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Background Information:
DCC-2036 is a unique switch-pocket, non-ATP competitive (allosteric) inhibitor with IC50 at low nanomolar concentration against a number of tyrosine kinases including FLT3 (1.7 nM), TRKA (7.0 nM), TIE-2 (2.7 nM) and BCR-ABL (2.0 nM). DCC-2036 has shown promising activity in a phase I/II clinical trial in chronic myeloid leukemia (CML), where plasma concentrations of 350 nM of DCC-2036 have been safely achieved. DCC-2036 has induced clinical and molecular remissions in patients with TKI-resistant CML expressing the ‘gate-keeper’ T315I BCR-ABL mutation, as well as demonstrated activity against mutations that cause BCR-ABL conformational escape resistant.
Reference:
1. W. W. Chan, et al., Cancer Cell. April 12, 2011; 19, 556-568.
2. C. A. Eide, et al., Cancer Res. 2011 May 1; 71(9): 3189–3195.
APIM050139: DCC-2036 (REBASTINIB)
CAS No.: 1020172-07-9.
Molecular Formula: C30H28FN7O3.
Molecular Weight: 553.59.
Purity: >99% (HPLC).
QC: 1HNMR, HPLC and MS.
Solubility: Soluble in DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.
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