LCL161

SKU: orb1306530

Description

LCL161 is an orally active SMAC mimetic and IAP antagonist, potently inhibiting cIAP1 (IC50=0.4 nM) and XIAP (IC50=35 nM). It demonstrates potential antitumor activity and has been utilized in preclinical research, including in vitro studies in cancer cell lines and in vivo models evaluating its efficacy against various tumors.

Research Area

Cell Biology

Key Properties

• CAS Number: 1005342-46-0
• MW: 500.63
• Purity: 99.79%
• Formula: C₂₆H₃₃FN₄O₃S
• SMILES: C([C@@H](NC([C@@H](NC)C)=O)[C@H]1CCCCC1)(=O)N2[C@@H](CCC2)C3=NC(C(=O)C4=CC=C(F)C=C4)=CS3
• Target: IAP
• Solubility: DMSO:93 mg/mL (185.77 mM);Ethanol:16 mg/mL (31.96 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  CIAP1 (MDA-MB-231 cells):0.4 nM|XIAP (HEK293 cells):35 nM
• In Vivo:
  METHODS: To test the antitumor activity in vivo, LCL161 (50 mg/kg twice daily) and PKC412 (40 mg/kg once daily) were administered by gavage to NCr nude mice injected with Ba/F3-FLT3-ITD-luc+ tumor cells for seven days. RESULTS: LCL161 significantly enhanced the ability of PKC412 to inhibit the growth of Ba/F3-FLT3-ITD-luc+ cells in vivo.The difference between the inhibition of leukemia growth by PKC412 or LCL161 alone and the combination of PKC412+LCL161 was also significant.The percentage of spleen weights in mice treated with PKC412+LCL161 was smaller than that in mice treated with PKC412. Mice treated with PKC412+LCL161 had a smaller percent spleen weight than mice treated with the vector or either drug alone.
• In Vitro:
  METHODS: MOLM13 cells were treated with LCL161 (1000-160,000 nM) and PKC412 (2.5-40 nM) for 3 days and cell viability was measured by trypan blue exclusion. RESULTS: LCL161 moderately inhibited cell growth when administered alone.Combined treatment of MOLM13-luc+ cells with LCL161 and PKC412 killed significantly more cells than either drug alone, and the Calcusyn Combination Index suggests a synergistic effect. METHODS: NSCLC cells A549 and H460 were treated with LCL161 (10 µM) and paclitaxel (10 µM) for 48 h. Apoptosis was detected by flow cytometry. RESULTS: Apoptosis was significantly reduced in the LCL161/paclitaxel combination treatment group compared to cells treated with LCL161 or paclitaxel alone.
• Cell Research:
  In vitro testing is performed using DIMSCAN (Only for Reference)

Storage & Handling

• Storage: keep away from direct sunlight,store at low temperature,store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

cIAP, LCL 161, LCL161, LCL-161, IAP, Inhibitor, inhibit

Compound Identifiers

PubChem CID

25113054