Lacutoclax

SKU: orb2277623

Description

Lacutoclax (LP-108) is a selective, orally bioavailable Bcl-2 inhibitor. It demonstrates potent antitumor activity in preclinical models, supporting its investigation in hematological malignancies such as lymphoma and leukemia through both in vitro and in vivo experimental studies.

Research Area

Cell Biology

Key Properties

• CAS Number: 2291166-56-6
• MW: 923.52
• Formula: C₄₈H₅₅ClN₈O₇S
• SMILES: C(NS(=O)(=O)C1=CC(N(=O)=O)=C(NCC2CCOCC2)C=C1)(=O)C3=C(N4C5=C(NC=6C(=C5)C=CN6)O[C@H](C)C4)C=C(C=C3)N7CCN(CC8=C(CC(C)(C)CC8)C9=CC=C(Cl)C=C9)CC7
• Target: Bcl-2 Family

Bioactivity

• Target IC50:
  H146 cells: 0.23 μM|H1963 cells: 0.45 μM
• In Vivo:
  In NOD/SCID mice bearing H146 or H1963 xenografts, intravenous administration of Lacutoclax (25–100 mg/kg, once daily for 10 consecutive days) led to dose-dependent tumor growth inhibition. At 100 mg/kg, some tumors completely regressed. Treated mice maintained stable body weight with no significant toxicity, demonstrating strong antitumor efficacy and good tolerability.
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• In Vitro:
  In small cell lung cancer (SCLC) cell lines such as H146 and H1963, treatment with the active metabolite Lacutoclax (0.1–10 μM for 24–72 hours)inhibited cell proliferation, with IC₅₀ values of 0.23 μM and 0.45 μM, respectively. The treatment induced apoptosis as evidenced by caspase activation, PARP cleavage, and increased Annexin V-positive cells, indicating a mitochondrial pathway–dependent mechanism.
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Storage & Handling

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

Alternative Names

LP108, LP-108

Compound Identifiers

PubChem CID

153515493