1610505-50-4

Basic information

• Product Name: C₁₆H₁₂N₄S₂
• Synonyms: C₁₆H₁₂N₄S₂
• CAS NO: 1610505-50-4
• Molecular Weight: 324.43
• Mol File: 1610505-50-4.mol
• Article Data: 3

Chemical Properties

• CAS DataBase Reference: C₁₆H₁₂N₄S₂(CAS DataBase Reference)
• NIST Chemistry Reference: C₁₆H₁₂N₄S₂(1610505-50-4)
• EPA Substance Registry System: C₁₆H₁₂N₄S₂(1610505-50-4)

Safety Data

• Hazardous Substances Data: 1610505-50-4(Hazardous Substances Data)

Upstream product

• 100-47-0 benzonitrile 
• 276670-60-1 5′-amino-[2,3′-bithiophene]-4′-carbonitrile 
• 885524-09-4 4-chloro-2-phenyl-5-thiophen-2-yl-thieno[2,3-d]pyrimidine 
• 10432-44-7 2-[1-(thiophen-2-yl)ethylidene]malononitrile 
• 88-15-3 2-Acetylthiophene 

Relevant articles and documents

Synthesis and biological evaluation of novel thieno[2,3-d]pyrimidine-based FLT3 inhibitors as anti-leukemic agents

The most common mutations in acute myeloid leukemia (AML) are those that cause the activation of FMS-like tyrosine kinase 3 (FLT3). Therefore, FLT3 is regarded as a potential target for the treatment of AML. A novel series of thieno[2,3-d]pyrimidine-based analogs was designed and synthesized as FLT3 inhibitors. All synthesized compounds were assayed for the tyrosine kinase activity of FLT3 and growth inhibitory activity in four human leukemia cell lines (THP1, MV4-11, K562, and HL-60). Among these compounds, compound 17a, which possesses relatively short and simple substituents at the C6 position of thieno[2,3-d]pyrimidine, emerged as the most promising anti-leukemic agent. Compound 17a exhibited potent inhibition of FLT3-positive leukemic cell growth and of the FLT3 D835Y kinase; such inhibition is required for the successful treatment of AML. The data supports the further investigation of this class of compounds as potential anti-leukemic agents.

Discovery of thienopyrimidine-based FLT3 inhibitors from the structural modification of known IKKβ inhibitors

Inactivation of the NF-κB signaling pathway by inhibition of IKKβ is a well-known approach to treat inflammatory diseases such as rheumatoid arthritis and cancer. Thienopyrimidine-based analogues were designed through modification of the known IKKβ inhibitor, SPC-839, and then biologically evaluated. The resulting analogues had good inhibitory activity against both nitric oxide and TNF-α, which are well-known inflammatory responses generated by activated NF-κB. However, no inhibitory activity against IKKβ was observed with these compounds. The thienopyrimidine-based analogues were subsequently screened for a target kinase, and FLT3, which is a potential target for acute myeloid leukemia (AML), was identified. Thienopyrimidine-based FLT3 inhibitors showed good inhibition profiles against FLT3 under 1 μM. Overall, these compounds represent a promising family of inhibitors for future development of a treatment for AML.