• Catalog Number:

  E1KS2634

• Amount:

  10mg1​ PHYSICAL AND CHEMICAL PROPERTIES

2​ Biological Activity DCC-2036 is an ABL switch control inhibitor with IC50 of 0.8 and 2 nM for u-ABL1native and p-ABL1native, respectively. DCC-2036 strongly prevents both unphosphorylated and phosphorylated ABL1 by inducing a type II inactive conformation, and retains efficacy against the majority of clinically relevant CML-resistance mutants, including T315I. DCC-2036 suppresses BCR-ABL1(T315I)-expressing cell lines, prolongs survival in mouse models of T315I mutant CML and B-lymphoblastic leukemia, and inhibits primary patient leukemia cells expressing T315I in vitro and in vivo, supporting its clinical development in TKI-resistant Ph(+) leukemia. In addition, DCC-2036 also inhibits other kinases with IC50 of 2,4,6,34,29 and 38 nM for Flt3, KDR, Tie2, Src, LYN and FGR kinases, respectively. [1] 3​ References: The ABL switch control inhibitor DCC-2036 is active against the chronic myeloid leukemia mutant BCR-ABLT315I and exhibits a narrow resistance profile. Eide CA et al. Cancer Res 2011 May 1;71(9):3189-95. Study Safety and Preliminary Efficacy of DCC-2036 in Patients With Leukemias Clinicaltrials October 2011 ; The pharmacological and toxicological properties of this product have not been fully investigated. Exercise caution in use and handling. This product must not be used in humans.