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AT-101

Cat. No. M1860
AT-101 Structure
Synonym:

R-(-)-gossypol acetic acid

Size Price Availability
25mg USD 250 Out of stock
50mg USD 400 Out of stock
100mg USD 650 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 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 518.56
Formula C30H30O8
CAS Number 90141-22-3
Purity >98%
Solubility DMSO
Ethanol
Storage at -20°C
References

Metronomic dosing of BH3 mimetic small molecule yields robust antiangiogenic and antitumor effects.
Imai A, et al. Cancer Res. 2012 Feb 1;72(3):716-25. PMID: 22158856.

A phase II study of AT-101 (Gossypol) in chemotherapy-sensitive recurrent extensive-stage small cell lung cancer.
Baggstrom et al. J Thorac Oncol. 2011 Oct;6(10):1757-60. PMID: 21918390.

Double-blind, placebo-controlled, randomized phase 2 study of the proapoptotic agent AT-101 plus docetaxel, in second-line non-small cell lung cancer.
Ready et al. J Thorac Oncol. 2011 Apr;6(4):781-5. PMID: 21289522.

AT-101 (R-(-)-gossypol acetic acid) enhances the effectiveness of androgen deprivation therapy in the VCaP prostate cancer model.
McGregor et al. J Cell Biochem. 2010 Aug 1;110(5):1187-94. PMID: 20589722.

AT-101, a pan-Bcl-2 inhibitor, leads to radiosensitization of non-small cell lung cancer.
Moretti et al. J Thorac Oncol. 2010 May;5(5):680-7. PMID: 20354451.

AT-101, a small molecule inhibitor of anti-apoptotic Bcl-2 family members, activates the SAPK/JNK pathway and enhances radiation-induced apoptosis.
Zerp et al. Radiat Oncol. 2009 Oct 23;4:47. PMID: 19852810.

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

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