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- Y Kaibori, .et al. EphA2 phosphorylation at Ser897 by the Cdk1/MEK/ERK/RSK pathway regulates M-phase progression via maintenance of cortical rigidity, the FASEB Journal, 2019, Jan 22:fj201801519RR PMID: 30668924
Biological Activity
NVP-BHG712 is a selective inhibitor of EphB4 kinase that exhibits selectivity for EphB4 over more than 40 other kinases in vitro, including FGFR3.
Targets
| Target | Value | |
|---|---|---|
| EphB4 | ED50 | 25nM |
| C-Raf | IC50: 0.395μM | |
| c-Src | IC50: 1.266μM | |
| c-Abl | IC50: 1.667μM | |
| Tie-2 | IC50: >10μM | |
| Axl | IC50: >10μM | |
| HER1 | IC50: >10μM | |
| PKA | IC50: >10μM | |
| CDK1 | IC50: >10μM | |
| PKB | IC50: >10μM | |
| PDK-1 | IC50: >10μM | |
| FGFR3 | IC50: >10μM | |
| c-Met | IC50: >10μM |
| In vitro (25°C) | DMSO | 90 mg/mL (178.75 mM) | |
| Water | Insoluble | ||
| Ethanol | 3 mg/mL (5.95 mM) | ||
| In vivo | NMP+PEG300 (10+90, v+v) | 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 | 19.86 mL | 99.3 mL | 198.61 mL |
| 0.5 mM | 3.97 mL | 19.86 mL | 39.72 mL |
| 1 mM | 1.99 mL | 9.93 mL | 19.86 mL |
| 5 mM | 0.4 mL | 1.99 mL | 3.97 mL |
*The above data is based on the productmolecular weight 503.5 . 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 | A10661 |
|---|---|
| Actions | Inhibitor |
| CAS No. | 940310-85-0 |
| Formula | C26H20F3N7O |
| M. Wt | 503.5 |
| Purity | >98% |
| Synonyms | NVPBHG712 |
| SMILES | CC1=C(C=C(C=C1)C(=O)NC2=CC=CC(=C2)C(F)(F)F)NC3=NC(=NC4=C3C=NN4C)C5=CN=CC=C5 |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
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