1370256-78-2

Basic information

• Product Name: 1-(5-(7-(3-morpholinopropoxy)quinazolin-4-ylthio)-1,3,4-thiadiazol-2-yl)-3-p-tolylurea
• Synonyms: 1-(5-(7-(3-morpholinopropoxy)quinazolin-4-ylthio)-1,3,4-thiadiazol-2-yl)-3-p-tolylurea;N-(4-Methylphenyl)-N'-[5-[[7-[3-(4-morpholinyl)propoxy]-4-quinazolinyl]thio]-1,3,4-thiadiazol-2-yl]urea;SKLB4771;AOB5016;CHEMBL2046883;SKLB477
• CAS NO: 1370256-78-2
• Molecular Formula: C₂₅H₂₇N₇O₃S₂
• Molecular Weight: 537.65698
• EINECS: -0
• Product Categories: Inhibitors
• Mol File: 1370256-78-2.mol
• Article Data: 1

Chemical Properties

• Appearance: /
• Density: 1.43±0.1 g/cm3(Predicted)
• PKA: 6.62±0.50(Predicted)
• CAS DataBase Reference: 1-(5-(7-(3-morpholinopropoxy)quinazolin-4-ylthio)-1,3,4-thiadiazol-2-yl)-3-p-tolylurea(CAS DataBase Reference)
• NIST Chemistry Reference: 1-(5-(7-(3-morpholinopropoxy)quinazolin-4-ylthio)-1,3,4-thiadiazol-2-yl)-3-p-tolylurea(1370256-78-2)
• EPA Substance Registry System: 1-(5-(7-(3-morpholinopropoxy)quinazolin-4-ylthio)-1,3,4-thiadiazol-2-yl)-3-p-tolylurea(1370256-78-2)

Safety Data

• Hazardous Substances Data: 1370256-78-2(Hazardous Substances Data)

Usage

Uses

FLT3-IN-1, is a FLT3 inhibitor.

Upstream product

• 16499-57-3 7-fluoro-3H-quinazolin-4-one 
• 196603-91-5 7-(3-morpholinopropoxy)quinazolin-4(3H)-one 
• 199327-94-1 4-(3-((4-chloro-quinazolin-7-yl)oxy)propyl)morpholine 
• 710311-95-8 1-(5-mercapto-[1,3,4]thiadiazol-2-yl)-3-p-tolylurea 
• 4441-30-9 3-morpholin-4-ylpropan-1-ol 

Relevant articles and documents

Discovery of the novel potent and selective FLT3 inhibitor 1-{5-[7-(3-morpholinopropoxy)quinazolin-4-ylthio]-[1,3,4]thiadiazol-2-yl} -3-p-tolylurea and its anti-acute myeloid leukemia (AML) activities in vitro and in vivo

Structure-activity relationship (SAR) studies of 2-(quinazolin-4-ylthio) thiazole derivatives, which are for optimizing the in vitro and in vivo antiacute myeloid leukemia (AML) activity of a previously identified FLT3 inhibitor 2-(6,7-dimethoxyquinazolin-4-ylthio)thiazole (1), are described. SAR studies centering around the head (thiazole) and tails (6- and 7-positions) of the quinazoline moiety of 1 led to the discovery of a series of compounds that exhibited significantly increased potency against FLT3-driven AML MV4-11 cells. Preliminary in vivo assays were carried out on three highly active compounds, whose results showed that 1-{5-[7-(3-morpholinopropoxy)quinazolin-4-ylthio]-[1, 3,4]thiadiazol-2-yl}-3-p-tolylurea (20c) had the highest in vivo activity. Further in vitro and in vivo anti-AML studies were then performed on 20c; in an MV4-11 xenograft mouse model, a once-daily dose of 20c at 100 mg/kg for 18 days led to complete tumor regression without obvious toxicity. Western blot and immunohistochemical analysis were carried out to illustrate the mechanism of action of 20c.