17-AAG

SKU: orb1300898

Description

Tanespimycin (KOS 953) is a potent and selective Hsp90 inhibitor (IC50=5 nM) that reduces intracellular levels and activity of STK38/NDR1 while also downregulating its gene expression. This compound has been utilized in both in vitro and in vivo research models to study oncogenic signaling pathways, protein degradation, and cancer therapeutics.

Research Area

Cardiovascular Research, Cell Biology, Protein Biochemistry

Key Properties

• CAS Number: 75747-14-7
• MW: 585.7
• Purity: >99%
• Formula: C₃₁H₄₃N₃O₈
• SMILES: CO[C@H]1C[C@H](C)CC2=C(NCC=C)C(=O)C=C(NC(=O)\C(C)=C\C=C/[C@H](OC)[C@@H](OC(N)=O)\C(C)=C\[C@H](C)[C@H]1O)C2=O
• Target: HSP (Heat shock protein)
• Solubility: Soluble in DMSO (up to 50 mg/ml) or in Ethanol (up to 5 mg/ml).

Bioactivity

• Target IC50:
  ECa-109 cells:1.1 μM|AU565 cells:0.003 μM|BT-474 cells:0.01 μM|HepG2 cells:0.32 μM|DU-145 cells:0.282 μM|A375 cells:1287 nM|HSP90:5 nM|A431 cells:0.069 μM|HT29 cells:0.1 nM|A549 cells:0.286 μM|HeLa cells:0.2 μM|K562 cells:0.15 μM|CNE2Z cells:8.41 μM|BGC-823 cells:847 nM|HCT116 cells:56.5 nM
• In Vivo:
  METHODS: To study the antitumor activity of Tanespimycin, lymphoma-inoculated mice were intraperitoneally injected with Tanespimycin (5-40 mg/kg) every other day for three weeks. RESULTS: Tanespimycin inhibited lymphoma in vivo.
• In Vitro:
  METHODS: Human A-431, A549, BGC-823, HepG2, HUVEC, L02, and MDA-MB-231 cells were treated with Tanespimycin (0-10 μM) for 72 hours, and the cell growth inhibition was detected by MTT assay. RESULTS: Tanespimycin inhibited A-431 (IC50=89 nM), A549 (IC50=81 nM), BGC-823 (IC50=847 nM), HepG2 (IC50=91 nM), HUVEC (IC50=282 nM), and L02 (IC50=99) nM), MDA-MB-231 (IC50=0.28 μM) cell growth. METHODS: CCA cells were treated with Tanespimycin (0.6 μM) for 72 hours, and the expression levels of target proteins were detected by Western Blot. RESULTS: Tanespimycin downregulated Bcl-2, Survivin and Cyclin B1 and upregulated cleaved PARP.
• Cell Research:
  Cells were seeded in 96-well plates at 2,000 cells per well in a final culture volume of 100 μl for 24 h before the addition of increasing concentrations of 17-AAG that was incubated for 5 days. Viable cell number was determined using the Celltiter 96 AQueous Nonradioactive Cell Proliferation Assay. The value of the background absorbance at 490 nm (A490) of wells not containing cells was subtracted. Percentage of viable cells (A490 of 17-AAG treated sample/A490 untreated cells) × 100. The IC50 was defined as the concentration that gave rise to 50% viable cell number .
• Animal Research:
  B10.BR mice were inoculated with 5×10^5 lymphoma cells through intraperitoneal injection. Seven days following tumor implantation, the mice were I.P. injected with 17-AAG or vehicle (10% DMSO + 40% Cremophor EL: Ethanol (3:1) (v/v) + 50 % PBS) every other day for three weeks. At the cessation of treatment, mice were monitored up to 80 days post tumor cell injection. To determine the effects of 17-AAG on lymphoma initiation in vivo, secondary B10.BR recipient mice were implanted by intraperitoneal injection of 1×10^5 lymphoma cells from the spleens of first-round mice that had been treated with 17-AAG or vehicle. These mice were followed up to 160 days post tumor cell injection to monitor differences in tumor initiation between the mice .

Storage & Handling

• Storage: RT
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Tanespimycin

Compound Identifiers

PubChem CID

6505803