Language:English
Language:

Xcessbio

Place your promotion here

You have no items in your shopping cart.

AGI-6780, Mutant IDH2 Inhibitor

AGI-6780, Mutant IDH2 Inhibitor

$109.00
The first highly potent and selective small molecule mutant IDH2 inhibitor.
Catalog No. Unit Price Qty
M60105-2s 2 mg solid $109.00
M60105-2 10 mM DMSO (0.415 mL) $109.00
M60105-50s 50 mg solid $750.00

Details

Product Information
Chemical Name: N-cyclopropyl-4-(thiophen-3-yl)-3-(3-(3-(trifluoromethyl)phenyl)ureido)benzenesulfonamide
Molecular Weight: 481.51
Formula: C21H18F3N3O3S2
Purity: ≥98%
CAS#: 1432660-47-3
Solubility: DMSO up to 50 mM
Storage: Powder: 4oC 1 year DMSO: 4oC 3 month -20oC 1 year



Biological Activity:

AGI-6780 is the first highly potent and selective small molecule inhibitor of mutant IDH2, which binds in an allosteric manner at the dimer interface of mutant IDH2-R140Q.  It 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. 


How to Use:

In vitro:  AGI-6780 was suggested to be used at 1-5 µM final concentration in vitro.

In vivo:  n/a


Reference:

  1. 1. Fang Wang, et al. Targeted Inhibition of Mutant IDH2 in Leukemia Cells Induces Cellular Differentiation. (2013) Science. 340(6132):622-6.




Products are for research use only. Not for human use.

Description

Details

Product Information
Chemical Name: N-cyclopropyl-4-(thiophen-3-yl)-3-(3-(3-(trifluoromethyl)phenyl)ureido)benzenesulfonamide
Molecular Weight: 481.51
Formula: C21H18F3N3O3S2
Purity: ≥98%
CAS#: 1432660-47-3
Solubility: DMSO up to 50 mM
Storage: Powder: 4oC 1 year DMSO: 4oC 3 month -20oC 1 year



Biological Activity:

AGI-6780 is the first highly potent and selective small molecule inhibitor of mutant IDH2, which binds in an allosteric manner at the dimer interface of mutant IDH2-R140Q.  It 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. 


How to Use:

In vitro:  AGI-6780 was suggested to be used at 1-5 µM final concentration in vitro.

In vivo:  n/a


Reference:

  1. 1. Fang Wang, et al. Targeted Inhibition of Mutant IDH2 in Leukemia Cells Induces Cellular Differentiation. (2013) Science. 340(6132):622-6.




Products are for research use only. Not for human use.

Reviews

Write Your Review

How do you rate this product? *

Price:
Value:
Quality: