DUN09716

DUN09716 is KRAS inhibitor with potential antitumor activity. DUN09716 was reported inn patent US 9884046.

Product information

CAS Number: 300809-71-6

Molecular Weight: 292.81

Formula: C13H9ClN2S2

Synonym:

DUN-09716

DUN 09716

Chemical Name: 4-[(Benzo[d]thiazol-2-yl)thio]-3-chloroaniline

Smiles: NC1=CC(Cl)=C(C=C1)SC1=NC2=CC=CC=C2S1

InChiKey: DTSNLMOLTVGCGZ-UHFFFAOYSA-N

InChi: InChI=1S/C13H9ClN2S2/c14-9-7-8(15)5-6-11(9)17-13-16-10-3-1-2-4-12(10)18-13/h1-7H,15H2

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 250 mg/mL (853.80 mM; Need ultrasonic)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

DUN09716 bound to KRASG12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity of -5.38, -5.41, and -3.97 kcal/mol, respectively. DUN09716 (0-100 μM) shows strong inhibition selectivity in NSCLC cells with IC50s ranging from 39.56 to 66.02 μM for H2122, H358 and H460 cells (at 72 hours). DUN09716 (0-100 μM; 24 hours) blocks GTP-KRAS formation in H2122, H358 and H460 cells. DUN09716 (25-100 μM; 48 hours) inhibits the activation of KRAS downstream signaling pathway. DUN09716 (0-100 μM; 24-72 hours) induces cell cycle arrest and apoptosis in NSCLC.

References:

1. Xie C, et al. Identification of a New Potent Inhibitor Targeting KRAS in Non-small Cell Lung Cancer Cells. Front Pharmacol. 2017;8:823. Published 2017 Nov 14.

Products are for research use only. Not for human use.