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CX-6258 is an orally valid Pim 1/2/3 kinase(IC50=5 nM/25 nM/16 nM) inhibitor. It has good biological activity and kinase specificity.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | 29 € | In Stock | |
5 mg | 69 € | In Stock | |
10 mg | 102 € | In Stock | |
25 mg | 208 € | In Stock | |
50 mg | 311 € | In Stock | |
100 mg | 471 € | In Stock | |
200 mg | 658 € | In Stock | |
1 mL x 10 mM (in DMSO) | 70 € | In Stock |
Description | CX-6258 is an orally valid Pim 1/2/3 kinase(IC50=5 nM/25 nM/16 nM) inhibitor. It has good biological activity and kinase specificity. |
Targets&IC50 | Pim1:5 nM, Pim2:25 nM, Pim3:16 nM |
In vitro | CX-6258 shows antiproliferative activity against a panel of human cancer cell lines with IC50 of 0.02-3.7 μM, mostly sensitive to acute leukemia cell lines. Combinations of CX-6258 with doxorubicin (10:1 molar ratio) and CX-6258 with paclitaxel (100:1 molar ratio) produces synergistic cell killing with combination index (CI50) values equal to 0.4 and 0.56, respectively. CX-6258 causes dose dependent inhibition of the phosphorylation of two pro-survival proteins, Bad and 4E-BP1, at the Pim kinase specific sites S112 and S65 and T37/46, respectively. [1] |
Kinase Assay | Pim activity assay: Pim-1 and Pim-2 inhibitions are measured in radiometric assays using human recombinant Pim-1 at [ATP] = 30 μM (substrate RSRHSSYPAGT) and human recombinant Pim-2 at [ATP] = 5 μM (substrate RSRHSSYPAGT). The radiometric assay for Pim-3 uses RSRHSSYPAGT as a substrate in the presence of [ATP] = 155 μM. |
Alias | CX 6258 |
Molecular Weight | 461.94 |
Formula | C26H24ClN3O3 |
Cas No. | 1202916-90-2 |
Smiles | CN1CCCN(CC1)C(=O)c1cccc(c1)-c1ccc(\C=C2\C(=O)Nc3ccc(Cl)cc23)o1 |
Relative Density. | 1.309 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
Solubility Information | DMSO: 22.5 mg/mL (48.71 mM) | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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