AGI-6780

Min.Order / FOB Price:Get Latest Price

100 Gram	FOB Price: USD 1.0000

100 Gram

FOB Price: USD 1.0000

Min.Order :100 Gram
Purity: 98%
Payment Terms : L/C

Keywords

AGI-6780 AGI6780;N-cyclopropyl-4-(thiophen-3-yl)-3-(3-(3-(trifluoroMethyl)phenyl)ureido)benzenesulfonaMide;N-Cyclopropyl-4-(3-thienyl)-3-[[[[3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-benzenesulfonamide;B 1432660-47-3

Quick Details

Appearance:White crystal
Application:CAS：1432660-47-3； Cell signaling pathway inhibitor
PackAge:100g,500g,1kg,25kg/drum
ProductionCapacity:1000|Gram|Week
Storage:Dry seal
Transportation:shipping

Superiority:

We are specialized in custom synthesis, chemical/pharmaceutical/ pesticides outsourcing and contract research.

We are committed to provide excellence in researching, manufacturing and drug discovery process.

Our research team of scientists consists of western-trained Ph.D.s with experience and capabilities in drug R&D methodologies and medicinal chemistry.

Details:

AGI-6780 is the first highly potent and selective small molecule inhibitor of isocitrate dehydrogenases, which binds in an allosteric manner at the dimer interface of mutant IDH2-R140Q (IC50=23 nM).
IC50 Value: 23 nM (IDH2-R140Q) [1]
Target: mutant IDH2-R140Q
in vitro: AGI-6780 inhibits IDH2-R140Q in vitro with an IC50 ~23 nM and inhibits 2-HG formation in human glioblastoma U87 and TF-1 cells expressing IDH2-R140Q with IC50 < 20 nM. AGI-6780 can reverse the differentiation blockade in TF-1 cells conferred by IDH2-R140Q, and induce blast differentiation in primary human IDH2-R140Q AML patient samples. It provides proof-of-concept that inhibitors targeting mutant IDH2-R140Q could have potential applications as a differentiation therapy for cancer [1].
in vivo: N/A
Toxicity: N/A
Clinical trial: Phase I Study of AG-221 in Subjects With Advanced Hematological Malignancies With an IDH2 Mutation. Phase 1