A-1331852

SKU: orb1300501

Description

A-1331852 is a potent and selective BCL-XL inhibitor used in cancer research to induce apoptosis in malignant cells. It is applied in studies of hematologic cancers and solid tumors, with utility demonstrated in both in vitro cellular assays and in vivo xenograft models for investigating therapeutic efficacy.

Research Area

Cell Biology

Key Properties

• CAS Number: 1430844-80-6
• MW: 658.81
• Purity: 98.15% (May vary between batches)
• Formula: C₃₈H₃₈N₆O₃S
• SMILES: Cc1c(cnn1CC12CC3CC(CC(C3)C1)C2)-c1ccc(nc1C(O)=O)N1CCc2cccc(C(=O)Nc3nc4ccccc4s3)c2C1
• Target: Bcl-2 Family
• Solubility: Ethanol: < 1 mg/mL (insoluble or slightly soluble). H2O: < 1 mg/mL (insoluble or slightly soluble). DMSO: 150 mg/mL (227.68 mM), sonication is recommended

Bioactivity

• Target IC50:
  BCL-W:4 nM (Ki)|Bcl-2:6 nM (Ki)|BCL-XL:0.01 nM (Ki)|MCL1:142 nM (Ki)
• In Vivo:
  A-1331852 demonstrates antitumor efficacy in the Molt-4 xenograft model, inducing tumor regressions as a single agent.
• In Vitro:
  A-1331852 exhibits remarkable potency both as a single agent and in combination with TKIs in killing primary CD34+ CML cell. Also, It has remarkable potency in inducing apoptosis in these cells at low nanomolar concentrations as early as 1 h post-treatment.
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• Cell Research:
  Immunoprecipitation of BCL-XL is carried out in K562 cells, exposed to A-1331852 (100 nM) for 0-2 h, and the eluted complexes are immunoblotted for the indicated proteins. The input cell lysates and the immunodepleted supernatant (labeled as Flow-through) are immunoblotted to check the efficiency of the immunoprecipitation. (Only for Reference)
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• Animal Research:
  Mice: The growth inhibition of established tumors in SCID-bg mice is studied. A-1331852 is administered orally daily for 14 days at 25 mg/kg and docetaxel is administered intravenously at 7.5 mg/kg. The change of tumor volume is monitored daily. They are for reference only.
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Storage & Handling

• Storage: Pure form: -20°C for 3 years. In solvent: -80°C for 1 year.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Mcl-1, Inhibitor, inhibit, A1331852, A-1331852, A 1331852, Bcl-2, Bcl-2 Family, Bcl-W, BCL-XL

Compound Identifiers

PubChem CID

71565985