| Bioactivity | ENMD-2076 is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively. | ||||||||||||
| Invitro | ENMD-2076 is selective toward Aurora A versus Aurora B (IC50=350 nM). ENMD-2076 inhibits HUVEC growth with an IC50 value of 0.15 mM. Against 10 human leukemia cell lines, the IC50 values range from 0.025 to 0.53 mM. Within this panel, MV4:11 cells are the most sensitive cells by a factor of greater than 4. The lymphoma-derived U937 cell line treated with ENMD-2076 shows that the ENMD-2076 induces a dose-dependent increase in G2-M-phase arrest as well as the induction of apoptosis. ENMD-2076 inhibits cellular Flt3 ligand (FL)-induced Flt3 autophosphorylation in THP-1 cells, which have been shown to express FL-responsive wild-type Flt- 3 (18) with an IC50 value of 28 nM. ENMD-2076 inhibits stem cell factor (SCF)-induced Kit autophosphorylation in MO7e cells with an IC50 value of 40 nM. ENMD-2076 inhibits VEGFR2/KDR autophosphorylation with an IC50 value of 7 nM[1]. | ||||||||||||
| Name | ENMD-2076 | ||||||||||||
| CAS | 934353-76-1 | ||||||||||||
| Formula | C21H25N7 | ||||||||||||
| Molar Mass | 375.47 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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ENMD-2076
CAS: 934353-76-1 F: C21H25N7 W: 375.47
ENMD-2076 is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt
Data collection：peptidedb@qq.com
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