ, Martin GS, Rossiter LM, Holst CL, Kim SH, Leavitt KJ, Mastalerz H, Han WC, Norris D, Goyal B, Swaminathan S, Patel B, Mathur A, Vyas DM, Tokarski JS, Yu C, Oppenheimer S, Zhang H, Marathe P, Fargnoli J, Lee FY, Wong TW, Vite GD. Discovery and preclinical evaluation of [4-[[1-(3-fluorophenyl)methyl]-1H-indazol-5-ylamino]-5-methylpyrrolo[2,1-f][1,2,4 ]triazin-6-yl]carbamic acid, (3S)-3-morpholinylmethyl ester (BMS-599626), a selective and orally efficacious inhibitor of human epidermal growth factor receptor 1 and 2 kinases. J Med Chem. 2009 Nov 12;52(21):6527-30. doi: 10.1021/jm9010065. PubMed PMID: 19821562.
    • Haluska P, Carboni JM, TenEyck C, Attar RM, Hou X, Yu C, Sagar M, Wong TW, Gottardis MM, Erlichman C. HER receptor signaling confers resistance to the insulin-like growth factor-I receptor inhibitor, BMS-536924. Mol Cancer Ther. 2008 Sep;7(9):2589-98. doi: 10.1158/1535-7163.MCT-08-0493. Epub 2008 Sep 2. PubMed PMID: 18765823; PubMed Central PMCID: PMC2614316.
    • Wong TW, Lee FY, Yu C, Luo FR, Oppenheimer S, Zhang H, Smykla RA, Mastalerz H, Fink BE, Hunt JT, Gavai AV, Vite GD. Preclinical antitumor activity of BMS-599626, a pan-HER kinase inhibitor that inhibits HER1/HER2 homodimer and heterodimer signaling. Clin Cancer Res. 2006 Oct 15;12(20 Pt 1):6186-93. PubMed PMID: 17062696.
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