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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $36 | In Stock | |
2 mg | $51 | In Stock | |
5 mg | $80 | In Stock | |
10 mg | $147 | In Stock | |
25 mg | $267 | In Stock | |
50 mg | $447 | In Stock | |
100 mg | $643 | In Stock | |
500 mg | $1,330 | In Stock | |
1 mL x 10 mM (in DMSO) | $89 | In Stock |
Description | CX-6258 hydrochloride (Pim-Kinase Inhibitor X) is an effective, orally efficacious Pim1/2/3 kinase inhibitor (IC50: 5/25/16 nM). |
Targets&IC50 | Pim1:5 nM, Pim3:16 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. |
Alias | Pim-Kinase Inhibitor X, CX-6258 HCl |
Molecular Weight | 498.4 |
Formula | C26H24ClN3O3·HCl |
Cas No. | 1353859-00-3 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
Solubility Information | H2O: 82 mg/mL (164.5 mM) DMSO: 53 mg/mL (106.3 mM) Ethanol: 1 mg/mL (2.0 mM), Heating is recommended. | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO/H2O
DMSO/H2O
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