DCC-2036 (Rebastinib)

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Cat No.

CEI-0258

CAS_No

1020172-07-9

Molecular Weight

553.59

Purity

>99%

Storage

2 years at -20 centigrade

Targets

v-Abl, c-Kit, PDGFR

Molecular Formula

C30H28FN7O3

Solubility

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.

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Our Products Cannot Be Used As Medicines Directly For Personal Use.

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