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CX-6258 hydrochloride

Catalog No. T6148 CAS 1353859-00-3

Synonyms: CX-6258 HCl, Pim-Kinase Inhibitor X

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

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CX-6258 hydrochloride, CAS 1353859-00-3

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Purity: 98%

Biological Description

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Storage & Solubility Information

Description	CX-6258 HCl is an effective, orally efficacious Pim1/2/3 kinase inhibitor (IC50: 5/25/16 nM).
Targets&IC50	Pim3:16 nM, Pim1:5 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.

Synonyms	CX-6258 HCl, Pim-Kinase Inhibitor X
Molecular Weight	498.4
Formula	C26H25Cl2N3O3
CAS No.	1353859-00-3

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

H2O: 82 mg/mL (164.5 mM)

DMSO: 53 mg/mL (106.3 mM)

Ethanol: 1 mg/mL (2.0 mM), warmed

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References 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：

Anti-Cancer Compound Library Hematonosis Compound Library Anti-Pancreatic Cancer Compound Library Inhibitor Library Immunology/Inflammation Compound Library Covalent Inhibitor Library Anti-Cancer Active Compound Library Kinase Inhibitor Library Chromatin Modification Compound Library Apoptosis Compound Library

Related Products

Related compounds with same targets

Hispidulin CX-6258 hydrochloride Pim1/AKK1-IN-1 SMI-16a K00135 (2R)-Octyl-α-hydroxyglutarate CX-6258 M-110

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

CX-6258 hydrochloride 1353859-00-3 JAK/STAT信号通路表观遗传 Pim Pim-Kinase Inhibitor X CX6258 hydrochloride CX-6258 HCl CX6258 CX-6258 Pim kinases 4E-BP1 CX 6258 hydrochloride Inhibitor CX 6258 Bad inhibit inhibitor

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