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CX-6258 hydrochloride

CX-6258 hydrochloride
CX-6258 hydrochloride (Pim-Kinase Inhibitor X) is an effective, orally efficacious Pim1/2/3 kinase inhibitor (IC50: 5/25/16 nM).
Catalog No. T6148Cas No. 1353859-00-3
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Purity:98.00%
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CX-6258 hydrochloride

Catalog No. T6148Alias Pim-Kinase Inhibitor X, CX-6258 HClCas No. 1353859-00-3

CX-6258 hydrochloride (Pim-Kinase Inhibitor X) is an effective, orally efficacious Pim1/2/3 kinase inhibitor (IC50: 5/25/16 nM).
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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2 mg$51In Stock
500 mg$1,330In Stock
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Product Introduction

Bioactivity
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.
AliasPim-Kinase Inhibitor X, CX-6258 HCl
Chemical Properties
Molecular Weight498.4
FormulaC26H24ClN3O3·HCl
Cas No.1353859-00-3
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM2.0064 mL10.0321 mL20.0642 mL100.3210 mL
DMSO/H2O
1mg5mg10mg50mg
5 mM0.4013 mL2.0064 mL4.0128 mL20.0642 mL
10 mM0.2006 mL1.0032 mL2.0064 mL10.0321 mL
20 mM0.1003 mL0.5016 mL1.0032 mL5.0161 mL
50 mM0.0401 mL0.2006 mL0.4013 mL2.0064 mL
100 mM0.0201 mL0.1003 mL0.2006 mL1.0032 mL

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Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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