17-AAG

CAS No. 75747-14-7

17-AAG( Tanespimycin | NSC 330507 | CP 127374 | 17AAG | 17 AAG )

Catalog No. M15881 CAS No. 75747-14-7

A potent Hsp90 inhibitor with IC50 of 5 nM in cell-free assays.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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10MG 53 In Stock
25MG 87 In Stock
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Biological Information

  • Product Name
    17-AAG
  • Note
    Research use only, not for human use.
  • Brief Description
    A potent Hsp90 inhibitor with IC50 of 5 nM in cell-free assays.
  • Description
    A potent Hsp90 inhibitor with IC50 of 5 nM in cell-free assays; induces cytosolic accumulation of cytochrome c and cleavage and activities of caspase-9 and caspase-3, triggering apoptosis of HL-60/Bcr-Abl and K562 cells; causes the degradation of HER2, HER3, Akt, and both mutant and wild-type androgen receptor; inhibits prostate cancer xenografts growth in mice.Skin Cancer Phase 2 Discontinued(In Vitro):Tanespimycin causes the degradation of HER2, Akt, and both mutant and wild-type AR and the retinoblastoma-dependent G1 growth arrest of prostate cancer cells. Tanespimycin inhibits prostate cancer cell lines with IC50s ranged from 25-45 nM (LNCaP, 25 nM; LAPC-4, 40 nM; DU-145, 45 nM; and PC-3, 25 nM).Tanespimycin (0.1-1 μM) induces a nearly complete loss of ErbB2 on ErbB2-overexpressing breast cancer cells. Tanespimycin inhibits cell growth and induces G2/M cell cycle arrest and apoptosis in CCA cells together with the down-regulation of Bcl-2, Survivin and Cyclin B1, and the up-regulation of cleaved PARP.(In Vivo):Tanespimycin (25-200 mg/kg, i.p.) causes a dose-dependent decline in AR, HER2, and Akt expression in prostate cancer xenografts. Tanespimycin treatment at doses sufficient to induce AR, HER2, and Akt degradation results in the dose-dependent inhibition of androgen-dependent and -independent prostate cancer xenograft growth without toxicity.Tanespimycin (60 mg/kg) with Rapamycin (30 mg/kg) inhibits A549 and MDA-MB-231 tumor growth and effects tumor cures in MDA-MB-231 tumor-bearing animals by tail vein injection.
  • In Vitro
    ——
  • In Vivo
    ——
  • Synonyms
    Tanespimycin | NSC 330507 | CP 127374 | 17AAG | 17 AAG
  • Pathway
    Cytoskeleton/Cell Adhesion Molecules
  • Target
    HSP
  • Recptor
    HSP90
  • Research Area
    Cancer
  • Indication
    Skin Cancer

Chemical Information

  • CAS Number
    75747-14-7
  • Formula Weight
    585.6884
  • Molecular Formula
    C31H43N3O8
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: ≥ 55 mg/mL
  • SMILES
    NC(O[C@@H](/C(C)=C/[C@H](C)[C@@H](O)[C@@H](OC)C[C@H](C)CC1=C2NCC=C)[C@@H](OC)/C=C/C=C(C)/C(NC(C1=O)=CC2=O)=O)=O
  • Chemical Name
    Geldanamycin, 17-demethoxy-17-(2-propenylamino)-

Shipping & Storage Information

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

Reference

1. Kamal A, et al. Nature. 2003 Sep 25;425(6956):407-10. 2. Solit DB, et al. Clin Cancer Res. 2002 May;8(5):986-93. 3. Nimmanapalli R, et al.Cancer Res. 2001 Mar 1;61(5):1799-804.
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