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  3. LYN-1604 dihydrochloride

LYN-1604 dihydrochloride 

Cat. No.: HY-101923B Purity: 98.73%
Handling Instructions

LYN-1604 dihydrochloride is a potent UNC-51-like kinase 1 (ULK1) activator (EC50=18.94 nM) for the research of triple negative breast cancer (TNBC).

For research use only. We do not sell to patients.

LYN-1604 dihydrochloride Chemical Structure

LYN-1604 dihydrochloride Chemical Structure

CAS No. : 2310109-38-5

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10 mM * 1  mL in DMSO USD 210 In-stock
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10 mg USD 255 In-stock
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25 mg USD 450 In-stock
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50 mg USD 750 In-stock
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100 mg USD 1150 In-stock
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Description

LYN-1604 dihydrochloride is a potent UNC-51-like kinase 1 (ULK1) activator (EC50=18.94 nM) for the research of triple negative breast cancer (TNBC)[1].

IC50 & Target[1]

ULK1

18.94 nM (EC50)

In Vitro

LYN-1604 is a potential ULK1 agonist (enzymatic activity=195.7% at 100 nM and IC50=1.66 μM against MDA-MB-231 cells) [1].
LYN-1604 binds to wild-type ULK1 with a binding affinity in the nanomole range (KD=291.4 nM) [1].
LYN-1604 (0.5, 1.0 and 2.0 μM) induces cell death via the ULK complex in MDA-MB-231 cells[1].
LYN-1604 (0.5-2 μM, 24 hours) induces remarkable up-regulation of Beclin-1 and degradation of p62, as well as transformation of LC3-I to LC3-II in MDA-MB-231 cells[1].
LYN-1604 induces ATG5-dependent autophagy via the ULK complex[1].
LYN-1604 can also increase cleavage of caspase3 and induce apoptosis[1].

Cell Viability Assay[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.5, 1.0 and 2.0 μM
Incubation Time:
Result: Induced cell death. Autophagy ratio was increased in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0, 0.5, 1, and 2 μM
Incubation Time: 24 hours
Result: Induced remarkable up-regulation of Beclin-1 and degradation of p62, as well as transformation of LC3-I to LC3-II.
In Vivo

LYN-1604 (low dose, 25 mg/kg; median dose, 50 mg/kg; high dose, 100 mg/kg; intragastric administration once a day for 14 days) inhibits the growth of xenograft TNBC by targeting ULK1-modulated cell death[1].

Animal Model: 24 female nude mice (BALB/c, 6-8 weeks, 20-22 g)[1]
Dosage: Low dose, 25 mg/kg; median dose, 50 mg/kg; high dose, 100 mg/kg
Administration: Intragastric administration; once a day for 14 days
Result: Significantly inhibited the growth of xenograft MDA-MB-231 cells. The body weights of mice were stable. By the end of the experiment, the liver and spleen weight indexes of mice were slightly increased in parts of the groups, while the kidney weight index was not affected in all dose groups.
Molecular Weight

657.54

Formula

C₃₃H₄₅Cl₄N₃O₂

CAS No.

2310109-38-5

SMILES

[H]Cl.ClC1=CC=C(C(CN2CCN(C(CN(CC(C)C)CC(C)C)=O)CC2)OCC3=CC=C(C=CC=C4)C4=C3)C(Cl)=C1.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (76.04 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5208 mL 7.6041 mL 15.2082 mL
5 mM 0.3042 mL 1.5208 mL 3.0416 mL
10 mM 0.1521 mL 0.7604 mL 1.5208 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (3.80 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (3.80 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

LYN-1604LYN1604LYN 1604ULKAutophagyApoptosisUnc-51 like kinaseactivatorULK1anti-tumorautophagytriplenegativebreastcancerTNBCInhibitorinhibitorinhibit

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Product Name:
LYN-1604 dihydrochloride
Cat. No.:
HY-101923B
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