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Description: Potent and selective Bcl-xL inhibitor; antitumor and inducer of apoptosis
Chemical Name: 6-[8-[(2-Benzothiazolylamino)carbonyl]-3,4-dihydro-2(1H)-isoquinolinyl]-3-[5-methyl-1-(tricyclo[3.3.1.13,7]dec-1-ylmethyl)-1H-pyrazol-4-yl]-2-pyridinecarboxylic acid
Purity: ≥98% (HPLC)
Biological Activity for A 1331852
A 1331852 is a high affinity and selective Bcl-xL inhibitor (Ki <0.01 nM), also inhibits Bcl-W, Bcl-2, and Mcl-1 (Ki values are 4, 6 and 142 nM, respectively). A 1331852 inhibits Bcl-xL-dependent Molt 4 acute lymphoblastic leukemia cell growth in vitro (EC50 = 6 nM). It enhances antitumor effects of Docetaxel (Cat. No. 4056) and Venetoclax (Cat. No. 6960) in xenograft models of breast and lung cancer. A 1331852 also induces apoptosis in and clears senescent biliary epithelial cells (BECs), and induces apoptosis in xenograft models of EBV-associated T- and natural killer cell lymphoma.
Technical Data for A 1331852
| M. Wt | 658.81 |
| Formula | C38H38N6O3S |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1430844-80-6 |
| PubChem ID | 71565985 |
| InChI Key | QCQQONWEDCOTBV-UHFFFAOYSA-N |
| Smiles | O=C(C1=C(CN(C2=CC=C(C3=C(C)N(CC4(C5)CC(C[C@@H]5C6)CC6C4)N=C3)C(C(O)=O)=N2)CC7)C7=CC=C1)NC8=NC9=C(S8)C=CC=C9 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for A 1331852
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 13.18 | 20 |
Preparing Stock Solutions for A 1331852
The following data is based on the product molecular weight 658.81. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.2 mM | 7.59 mL | 37.95 mL | 75.89 mL |
| 1 mM | 1.52 mL | 7.59 mL | 15.18 mL |
| 2 mM | 0.76 mL | 3.79 mL | 7.59 mL |
| 10 mM | 0.15 mL | 0.76 mL | 1.52 mL |
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Product Datasheets for A 1331852
References for A 1331852
References are publications that support the biological activity of the product.
Bierbrauer et al (2020) A direct comparison of selective BH3-mimetics reveals BCL-XL, BCL-2 and MCL-1 as promising therapeutic targets in neuroblastoma. Br.J.Cancer 122 1544 PMID: 32203216
Moujalled et al (2020) Cotargeting BCL-2 and MCL-1 in high-risk B-ALL. Blood Adv. 4 2762 PMID: 32569380
Sasaki et al (2020) Increased p16INK4a-expressing senescent bile ductular cells are associated with inadequate response to ursodeoxycholic acid in primary biliary cholangitis. J.Autoimmun. 107 102377 PMID: 31812332
Sejic et al (2020) BCL-XL inhibition by BH3-mimetic drugs induces apoptosis in models of Epstein-Barr virus-associated T/NK-cell lymphoma. Blood Adv. 4 4775 PMID: 33017468
Leverson et al (2015) Exploiting selective BCL-2 family inhibitors to dissect cell survival dependencies and define improved strategies for cancer therapy. Sci.Transl.Med. 7 279ra40 PMID: 25787766
If you know of a relevant reference for A 1331852, please let us know.
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Citations for A 1331852
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Parkinson's Disease Poster
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.
Programmed Cell Death Poster
There are two currently recognized forms of programmed cell death: apoptosis and necroptosis. This poster summarizes the signaling pathways involved in apoptosis, necroptosis and cell survival following death receptor activation, and highlights the influence of the molecular switch, cFLIP, on cell fate.
Pathways for A 1331852
