AT-101 (AT101)
AT101
CAS: 866541-93-7
Molecular Formula: C32H34O10
AT-101 (AT101) - Names and Identifiers
| Name | AT101 |
| Synonyms | AT101 AT101 acetate AT-101 (AT101) AT-101 (acetic acid) (-)-Gossypol acetic acid AT-101 [2,2'-Binaphthalene]-8,8'-dicarboxaldehyde, 1,1',6,6',7,7'-hexahydroxy-3,3'-dimethyl-5,5'-bis(1-methylethyl)-, (2R)-, compd. wi |
| CAS | 866541-93-7 |
AT-101 (AT101) - Physico-chemical Properties
| Molecular Formula | C32H34O10 |
| Molar Mass | 578.60636 |
| Storage Condition | -20℃ |
| In vitro study | AT-101 inhibits a group of different lymphoproliferative malignancies. After 24 hours of treatment, the IC50 is 1.2 μm to 7.4 μm. After 48 hours of treatment, the IC50 was 0.7 μm to 3.9 μm, and after 72 hours of treatment, the IC50 was 0.3 μm to 1.7 μm. AT-101 (10 μm) disrupts mitochondrial membrane potential (Δψm) in diffuse large B- cell and mantle cell lymphoma cell lines in a concentration-and time-dependent manner. AT-101 (1 μm or 2 μm) in combination with Carfilzomib (6 nM or 10 nM) induced apoptosis in HBL-2 and Granta cell lines. Treatment of CLL lymphocytes in suspension culture and stromal cell co-culture with AT-101(20 μm) for 24 hours resulted in 72% apoptosis and down-regulation of Mcl-1. AT-101 acts on stromal cells that express undetectable levels of anti-apoptotic but have high levels of activated ERK and AKT proteins, resulting in low or no apoptosis. AT-101 induced apoptosis in Jurkat T and U937 cells with ED50 values of 1.9 mM and 2.4 mM, respectively, in a time-and dose-dependent manner. The combination of AT-101(10 μm) and radiation (32 Gy) induced more apoptosis than radiation alone, and the therapeutic effect exceeded the sum of the effects caused by single-dose therapy. AT-101 activated SAPK/JNK in a dose-and time-dependent manner. AT-101(10 µm) acts on VCaP cells by activating caspase-9, -3, And -7 induced apoptosis. AT-101 (10 µm) acts on VCaP cells to reduce Bcl-2 and Mcl-1 expression. AT-101 (< 20 μm) also inhibits multiple myeloma cell growth. AT-101 (10 μm) induces apoptosis in multiple myeloma cells by activating caspases 3, caspases 9 and PARP. AT-101(10 μm) promotes apoptosis in multiple myeloma cells by disrupting the Bax/Bcl-2 ratio and mitochondrial membrane potential. |
| In vivo study | AT-101 treatment of SCID beige mice bearing RL-DLBCL xenograft tumors, AT-101 was still detectable in plasma, with an average concentration of 0.49 μm in the 35 mg/kg group, the average concentration in the 200 mg/kg group was 0.39 μm. SCID beige mice were treated with AT-101, and peak plasma concentrations were observed 30 min later, mean plasma concentrations were almost 4-fold higher in the 200 mg/kg group than in the 35 mg/kg group (7.88 μm and 27.78 μm, respectively). AT-101(25 mg/kg to 100 mg/kg) orally administered to SCID beige mice, the early onset of weight loss corresponds to the use of more than 10% pretreatment. AT-101(35 mg/kg, daily oral treatment for 10 days) in combination with Cyclophosphamide (Cy)(I. P.) and Rituximab (R)(I. P.), there was a significant tumor volume control effect compared to any other treatment group. AT-101(15 mg/kg, oral treatment, 5 days per week) alone treated intact mice, AT weeks 2 to 6, compared with untreated mice, significantly reduced the incidence of VCaP tumor growth. AT-101 combined with surgical castration delayed the onset of hormone-independent VCaP tumor growth compared with castration alone or AT-101 alone. |
AT-101 (AT101) - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.728 ml | 8.641 ml | 17.283 ml |
| 5 mM | 0.346 ml | 1.728 ml | 3.457 ml |
| 10 mM | 0.173 ml | 0.864 ml | 1.728 ml |
| 5 mM | 0.035 ml | 0.173 ml | 0.346 ml |
Last Update：2024-01-02 23:10:35
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Product Name: AT101 Visit Supplier Webpage Request for quotationCAS: 866541-93-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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