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R547 is a novel, selective inhibitor of cell cycle and transcriptional cyclin dependent kinases (CDKs) (Ki = 1, 3, and 1 nM for CDK1, CDK2, and CDK4, respectively) with excellent in vitro cellular potency that inhibits the growth of various human tumor cell lines.
Targets
| Target | Value |
|---|---|
| CDK4/CyclinD1 | ki: 1nM |
| CDK1/CyclinB | ki: 2nM |
| CDK2/CyclinE | ki: 3nM |
| PKA | ki: >5μM |
| PKB | ki: >5μM |
| PKCα | ki: >5μM |
| PKCβ | ki: >5μM |
| Fyn | ki: >5μM |
| EphB3 | ki: >5μM |
| SGK | ki: >5μM |
| KDR | ki: >5μM |
| FGFR | ki: >5μM |
| EGFR | ki: >5μM |
| PDGFR | ki: >5μM |
| IGFR | ki: >5μM |
| Src | ki: >5μM |
| FAK | ki: >5μM |
| AuroraA | ki: >5μM |
| GSK-3β | ki: 8μM |
| p38 | ki: >50μM |
| MAPK2 | ki: >50μM |
| In vitro (25°C) | DMSO | 56 mg/mL (126.85 mM) | |
| Water | Insoluble | ||
| Ethanol | Insoluble | ||
| In vivo | 1% hydroxyethyl cellulose+0.2% 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 | 22.65 mL | 113.26 mL | 226.53 mL |
| 0.5 mM | 4.53 mL | 22.65 mL | 45.31 mL |
| 1 mM | 2.27 mL | 11.33 mL | 22.65 mL |
| 5 mM | 0.45 mL | 2.27 mL | 4.53 mL |
*The above data is based on the productmolecular weight 441.45. 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 | A11190 |
|---|---|
| Actions | Inhibitor |
| CAS No. | 741713-40-6 |
| Formula | C18H21F2N5O4S |
| M. Wt | 441.45 |
| Purity | >98% |
| Synonyms | R-547 |
| SMILES | COC1=C(C(=C(C=C1)F)F)C(=O)C2=CN=C(N=C2N)NC3CCN(CC3)S(=O)(=O)C |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
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