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Biological Activity
P276-00 is a novel CDK1, CDK4 and CDK9 inhibitor with IC50 of 79 nM, 63 nM and 20 nM, respectively. In Phase 2/3
Targets
| Target | Value |
|---|---|
| CDK9/CyclinT1 | IC50: 20nM |
| CDK4/CyclinD1 | IC50: 63nM |
| CDK1/CyclinB | IC50: 79nM |
| CDK2/CyclinA | IC50: 224nM |
| CDK6/CyclinD3 | IC50: 396nM |
| CDK2/CyclinE | IC50: 2.54μM |
| GSK-3β | IC50: 2.771μM |
| CDK7/CyclinH | IC50: 2.87μM |
| c-Src | IC50: <10μM |
| PKCα | IC50: 10μM |
| MAPK1 | IC50: 22μM |
| PKC | IC50: 25μM |
| MAPK2 | IC50: >100μM |
| PKA | IC50: 575μM |
| In vitro (25°C) | DMSO | 79 mg/mL (180.24 mM) | |
| Water | 79 mg/mL (180.24 mM) | ||
| Ethanol | 6 mg/mL (13.69 mM) | ||
| In vivo | 30% propylene glycol, 5% Tween 80, 65% D5W | 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 | 22.82 mL | 114.08 mL | 228.15 mL |
| 0.5 mM | 4.56 mL | 22.82 mL | 45.63 mL |
| 1 mM | 2.28 mL | 11.41 mL | 22.82 mL |
| 5 mM | 0.46 mL | 2.28 mL | 4.56 mL |
*The above data is based on the productmolecular weight 438.3. 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 | A13547 |
|---|---|
| Actions | Inhibitor |
| CAS No. | 920113-03-7 |
| Formula | C21H20ClNO5.HCl |
| M. Wt | 438.3 |
| Purity | >98% |
| Synonyms | P276, P276-00 |
| SMILES | CN1CC[[email protected]]([[email protected]@H]1CO)C2=C(C=C(C3=C2OC(=CC3=O)C4=CC=CC=C4Cl)O)O.Cl |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
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