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LCL161

Cat. No. M4801
LCL161 Structure
Synonym:

LCL-161

Size Price Availability Quantity
10mM*1mL in DMSO USD 120  USD120 In stock
5mg USD 105  USD105 In stock
10mg USD 150  USD150 In stock
25mg USD 310  USD310 In stock
50mg USD 550  USD550 In stock
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Quality Control & Documentation
Biological Activity

LCL161 enhanced the proapoptotic effects of nilotinib and PKC412, against leukemic disease in vitro and potentiated the activity of both kinase inhibitors against leukemic disease in vivo. In addition, LCL161 synergized in vivo with nilotinib to reduce leukemia burden significantly below the baseline level suppression exhibited by a moderate-to-high dose of nilotinib. Finally, LCL161 displayed antiproliferative effects against cells characterized by intrinsic resistance to tyrosine kinase inhibitors as a result of expression of point mutations in the protein targets of compound inhibition. T lymphocytes treated with LCL161 demonstrated significantly enhanced cytokine secretion upon activation, with little effect on CD4 and CD8 T-cell survival or proliferation. LCL161 treatment of peripheral blood mononuclear cells significantly enhanced priming of naïve T cells with synthetic peptides in vitro. LCL161 may be a useful agent in combination with paclitaxel to treat liver tumours.

Chemical Information
Molecular Weight 500.63
Formula C26H33FN4O3S
CAS Number 1005342-46-0
Solubility (25°C) DMSO: 100 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Infante JR, et al. J Clin Oncol. Phase I dose-escalation study of LCL161, an oral inhibitor of apoptosis proteins inhibitor, in patients with advanced solid tumors.

[2] Tian A, et al. Cancer Lett. Synergistic effects of IAP inhibitor LCL161 and paclitaxel on hepatocellular carcinoma cells.

[3] Knights AJ, et al. Cancer Immunol Immunother. Inhibitor of apoptosis protein (IAP) antagonists demonstrate divergent immunomodulatory properties in human immune subsets with implications for combination therapy.

[4] Weisberg E, et al. Leukemia. Smac mimetics: implications for enhancement of targeted therapies in leukemia.

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