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  3. CX-6258 hydrochloride

CX-6258 hydrochloride 

目录号: HY-18095B
产品使用指南

CX-6258 hydrochloride是一种强效的、激酶选择性的 pan-Pim 激酶抑制剂,对 Pim-1, Pim-2 和 Pim-3 作用的 IC50 值分别为 5 nM、25 nM 和 16 nM。

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CX-6258 hydrochloride Chemical Structure

CX-6258 hydrochloride Chemical Structure

CAS No. : 1353859-00-3

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Description

CX-6258 hydrochloride is a potent and kinase selective pan-Pim kinases inhibitor, with IC50s of 5 nM, 25 nM and 16 nM for Pim-1, Pim-2 and Pim-3, respectively[1].

IC50 & Target

IC50: 5 nM (Pim-1), 25 nM (Pim-2), 16 nM (Pim-3)[1].

In Vitro

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].
CX-6258 treatment (12 mM, 3 h) treatment diminishes steady-state levels of ectopic NKX3.1 in PC3 cells[2].
CX-6258 treatment results in a significant reduction in NKX3.1 half-life[2].

Western Blot Analysis[1]

Cell Line: MV-4-11 human AML cells.
Concentration: 0.1 μM, 1 μM, 10 μM.
Incubation Time: 2 hours.
Result: Caused 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.
In Vivo

CX-6258 (50-100 mg/kg; p.o; daily; over a period of 21 days) exhibits robust in vivo efficacy in two Pim kinases driven tumor models[1].

Animal Model: Nude mice, MV-4-11 xenograft models[1]
Dosage: 50 mg/kg, 100 mg/kg.
Administration: Oral administration; once daily; over a period of 21 days.
Result: Exhibitd dose dependent efficacy, with a 50 mg/kg dose producing 45% tumor growth inhibition (TGI) and a 100 mg/kg dose producing 75% TGI.
Molecular Weight

498.40

Formula

C₂₆H₂₅Cl₂N₃O₃

CAS No.

1353859-00-3

SMILES

O=C1NC2=CC=C(Cl)C=C2/C1=C\C3=CC=C(C4=CC=CC(C(N5CCCN(C)CC5)=O)=C4)O3.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

CX-6258CX6258CX 6258PimPim kinasesBad4E-BP1Inhibitorinhibitorinhibit

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CX-6258 hydrochloride
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HY-18095B
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