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Biological Activity
ENMD-2076 has selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold selective for Aurora A than over Aurora B and less potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and PDGFRα. Phase 2.
Targets
| Target | Value |
|---|---|
| FLT3 | IC50: 1.86nM |
| RET | IC50: 10.4nM |
| AuroraA | IC50: 14nM |
| VEGFR3/FLT4 | IC50: 15.9nM |
| Src | IC50: 20.2nM |
| NTRK1/TRKA | IC50: 24.2nM |
| CSF-1R/c-Fms | IC50: 24.8nM |
| LCK | IC50: 43.7nM |
| FAK | IC50: 54.9nM |
| PDGFRα | IC50: 56.4nM |
| VEGFR2/KDR | IC50: 58.2nM |
| BLK | IC50: 69.4nM |
| FGFR2 | IC50: 70.8nM |
| YES1 | IC50: 78.4nM |
| Abl1(T315I) | IC50: 81.3nM |
| FGFR1 | IC50: 92.7nM |
| Fyn | IC50: 112nM |
| JAK2 | IC50: 120nM |
| Kit | IC50: 120nM |
| AuroraB | IC50: 350nM |
| In vitro (25°C) | DMSO | 101 mg/mL (268.99 mM) | |
| Water | 1 mg/mL (2.66 mM) | ||
| Ethanol | Insoluble | ||
| In vivo | 0.5% CMC+0.25% Tween 80 | 28 mg/mL | |
|
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
|||
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 26.63 mL | 133.16 mL | 266.31 mL |
| 0.5 mM | 5.33 mL | 26.63 mL | 53.26 mL |
| 1 mM | 2.66 mL | 13.32 mL | 26.63 mL |
| 5 mM | 0.53 mL | 2.66 mL | 5.33 mL |
*The above data is based on the productmolecular weight 375.5 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Catalog Num | A10352 |
|---|---|
| Actions | Inhibitor |
| CAS No. | 934353-76-1, 1291074-87-7 |
| Formula | C21H25N7 |
| M. Wt | 375.5 |
| Purity | >98% |
| Synonyms | ENMD2076, ENMD 2076 |
| SMILES | CC1=CC(=NN1)NC2=NC(=NC(=C2)N3CCN(CC3)C)/C=C/C4=CC=CC=C4 |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
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