A-1155463

SKU: orb1300502

Description

A-1155463

Research Area

Cell Biology

Key Properties

• CAS Number: 1235034-55-5
• MW: 669.79
• Purity: 96.10% (May vary between batches)
• Formula: C₃₅H₃₂FN₅O₄S₂
• SMILES: C(NC1=NC=2C(S1)=CC=CC2)(=O)C3=C4C(CCN(C4)C5=NC(C(O)=O)=C(CCCOC6=C(F)C=C(C#CCN(C)C)C=C6)S5)=CC=C3
• Target: Bcl-2 Family
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:100 mg/mL (149.3 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (5.97 mM);DMSO:100 mg/mL (149.3 mM)

Bioactivity

• Target IC50:
  BCL-XL:<0.01 nM(Ki)|Bcl-2:80 nM (Ki)
• In Vivo:
  Following a single 5 mg/kg IP dose of A-1155463 in nontumor bearing SCID-Beige mice, platelet counts fall dramatically as measured at 6 h postdose and then rebound to normal levels within 72 h. Daily Dosing at 5 mg/kg IP to SCID-Beige mice that had been inoculated with BCL-XL-dependent H146 tumor cells for 14 days causes a statistically significant inhibition of tumor growth (maximum tumor growth inhibition = 44%), which is alleviated upon cessation of dosing.
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• In Vitro:
  A-1155463 disrupts BCL-XL-BIM but not BCL-2-BIM complexes in cells. A-1155463 kills BCL-XL-dependent Molt-4 cells (EC50=70 nM) but has no measurable cytotoxicity against BCL-2-dependent RS4;11 cells (EC50>5 mM). A-1155463 induces the hallmarks of apoptosis, as evidenced by the release of cytochrome c from mitochondria, caspase activation, and the accumulation of caspase-dependent sub-G0-G1 DNA content in BCL-XL-dependent H146 cells.
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• Cell Research:
  Cells are treated with increasing concentration of A-1155463. Cells are assayed for viability after 72 h using the CellTiter-Glo luminescent cell viability assay according to the manufacturer's protocol. Results are normalized to cells without treatment. EC50 is calculated using the GraphPad Prism software.(Only for Reference)
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• Animal Research:
  Animal Models: SCID-Beige MiceFormulation: 5% DMSO, 10% EtOH, 20% Cremaphor ELP, and 65% D5WDosages: 5 mg/kgAdministration: i.p.

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, inhibit, A 1155463, A1155463, A-1155463, Bcl-2, Bcl-2 Family, Bcl-xL

Compound Identifiers

PubChem CID

59447577