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Apexbio Technology LLC DCC-2036 (Rebastinib) 1020172-07-9 50mg
Supplier: Apexbio Technology LLC B140450
DCC-2036 (Rebastinib CAS 1020172-07-9) is a synthetic small molecule that acts as a conformational control inhibitor of ABL1 kinase By binding simultaneously to the E282/R386 switch-control pocket and the Met318 ATP hinge region DCC-2036 promotes the inactive type II conformation of ABL1 It exhibits potent inhibition of wild-type ABL1 (IC50 0 8 nM) and retains activity against the gatekeeper mutant ABL1T315I (IC50 4 nM) DCC-2036 demonstrates non-ATP-competitive inhibition and suppresses the proliferation of Ba/F3 and K562 cells in vitro It also extends survival in mouse models engrafted with BCR-ABL1T315I leukemic cells indicating its utility in research on tyrosine kinase inhibitor resistance in leukemia
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