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A-1331852

Chemical Structure : A-1331852

CAS No.: 1430844-80-6

A-1331852 (A1331852;A 1331852)

Catalog No.: PC-45700Not For Human Use, Lab Use Only.

A-1331852 (A1331852) is a potent and selective BCL-XL inhibitor (Ki<10 pM).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

A-1331852 (A1331852) is a potent and selective BCL-XL inhibitor (Ki<10 pM).
A-1331852 shows much weaker affinity for BCL-2 (Ki=6 nM), BCL-W (Ki=4 nM), and MCL-1 (Ki=142 nM).
A-1331852 selectively disrupts BCL-XL–BIM complexes and induces the hallmarks of apoptosis in BCL-XL–dependent Molt-4 cells (Molt-4 viability IC50=6 nM).
A-1331852 demonstrates antitumor efficacy in the Molt-4 xenograft model; orally active.

Physicochemical Properties

M.Wt 658.8117
Formula C38H38N6O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 12 mg/mL

Chemical Name/SMILES

2-Pyridinecarboxylic acid, 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]-

References

1. Leverson JD, et al. Sci Transl Med. 2015 Mar 18;7(279):279ra40.

2. Punnoose EA, et al. Mol Cancer Ther. 2016 May;15(5):1132-44.

3. Lucas CM, et al. Leukemia. 2016 Jun;30(6):1273-81.

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