Powder: -20°C for 3 years
In solvent: -80°C for 2 years
CX-6258 HCl is an effective, orally efficacious Pim1/2/3 kinase inhibitor (IC50: 5/25/16 nM).
Description | CX-6258 HCl is an effective, orally efficacious Pim1/2/3 kinase inhibitor (IC50: 5/25/16 nM). |
Targets&IC50 | Pim3:16 nM, Pim1:5 nM, Pim2:25 nM |
In vitro | CX-6258 has anti-proliferative activity against a panel of human cancer cell lines (IC50: 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 (CI50: 0.4 and 0.56). |
In vivo | In mice carrying MV-4-11 xenografts, CX-6258 dose-dependently suppresses the tumor growth , with a 50/100 mg/kg dose producing 45%/75% tumor growth inhibition. |
Kinase 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 HCl, Pim-Kinase Inhibitor X |
Molecular Weight | 498.4 |
Formula | C26H25Cl2N3O3 |
CAS No. | 1353859-00-3 |
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
H2O: 82 mg/mL (164.5 mM)
DMSO: 53 mg/mL (106.3 mM)
Ethanol: 1 mg/mL (2.0 mM), warmed
( < 1 mg/ml refers to the product slightly soluble or insoluble )
You can also refer to dose conversion for different animals. More
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CX-6258 hydrochloride 1353859-00-3 JAK/STAT信号通路 表观遗传 Pim Pim-Kinase Inhibitor X CX6258 hydrochloride CX-6258 HCl CX6258 CX-6258 Pim kinases 4E-BP1 CX 6258 hydrochloride Inhibitor CX 6258 Bad inhibit inhibitor