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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

Purity: 98.00%
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.
Pack SizePriceAvailabilityQuantity
1 mg$36In Stock
2 mg$51In Stock
5 mg$80In Stock
10 mg$147In Stock
25 mg$267In Stock
50 mg$447In Stock
100 mg$643In Stock
500 mg$1,330In Stock
1 mL x 10 mM (in DMSO)$89In 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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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。
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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