Free shipping on all orders over $ 500

Geldanamycin

Cat. No. M3561
Geldanamycin Structure
Synonym:

NSC 122750

Size Price Availability Quantity
5mg USD 90 In stock
10mg USD 140 In stock
50mg USD 400 In stock
Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Geldanamycin is a benzoquinone ansamycin antibiotic that binds to Hsp90 (Heat Shock Protein 90) and alters its function. Geldanamycin induces the degradation of proteins that are mutated in tumor cells such as v-Src, Bcr-Abl and p53 preferentially over their normal cellular counterparts. This effect is mediated via HSP90. Despite its potent antitumor potential, geldanamycin presents several major drawbacks as a compound candidate (namely, hepatotoxicity) that have led to the development of geldanamycin analogues, in particular analogues containing a derivatisation at the 17 position:17-AAG,17-DMAG.

Protocol
Cell Experiment
Cell lines A2780 human ovarian cell line
Preparation method Treating exponentially growing cells with Geldanamycin and assessing at various times DNA synthesis by incorporation of bromodeoxyuridine (BrdUrd) and flow cytometric analysis. No marked difference in total cell number is noted during this time course for treated and untreated cultures. BrdUrd (10 μM) is incorporated over a 4-h incubation period at 37 °C and cells are harvested and fixed in 70% ethanol. After denaturation of the DNA with 2 N HC1, incubating cells with an anti-BrdUrd mouse monoclonal antibody followed by a fluorescein isothiocyanate (FITC)-linked goat anti-mouse IgG. Staining cells for 30 minutes at room temperature with propidium iodide and analysing by flow cytometry using a Coulter EPICS Profile Analyzer.
Concentrations 0.001-10 μM
Incubation time 3 hours
Animal Experiment
Animal models FRE/erbB-2 tumors in nu/nu mice
Formulation Geldana50 mg/kgmycin is dissolved in DMSO.
Dosages 50 mg/kg
Administration Administered via i.p.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 560.64
Formula C29H40N2O9
CAS Number 30562-34-6
Purity >99%
Solubility DMSO 100 mg/mL
Storage at -20°C
Related HSP90 Products
Teprenone

Teprenone(Geranylgeranylacetone; GGA)is commonly utilized to protect the gastric mucosa in peptic ulcer disease; has been shown to protect the myocardium from ischemia/reperfusion by activating heat shock proteins.

Celastrol

Celastrol is a potent antioxidant and anti-inflammatory agent and a novel HSP90 inhibitor.

CH5138303

CH5138303 is an orally available Hsp90 inhibitor with Kd of 0.48 nM.

Retaspimycin

Retaspimycin is a novel, water-soluble, potent inhibitor of heat-shock protein 90 (Hsp90).

KW-2478

KW-2478 is a nonansamycin HSP90 inhibitor with IC50 of 3.8 nM.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Geldanamycin, NSC 122750 supplier, HSP90, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.