DCC-2036 (Rebastinib)

DCC-2036 (Rebastinib)

报价:¥1298
供货周期: 7天
品牌:
型号: 2mg
货号: K1328
CAS号: 1020172-07-9
上海高创化学科技有限公司
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SKU:K1328   M. Wt:553.59  
Formula:C30H28FN7O3   Solubility:No  
Purity:>99%   Storage:2 years at -20 degrees centigrade  
CAS No.:1020172-07-9   Synonyms:N/A  
Chemical NameN/A
Biological Activity
Description DCC-2036 (Rebastinib)
Targets          
IC50 N/A        
In vitro The lead "switch-control" inhibitor, DCC-2036, can potently inhibit autophosphorylation of ABL and ABL(T315I) enzymes with IC50 of 0.8 nM and 4 nM. DCC-2036 inhibitS Ba/F3 cells expressing BCR-ABL and BCR-ABL(T315I) with IC50 of 19 nM and 63 nM. Ex vivo exposure of CML cells from patients harboring BCR-ABL or BCR-ABL(T315I) to DCC-2036 reveals marked inhibition of colony formation and reduces phosphorylation of the direct BCR-ABL target CrkL. DCC-2036 potently inhibits 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.
In vivo DCC-2036 inhibits 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.
Clinical Trials N/A
Features N/A

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