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TCS PIM-1 1 is a potent, ATP-competitive inhibitor of Pim-1 kinase. This compound displays selectivity over Pim-2 and MEK1/MEK2 (IC50 values are 50, >20000 and >20000 nM for Pim-1, Pim-2, and MEK1/MEK2, respectively). TCS PIM-1 1 bound convincingly within the ATP-binding site of Pim-1 suggesting an ATP-competitive inhibitory mechanism.
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Source | Cancer Lett (2012). Figure 2. TCS PIM-1 1 |
| Method | Effect of Pim-1 on microtubule formation | |
| Cell Lines | PC-3 cells | |
| Concentrations | - | |
| Incubation Time | 18 h | |
| Results | The knockdown of Pim-1 did not modify the effect of these agents on tubulin polymerizing activity, indicating that the induction and potentiation of apoptosis in Pim-1 knock- down cells were not relevant to tubulin dynamics when exposed to these agents. |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
| Molecular Weight | 367.2 |
| Formula | C18H11BrN2O2 |
| CAS Number | 491871-58-0 |
| Purity | >98% |
| Solubility | DMSO |
| Storage | at -20°C |
Identification and structure-activity relationships of substituted pyridones as inhibitors of Pim-1 kinase.
Cheney IW, et al. Bioorg Med Chem Lett. 2007 Mar 15;17(6):1679-83. PMID: 17251021.
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| TCS-PIM-1-4a
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AZD1208 is a potent, highly selective, and orally available Pim kinase inhibitor that effectively inhibits all three isoforms at <5 nM or <150 nM in enzyme and cell assays, respectively. |
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