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CX-6258

Catalog No. T1834   CAS 1202916-90-2
Synonyms: 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.

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CX-6258 Chemical Structure
CX-6258, CAS 1202916-90-2
Pack Size Availability Price/USD Quantity
1 mg In stock $ 34.00
2 mg In stock $ 48.00
5 mg In stock $ 80.00
10 mg In stock $ 128.00
25 mg In stock $ 255.00
50 mg In stock $ 413.00
100 mg In stock $ 590.00
200 mg In stock $ 857.00
1 mL * 10 mM (in DMSO) In stock $ 89.00
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Biological Description
Chemical Properties
Storage & Solubility Information
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 Pim3:16 nM, Pim 1:5 nM, Pim2:25 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.
Synonyms CX 6258
Molecular Weight 461.94
Formula C26H24ClN3O3
CAS No. 1202916-90-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 22.5 mg/mL (48.71 mM)

TargetMolReferences and Literature

1. Haddach M, et al. ACS Medicinal Chemistry Letters, 3 (2) , 135-139

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Inhibitor Library Kinase Inhibitor Library Bioactive Compounds Library Max Epigenetics Compound Library Anti-Liver Cancer Compound Library Anti-Pancreatic Cancer Compound Library Anti-Prostate Cancer Compound Library Anti-Cancer Compound Library Anti-Lung Cancer Compound Library

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TP-3654 TCS PIM-1 1 Pim1/AKK1-IN-1 FD1024 XL413 Hispidulin Pim-1/2 kinase inhibitor 1 AZD1208

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Keywords

CX-6258 1202916-90-2 Chromatin/Epigenetic JAK/STAT signaling Pim CX6258 Pim kinases Inhibitor inhibit Bad 4E-BP1 CX 6258 inhibitor

 

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