A-1155463

SKU: orb1226705

Description

A-1155463 is a highly potent and selective BCL-XL inhibitor (Ki=10 pM); shows >1000-fold weaker binding to BCL-2, BCL-W (Ki =19 nM) and MCL-1 (Ki >440 nM); inhibits H146 SCLC xenograft tumor growth in vivo.(In Vitro):A-1155463 shows picomolar binding affinity to BCL-XL (Ki＜0.01 nM), and >1000-fold weaker binding to BCL-2 (Ki= 80 nM) and related proteins BCL-W (Ki= 19 nM) and MCL-1 (Ki> 440 nM) . A-1155463 demonstrates strong growth inhibition of over half of the colorectal cell lines as defined by EC50 values ≤0.5 μM in the presence of 10 % FBS.(In Vivo):A-1155463 caused a mechanism-based and reversible thrombocytopenia in mice and inhibited H146 small cell lung cancer xenograft tumor growth in vivo following multiple doses.

Key Properties

• CAS Number: 1235034-55-5
• MW: 669.7881
• Purity: >98% (HPLC)
• Formula: C₃₅H₃₂FN₅O₄S₂
• SMILES: O=C(C1=C(CCCOC2=CC=C(C#CCN(C)C)C=C2F)SC(N3CC4=C(C=CC=C4C(NC5=NC6=CC=CC=C6S5)=O)CC3)=N1)O
• Target: Bcl-2
• Solubility: DMSO: ≥ 31 mg/mL

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

A1155463 | A 1155463

Quick Database Links

Gene Symbol

Bcl-2