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LCL161

Cat. No. M4801

LCL161 Structure

Synonym: LCL-161

Size Price Availability Quantity
5mg USD 120 In stock
10mg USD 180 In stock
50mg USD 540 In stock
100mg USD 800 In stock
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Quality Control
  • Current batch:
  • Purity 98%
  • COA
  • MSDS
Biological Activity

The novel IAP inhibitor, LCL161, [corrected] was observed to potentiate the effects of tyrosine kinase inhibition against leukemic disease both in the absence and presence of a stromal-protected [corrected] environment. 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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 500.63
Formula C26H33FN4O3S
CAS Number 1005342-46-0
Purity 98%
Solubility DMSO
Storage at -20°C
References

Phase I dose-escalation study of LCL161, an oral inhibitor of apoptosis proteins inhibitor, in patients with advanced solid tumors.
Infante JR, et al. J Clin Oncol. 2014 Oct 1;32(28):3103-10. PMID: 25113756.

Synergistic effects of IAP inhibitor LCL161 and paclitaxel on hepatocellular carcinoma cells.
Tian A, et al. Cancer Lett. 2014 Sep 1;351(2):232-41. PMID: 24976294.

Inhibitor of apoptosis protein (IAP) antagonists demonstrate divergent immunomodulatory properties in human immune subsets with implications for combination therapy.
Knights AJ, et al. Cancer Immunol Immunother. 2013 Feb;62(2):321-35. PMID: 22923192.

Smac mimetics: implications for enhancement of targeted therapies in leukemia.
Weisberg E, et al. Leukemia. 2010 Dec;24(12):2100-9. PMID: 20844561.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: LCL161, LCL-161 supplier, IAP, inhibitors

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