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CX-6258

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Catalog No. T1834Cas No. 1202916-90-2
Alias CX 6258

CX-6258 is an orally valid Pim 1/2/3 kinase(IC50=5 nM/25 nM/16 nM) inhibitor. It has good biological activity and kinase specificity.

CX-6258

CX-6258

🥰Excellent
Purity: 95.88%
Catalog No. T1834Alias CX 6258Cas No. 1202916-90-2
CX-6258 is an orally valid Pim 1/2/3 kinase(IC50=5 nM/25 nM/16 nM) inhibitor. It has good biological activity and kinase specificity.
Pack SizePriceAvailabilityQuantity
1 mg29 €In Stock
5 mg69 €In Stock
10 mg102 €In Stock
25 mg208 €In Stock
50 mg311 €In Stock
100 mg471 €In Stock
200 mg658 €In Stock
1 mL x 10 mM (in DMSO)70 €In Stock
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Purity:95.88%
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Product Introduction

Bioactivity
Description
CX-6258 is an orally valid Pim 1/2/3 kinase(IC50=5 nM/25 nM/16 nM) inhibitor. It has good biological activity and kinase specificity.
Targets&IC50
Pim1:5 nM, Pim2:25 nM, Pim3:16 nM
In vitro
CX-6258 shows antiproliferative activity against a panel of human cancer cell lines with IC50 of 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 with combination index (CI50) values equal to 0.4 and 0.56, respectively. CX-6258 causes dose dependent inhibition of the phosphorylation of two pro-survival proteins, Bad and 4E-BP1, at the Pim kinase specific sites S112 and S65 and T37/46, respectively. [1]
Kinase Assay
Pim activity 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.
AliasCX 6258
Chemical Properties
Molecular Weight461.94
FormulaC26H24ClN3O3
Cas No.1202916-90-2
SmilesCN1CCCN(CC1)C(=O)c1cccc(c1)-c1ccc(\C=C2\C(=O)Nc3ccc(Cl)cc23)o1
Relative Density.1.309 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 22.5 mg/mL (48.71 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.1648 mL10.8239 mL21.6478 mL108.2392 mL
5 mM0.4330 mL2.1648 mL4.3296 mL21.6478 mL
10 mM0.2165 mL1.0824 mL2.1648 mL10.8239 mL
20 mM0.1082 mL0.5412 mL1.0824 mL5.4120 mL

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