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CX-6258 hydrochloride

Catalog No. T6148Cas No. 1353859-00-3
Alias Pim-Kinase Inhibitor X, CX-6258 HCl

CX-6258 hydrochloride (Pim-Kinase Inhibitor X) is an effective, orally efficacious Pim1/2/3 kinase inhibitor (IC50: 5/25/16 nM).

CX-6258 hydrochloride

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).
Pack SizePriceAvailabilityQuantity
1 mg$36In Stock
5 mg$80In Stock
10 mg$129In Stock
25 mg$247In Stock
50 mg$396In Stock
100 mg$596In Stock
200 mg$847In Stock
1 mL x 10 mM (in DMSO)$89In Stock
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Purity:98.00%
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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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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
For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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