KRN383
KRN383 is a novel Flt3 inhibitor with potential anticancer activity. KRN383 inhibited the autophosphorylation of Flt3 bearing internal tandem duplications (ITDs) and the Asp835Tyr (D835Y) point mutation with half-maximal inhibitory concentration (IC(50)) values of < or =5.9 and 43 nM, respectively. KRN383 also inhibited the proliferation of the ITD-positive cell lines with IC(50) values of < or =2.9 nM. A single oral administration of 80 mg/kg of KRN383 eradicated ITD-positive xenograft tumors in nude mice and prolonged the survival of SCID mice carrying ITD-positive AML cells. The effectiveness of a single oral dose of KRN383 suggests that it has the potential to be used in a wide variety of clinical regimens, including multicycle and combination therapies.
| Supplier | BOC Sciences |
|---|---|
| Product # | 919767-02-5 |
| Pricing | Inquire |
| Cas | 919767-02-5 |
| Molecular Weight | 327.34 |
| Molecular Formula | C17H17N3O4 |
| Canonical SMILES | COC1=CC2=C(C=CN=C2C=C1O)OC3CC=C(C=C3)NC(=O)N |