| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
Gossypol Acetate (Pogosin, AT101; BL-193; AT-101) is a naturally occuring polyphenolic aldehyde with potential anticancer activity. It inhibit Bcl-xL and Bcl-2 proteins with Kis of 0.5-0.6 μM and 0.2-0.3 mM, respectively. It also acts as an inhibitor for various dehydrogenase enzymes. Gossypol, a known antispermatogenic agent from the cotton plant genus Gossypium, was found to inhibit yellow perch sperm motility in vitro and lactate dehydrogenase activity in spermatozoa when used in a dose-dependent manner. Gossypol has been approved to have antiproliferative and apoptosis-inducing effects on some kinds of cancer cell lines in vitro.
| ln Vitro |
One natural substance that has been investigated as an anticancer agent is gingsypol, which is extracted from cottonseeds and roots. Tested in multiple clinical trials, the racemic version of Gossypol [(±)-Gossypol] is well tolerated. -Gossypol) has a Ki of 0.5 to 0.6 μM when binding to the Bcl-xL protein. Additionally, (±)-Gossypol binds to Bcl-2 protein potently, with a Ki value of 0.2-0.3 mM. The (-)-Gossypol and (+)-Gossypol enantiomers are the two enantiomers of the natural racemic Gossypol. In 6-day MTT tests, the racemic form and all enantiomers of Gossypol are evaluated against UM-SCC-6 and UM-SCC-14A. shows higher growth inhibition in comparison to (+)-Gossypol compared to (±)-Gossypol in both evaluated cell lines (P<0.001). With (±)-Gossypol, an intermediate growth inhibitory impact is seen, however this effect is only noticeable at the higher dose (10 μM, P<0.0001)[1].
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| ln Vivo |
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| Additional Infomation |
Gossypol Acetic Acid is the naturally occurring acetic acid form of gossypol, and an orally available polyphenolic aldehyde derived mostly from cottonseed with potential antineoplastic activity. The biologic activities of gossypol acetic acid are similar to those of gossypol and include suppression of DNA replication, inhibition of tumor cell proliferation, and male contraceptive effects. (NCI04)
R-(-)-Gossypol Acetic Acid is the orally bioavailable solvate of the R-(-) enantiomer of gossypol and acetic acid with potential antineoplastic activity. As a BH3 mimetic, R-(-)-gossypol binds to the hydrophobic surface binding groove BH3 of the anti-apoptotic proteins Bcl-2 and Bcl-xL, blocking their heterodimerization with pro-apoptotic members of the Bcl-2 family of proteins such as Bad, Bid, and Bim; this may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. Racemic gossypol is a polyphenolic compound isolated from cottonseed. |
| Molecular Formula |
C32H34O10
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| Molecular Weight |
578.61
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| Exact Mass |
578.215
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| CAS # |
12542-36-8
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| Related CAS # |
Gossypol;303-45-7;(R)-(-)-Gossypol acetic acid;866541-93-7;(S)-Gossypol (acetic acid);1189561-66-7;(R)-(-)-Gossypol;90141-22-3
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| PubChem CID |
227456
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| Appearance |
Light yellow to yellow solid powder
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| Boiling Point |
707.9ºC at 760 mmHg
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| Melting Point |
164-168ºC
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| Flash Point |
395.9ºC
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| Vapour Pressure |
1.05E-20mmHg at 25°C
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| LogP |
6.473
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| Hydrogen Bond Donor Count |
7
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
42
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| Complexity |
811
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
NIOHNDKHQHVLKA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C30H30O8.C2H4O2/c1-11(2)19-15-7-13(5)21(27(35)23(15)17(9-31)25(33)29(19)37)22-14(6)8-16-20(12(3)4)30(38)26(34)18(10-32)24(16)28(22)36;1-2(3)4/h7-12,33-38H,1-6H3;1H3,(H,3,4)
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| Chemical Name |
acetic acid;7-(8-formyl-1,6,7-trihydroxy-3-methyl-5-propan-2-ylnaphthalen-2-yl)-2,3,8-trihydroxy-6-methyl-4-propan-2-ylnaphthalene-1-carbaldehyde
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.32 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7283 mL | 8.6414 mL | 17.2828 mL | |
| 5 mM | 0.3457 mL | 1.7283 mL | 3.4566 mL | |
| 10 mM | 0.1728 mL | 0.8641 mL | 1.7283 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05338931 | Recruiting | Drug: AT101(Anti-CD19 Chimeric Antigen Receptor T cell) |
B-cell Non Hodgkin Lymphoma | AbClon | March 15, 2022 | Phase 1 Phase 2 |
| NCT00934076 | Withdrawn | Drug: Tarceva plus AT-101 | Carcinoma, Non Small Cell Lung | University of Alabama at Birmingham | February 2010 | Phase 1 |
| NCT00848016 | Completed Has Results | Drug: R-(-)-gossypol acetic acid | Recurrent Adrenocortical Carcinoma Stage III Adrenocortical Carcinoma |
National Cancer Institute (NCI) | February 2009 | Phase 2 |
| NCT00286793 | Completed | Drug: AT-101 | Prostate Cancer | Ascenta Therapeutics | February 2006 | Phase 1 Phase 2 |
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