A 1331852

Name: A 1331852
Brand: Tocris Bioscience
SKU: 7661

Tocris Bioscience, part of Bio-Techne | Catalog # 7661

COA / SDS

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
Chemical Name:	6-[8-[(2-Benzothiazolylamino)carbonyl]-3,4-dihydro-2(1H)-isoquinolinyl]-3-[5-methyl-1-(tricyclo[3.3.1.1^3,7]dec-1-ylmethyl)-1H-pyrazol-4-yl]-2-pyridinecarboxylic acid
Purity:	≥98% (HPLC)
Molecular Weight:	658.81

View Full Technical Details for A 1331852

Technical Data
Citations

Biological Activity for A 1331852

A 1331852 is a high affinity and selective Bcl-xL inhibitor (K_i <0.01 nM), also inhibits Bcl-W, Bcl-2, and Mcl-1 (K_i 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 for A 1331852

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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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References for A 1331852

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 p16^INK4a-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-X_L, BCL-2 and MCL-1 as promising therapeutic targets in neuroblastoma. Br.J.Cancer 2020 PMID: 32203216