Product Name | Rebastinib (DCC-2036) |
---|---|
CAS | 1020172-07-9 |
Formula | C30H28FN7O3 |
MW | 553.59 |
Appearance | White to off-white powder |
Storage condition | Dry, dark and at 0 - 4 ℃ for short term (days to weeks) or -20 ℃ for long term (months to years). |
Rebastinib (formerly also known as DCC-2036), a novel, potent and orally bioavailable small-molecule inhibitor of multiple tyrosine kinases with potential antineoplastic activity, is a conformational control Bcr-Abl inhibitor for Abl1(WT) and Abl1(T315I) with IC50s of 0.8 nM and 4 nM. It also inhibits other kinases such as SRC, LYN, FGR, HCK, KDR, FLT3, and Tie-2, and has low activity towards c-Kit. DCC-2036 inhibits ABL1 through forcing the kinase domains into inhibitor-bound, inactive Type II conformations. In cellular assay, DCC-2036 inhibits the proliferation of Ba/F3 and K562 cells with IC50 values of 5.4nM and 5.5nM, respectively.
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