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Lys05

Cat. No. M8783
Lys05 Structure
Synonym:

Lys01 trihydrochloride

Size Price Availability
5mg USD 100 4-7 Days
10mg USD 150 4-7 Days
25mg USD 300 4-7 Days
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

Lys05 (Lys01 trihydrochloride) is a dimeric chloroquine (CQ) that deacidifies the lysosome and causes impairment of lysosomal enzymes, exhibiting more than 10-fold higher autophagy inhibitory potency than hydroxychloroquine (HCQ) and CQ (LC3II/LC3I ratio = 15.4 post 4 hr 10 μM treatment in LN229 glioblastoma cells vs. <6.4 with 100 μM CQ or HCQ). Lys05 also shows higher anticancer activity both in vitro (IC50 3.6-6.0 μM vs. 15.6-23.8 μM with HCQ in 1205Lu, c8161, LN229, HT-29 cultures) and in mice in vivo (EC50 in reducing tumor growth rate ∼10 mg/kg/day i.p.; HT29 xenografts) with toxicity observed only at high doses (≥80 mg/kg) as a result of significant lysozyme reduction.

CAS#: 1391426-22-4 (free base)

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 549.75
Formula C23H23Cl2N5.3HCl
CAS Number 1391426-24-6
Purity >98%
Solubility DMSO 2 mg/mL
Water 5 mg/mL
Storage at -20°C
References

Autophagy inhibitor Lys05 has single-agent antitumor activity and reproduces the phenotype of a genetic autophagy deficiency.
McAfee Q, et al. Proc Natl Acad Sci U S A. 2012 May 22;109(21):8253-8. PMID: 22566612.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Lys05, Lys01 trihydrochloride supplier, Autophagy, inhibitors

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