A 1331852
Tocris Bioscience, part of Bio-Techne | Catalog # 7661
Potent and selective Bcl-xL inhibitor; antitumor and inducer of apoptosis
Key Product Details
Description
Potent and selective Bcl-xL inhibitor; antitumor and inducer of apoptosis
Product Description
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.Product Specifications
Molecular Weight
658.81
Formula
C38H38N6O3S
Storage
Store at -20°C
Purity
≥98% (HPLC)
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
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.
Solubility
| 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Leverson Exploiting selective BCL-2 family inhibitors to dissect cell survival dependencies and define improved strategies for cancer therapy. Sci.Transl.Med. 2015 PMID: 25787766
- Sejic BCL-XL inhibition by BH3-mimetic drugs induces apoptosis in models of Epstein-Barr virus-associated T/NK-cell lymphoma. Blood Adv. 2020 PMID: 33017468
- Moujalled Cotargeting BCL-2 and MCL-1 in high-risk B-ALL. Blood Adv. 2020 PMID: 32569380
- Sasaki Increased p16INK4a-expressing senescent bile ductular cells are associated with inadequate response to ursodeoxycholic acid in primary biliary cholangitis. J.Autoimmun. 2020 PMID: 31812332
- Bierbrauer A direct comparison of selective BH3-mimetics reveals BCL-XL, BCL-2 and MCL-1 as promising therapeutic targets in neuroblastoma. Br.J.Cancer 2020 PMID: 32203216
Product Specific Notices for A 1331852
For research use only
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