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AGI-6780 CAS NO.1432660-47-3
- FOB Price: USD: 1.00-1.00 /Gram Get Latest Price
- Min.Order: 100 Gram
- Payment Terms: L/C
- Available Specifications:
≥98.0%(100-500)Gram≥98.0%(1000-5000)Gram
- Product Details
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
- ProName: AGI-6780
- CasNo: 1432660-47-3
- Molecular Formula: C21H18F3N3O3S2
- Appearance: White crystal
- Application: CAS：1432660-47-3； Cell signaling path...
- DeliveryTime: 2 months
- PackAge: 100g,500g,1kg,25kg/drum
- Port: shang hai
- ProductionCapacity: 1000 Gram/Week
- Purity: 98%
- Storage: Dry seal
- Transportation: shipping
- LimitNum: 100 Gram
Superiority
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