Cat. No. Name Size Price Add Cart
KI2798ABT-19910 mg$330
ABT-19950 mg$870

Chemical Characteristic

Product NameABT-199
SynonymsABT199,GDC0199,RG7601
CAS No.1257044-40-8
Molecular Weight 868.44
FormulaC45H50ClN7O7S
Chemical Name4-[4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-N-[3-nitro-4-(oxan-4-ylmethylamino)phenyl]sulfonyl-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide
SmilesC(=O)(c1c(cc(cc1)N1CCN(CC1)CC1=C(CC(CC1)(C)C)c1ccc(cc1)Cl)Oc1cc2c(nc1)[nH]cc2)NS(=O)(=O)c1cc(c(cc1)NCC1CCOCC1)[N](=O)O
Chemical Structure
DocumentsHNMR HPLC

Biological activities

ABT-199 is a potent and selective BCL-2 inhibitor. ABT-199 inhibits BCL-2 with an IC50 of < 0.010 nM.[1] ABT-199 also shows less sensitivity to Bcl-xL, Mcl-1 and Bcl-w with IC50s of 48, 444 and 245 nM, respectively. The EC50s of ABT-199 against FL5.12-Bcl-2, FL5.12-Bcl-xL and RS4;11 cells are 4, 261 and 8 nM, respectively.[1] In vitro, ABT-199 potently kills a diverse array of non-Hodgkin?? lymphoma (NHL) and acute myelogenous leukemia cell lines by the mitochondrial pathway of apoptosis.[2] In vivo, in human hematologic tumor xenograft models, ABT-199 suppresses tumor growth and shows at least additive efficacy in combination with chemotherapy.[2]

Protocols

In vitro, ABT-199 is dissolved in DMSO.[2]

References

[1]Souers AJ, et al. ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets. Nat Med. 2013, 19(2): 202-208.
[2]Davids MS, et al. ABT-199: taking dead aim at BCL-2. Cancer Cell. 2013, 23 (2): 139-141.

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