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DCC-2036, known as the lead "switch-control" inhibitor, 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. 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.
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Source | PLoS One (2013). Figure 1. DCC-2036 |
| Method | Immunoblotting | |
| Cell Lines | EOL-1 cells | |
| Concentrations | 6 nM | |
| Incubation Time | 24 h | |
| Results | DCC-2036 effectively decreased the phosphorylated-PDGFRa in BaF3 cells expressing FIP1L1-PDGFRa T674I mutant in a concentration- and time-dependent manner while the total protein level of PDGFRa was not affected. |
| Cell Experiment | |
|---|---|
| Cell lines | Ba/F3 cells or primary Ph+ leukemia cells |
| Preparation method | Cell Proliferation Assays Ba/F3 cells (3×103 cells/well) or primary Ph+ leukemia cells (5×104 cells/well) were plated in triplicate in 96-well plates containing test compounds. After 72h, viable cells were quantified by resazurin (O’Brien et al., 2000) or MTT (Roumiantsev et al., 2002) assay as described. Results represent an average of at least three independent experiments. |
| Concentrations | 0.1~10 mM |
| Incubation time | 72 h |
| Animal Experiment | |
|---|---|
| Animal models | Allograft and retroviral BM transduction/transplantation mouse models of BCR-ABL1-induced leukemia |
| Formulation | 0.5% CMC/1% Tween-80 |
| Dosages | 100 mg/kg once daily |
| Administration | oral gavage |
| Molecular Weight | 553.59 |
| Formula | C30H28FN7O3 |
| CAS Number | 1020172-07-9 |
| Solubility (25°C) | DMSO 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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