Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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 | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 34.00 | |
2 mg | In stock | $ 48.00 | |
5 mg | In stock | $ 80.00 | |
10 mg | In stock | $ 128.00 | |
25 mg | In stock | $ 255.00 | |
50 mg | In stock | $ 413.00 | |
100 mg | In stock | $ 590.00 | |
200 mg | In stock | $ 857.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 89.00 |
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 | Pim3:16 nM, Pim 1:5 nM, Pim2:25 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. |
Synonyms | CX 6258 |
Molecular Weight | 461.94 |
Formula | C26H24ClN3O3 |
CAS No. | 1202916-90-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 22.5 mg/mL (48.71 mM)
You can also refer to dose conversion for different animals. More
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CX-6258 1202916-90-2 Chromatin/Epigenetic JAK/STAT signaling Pim CX6258 Pim kinases Inhibitor inhibit Bad 4E-BP1 CX 6258 inhibitor