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AT-101

Cat. No. M1860
AT-101 Structure
Synonym:

R-(-)-gossypol acetic acid

Size Price Availability
25mg USD 250  USD250 Out of stock
50mg USD 400  USD400 Out of stock
100mg USD 650  USD650 Out of stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

AT-101 (R-(-)-gossypol acetic acid) is a polyphenolic compound isolated from cottonseeds. AT-101 induces Apoptosis through activation of caspase-9, -3, and -7 in VCaP cells. It inhibits Bcl-2 by acting as a BH3 mimetic and disrupts the heterodimerization of Bcl-2 with proapoptotic family members. AT-101 was found to mimic the proapoptosis proteins and is able to bind to the BH3 domains of Bcl-2, Mcl-1, and Bcl-xL. AT-101 has been shown to be therapeutically active as a single agent in several mouse models including breast, prostate, colon, and non-small cell lung cancer. We demonstrate that AT-101 administration delays the onset of androgen-independent prostate cancer in vivo. The use of AT-101 and ADT may further delay the onset of AI disease, resulting in prolonged progression-free survival of prostate cancer.

Protocol
Cell Experiment
Cell lines HDMEC, OSCC3, UM-SCC-17B, UM-SCC-74A cells line
Preparation method SRB assay
Sulforhodamine B (SRB) cytotoxicity assays were done as described (25). Briefly, cells were seeded at 2×103 cells per well of 96-well plates, allowed to attach overnight, and treated with AT101 and/or taxotere for 72–96 hours. Cells were fixed with 10% trichloroacetic acid, stained with 0.4% SRB (Sigma-Aldrich, St. Louis, MO) in 1% acetic acid, and plates were read in a microplate reader at 560 nm (GENios; Tecan, Graz, Austria). Test results were normalized against initial plating density and drug-free controls. Data were obtained from triplicate wells per condition and is representative of three independent experiments.
Concentrations 0~100µM
Incubation time 72-96 h
Animal Experiment
Animal models SCID Mouse Model of Human Tumor Angiogenesis
Formulation resuspended in carboxymethyl cellulose and sonicated for 30 minutes
Dosages 10mg/kg daily or 70mg/kg weekly
Administration orally
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 518.56
Formula C30H30O8
CAS Number 90141-22-3
Purity >98%
Solubility DMSO
Ethanol
Storage at -20°C
References

[1] Imai A, et al. Cancer Res. Metronomic dosing of BH3 mimetic small molecule yields robust antiangiogenic and antitumor effects.

[2] Baggstrom et al. J Thorac Oncol. A phase II study of AT-101 (Gossypol) in chemotherapy-sensitive recurrent extensive-stage small cell lung cancer.

[3] Ready et al. J Thorac Oncol. Double-blind, placebo-controlled, randomized phase 2 study of the proapoptotic agent AT-101 plus docetaxel, in second-line non-small cell lung cancer.

[4] McGregor et al. J Cell Biochem. AT-101 (R-(-)-gossypol acetic acid) enhances the effectiveness of androgen deprivation therapy in the VCaP prostate cancer model.

[5] Moretti et al. J Thorac Oncol. AT-101, a pan-Bcl-2 inhibitor, leads to radiosensitization of non-small cell lung cancer.

[6] Zerp et al. Radiat Oncol. AT-101, a small molecule inhibitor of anti-apoptotic Bcl-2 family members, activates the SAPK/JNK pathway and enhances radiation-induced apoptosis.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: AT-101, R-(-)-gossypol acetic acid supplier, Bcl-2, inhibitors

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