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PIM447 (LGH447) is an oral, selective pan-PIM kinase inhibitor with antitumor and bone-protective effects. It inhibits PIM1, PIM2, and PIM3, induces apoptosis, and decreases the viability, proliferation, and motility of HuH6 and COA67 cells. PIM447 suppresses tumorigenesis in hepatocellular carcinoma and can be used in the study of multiple myeloma.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $118 | In Stock | |
5 mg | $293 | In Stock | |
10 mg | $478 | In Stock | |
25 mg | $767 | In Stock | |
50 mg | $987 | In Stock | |
1 mL x 10 mM (in DMSO) | $323 | In Stock |
Description | PIM447 (LGH447) is an oral, selective pan-PIM kinase inhibitor with antitumor and bone-protective effects. It inhibits PIM1, PIM2, and PIM3, induces apoptosis, and decreases the viability, proliferation, and motility of HuH6 and COA67 cells. PIM447 suppresses tumorigenesis in hepatocellular carcinoma and can be used in the study of multiple myeloma. |
Targets&IC50 | Pim1:6 pM (Ki), Pim3:9 pM (Ki), Pim2:18 pM (Ki) |
In vitro | HuH6 and COA67 cells were treated with PIM447 (0-20 μM, 72h), and the activity of PIM447 was significantly reduced with LD50 of 13 μM and 10 μM, respectively. Treatment with PIM447 (7.5 μM, 8h) resulted in increased apoptosis of HuH6 and COA67 cells. PIM447 (5 μM, 48h) reduced cancer cell dryness in HuH6 and COA67 cells. [1] |
In vivo | PIM447 significantly reduced tumor load and prevented tumor-associated bone loss in a disseminated mouse model of human myeloma. [2] |
Alias | PIM 447, LGH447, LGH 447 |
Molecular Weight | 440.46 |
Formula | C24H23F3N4O |
Cas No. | 1210608-43-7 |
Smiles | FC1=C(N=C(C(NC=2C(=CC=NC2)[C@@H]3C[C@H](C)C[C@H](N)C3)=O)C=C1)C4=C(F)C=CC=C4F |
Relative Density. | 1.290 g/cm3 (Predicted) |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 80 mg/mL (181.63 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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