A-1210477

SKU: orb1225982

Description

A-1210477 is a potent, selective Mcl-1 inhibitor that bind to Mcl-1 (Ki=0.45 nM) to disrupt MCL-1-BIM complexes, shows much weaker against Bcl-2 (Ki=132 nM) and Bcl-XL (Ki>660 nM); induces the hallmarks of intrinsic apoptosis and demonstrates single agent killing of multiple myeloma and non-small cell lung cancer cell lines, synergizes with the BCL-2/BCL-XL inhibitor navitoclax to kill a variety of cancer cell lines; also enhances cobimetinib-induced apoptosis in vitro.

Key Properties

• CAS Number: 1668553-26-1
• MW: 850.0366
• Purity: >98% (HPLC)
• Formula: C₄₆H₅₅N₇O₇S
• SMILES: O=C(C(N1CCN2CCOCC2)=C(CCCOC3=C(C=CC=C4)C4=CC=C3)C5=C1C(C6=C(COC7=CC=C(N8CCN(S(=O)(N(C)C)=O)CC8)C=C7)N(C)N=C6C)=CC=C5)O
• Target: Bcl-2
• Solubility: DMSO: < 4.8 mg/mL

Bioactivity

• In Vitro:
  A-1210477 (10 μM) reduces the amount of BIM co-immunoprecipitated with MCL-1 antibody, and triggers MCL-1 elevation in a variety of cancer cell lines, including the breast cancer cell line HCC-1806. A-1210477 inhibits MCL-1-NOXA interactions with an IC50 of approximately 1 μM, while having no effect on BCL-2-BIM or BCL-XL-BCL-XS interactions. The NSCLC cell lines H2110 and H23 are sensitive to A-1210477 with cell viability IC50<10 μM, confirming that A-1210477 can kill MCL-1-dependent cell lines.

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

A1210477

Quick Database Links

Gene Symbol

Bcl-2