DUN09716 is KRAS inhibitor with potential antitumor activity. DUN09716 was reported inn patent US 9884046.
CAS Number: 300809-71-6
Molecular Weight: 292.81
Chemical Name: 4-[(Benzo[d]thiazol-2-yl)thio]-3-chloroaniline
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
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.
- 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.
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