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LYN-1604 2HCl

Cat. No. M10069
LYN-1604 2HCl Structure
Synonym:

LYN1604

Size Price Availability Quantity
2mg USD 145  USD145 In stock
5mg USD 247  USD247 In stock
10mg USD 375  USD375 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

LYN-1604 is a novel activator of ULK1, inducing cell death involved in ATF3, RAD21, and caspase3, accompanied by autophagy and apoptosis. LYN-1604 has an IC50 of 1.66 μM against MDA-MB-231 cells, and it binds to wild-type ULK1 with a binding affinity in the nanomole range (Kd=291.4 nM). The ULK1 (Y89A) mutant protein caused a sharp decrease in binding affinity with lower response and Kd than wild-type ULK1, ULK1 (K50A) and ULK1 (L53A) mutants.

Protocol
Cell Experiment
Cell lines MDA-MB-231 cells
Preparation method Cells are dispensed in 96-well plates at a density of 5 × 104 cells per mL. After 24 h of incubation, cells are treated with different concentrations of compounds for the indicated time periods. Cell viability is measured by the MTT assay.
Concentrations 0.5, 1.0 and 2.0 μM
Incubation time 24 h
Animal Experiment
Animal models MDA-MB-231 xenograft model (BALB/c nude mice)
Formulation -
Dosages 25 mg/kg, 50 mg/kg, 100 mg/kg
Administration intragastric administration
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 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.

Chemical Information
Molecular Weight 657.54
Formula C33H45Cl4N3O2
CAS Number 2088939-99-3
Purity >99%
Solubility Water 90 mg/mL
DMSO 45 mg/mL
Storage at -20°C
References

[1] Lan Zhang, et al. Chem Sci. Discovery of a small molecule targeting ULK1-modulated cell death of triple negative breast cancer in vitro and in vivo

[2] Liang Ouyang, et al. Autophagy. A small-molecule activator induces ULK1-modulating autophagy-associated cell death in triple negative breast cancer

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Keywords: LYN-1604 2HCl, LYN1604 supplier, ULK, inhibitors

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