A 1331852

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Cat.No. 7661 - A 1331852 | C38H38N6O3S | CAS No. 1430844-80-6
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)
Datasheet
Citations
Reviews
Literature (4)
Pathways (1)

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.

Select a batch to recalculate based on the batch molecular weight:
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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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


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Keywords: A 1331852, A 1331852 supplier, A1331852, potent, selective, bclxl, bcl-xl, inhibitors, antitumor, apoptosis, apoptotic, xenograft, lymphoma, SCLC, breast, leukemia, senescent, biliary, epithelial, cells, EBV, epstein, barr, virus, Bcl-2, Family, Other, Apoptosis, 7661, Tocris Bioscience

Citations for A 1331852

Citations are publications that use Tocris products.

Currently there are no citations for A 1331852. Do you know of a great paper that uses A 1331852 from Tocris? Please let us know.

Reviews for A 1331852

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Literature in this Area

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Pathways for A 1331852

Apoptosis Signaling Pathway

Apoptosis Signaling Pathway

Apoptosis is a physiological process for cell death that is critical during aging and development. It may also be referred to as cell 'suicide'. Apoptosis can be triggered by events both inside and outside of the cell.