[CAS NO. 1859141-26-6]  ROC-325

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PRODUCTS SPECIFICATIONS [1859141-26-6]

Catalog
SLK-S8527
Brand
Selleck
CAS
1859141-26-6

DESCRIPTION [1859141-26-6]

Overview

MDLMFCD31619252
Molecular Weight503.06
Molecular FormulaC28H27ClN4OS
SMILESO=C1C2=C(SC3=C1C=CC=C3)C(C)=CC=C2NCCN(CCNC4=CC=NC5=CC(Cl)=CC=C45)C

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM1.9878 mL9.9392 mL19.8783 mL
5 mM0.3976 mL1.9878 mL3.9757 mL
10 mM---
50 mM---

Description

ROC-325 is an orally available novel inhibitor of lysosomal-mediated which diminishes AML cell viability with the IC50 range of 0.7-2.2 μM.

Targets

Autophagy [1]

In vitro

Treatment with ROC-325 triggers all of the hallmark features of autophagy inhibition including the accumulation of autophagosomes with undegraded cargo, an increase in lysosomal membrane permeability, deacidification of lysosomes, and elevated LC3B, p62, and cathepsin D expression. In vitro treatment of a panel of human AML cell lines and normal human bone marrow progenitors demonstrate that ROC-325 diminishes AML cell viability (IC50 range 0.7-2.2 µM), antagonizes clonogenic survival, and induces apoptosis in a manner that is therapeutically selective.

In vivo

ROC-325 is well tolerated and no notable toxicities are observed other than a modest, non-significant reversible reduction in mean body weight. Oral administration of ROC-325 to mice bearing RCC xenografts is well tolerated and yields dose-dependent inhibition of tumor growth that is significantly more efficacious than a higher dose of HCQ.