CX-6258

Alias: CX6258; CX 6258;CX-6258
Cat No.:V2552 Purity: ≥98%
CX-6258 is a novel, potent, selective and orally bioactive pan-Pim kinase inhibitor with IC50 of 5 nM, 25 nM and 16 nM for Pim1, Pim2, and Pim3, respectively.
CX-6258 Chemical Structure CAS No.: 1202916-90-2
Product category: Pim
This product is for research use only, not for human use. We do not sell to patients.
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25mg
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Other Forms of CX-6258:

  • CX-6258 hydrochloride hydrate
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

CX-6258 is a novel, potent, selective and orally bioactive pan-Pim kinase inhibitor with IC50 of 5 nM, 25 nM and 16 nM for Pim1, Pim2, and Pim3, respectively. At CX-6258 showed robust antiproliferative potencies against all cell lines tested derived from human solid tumors and hematological malignancies. In mechanistic cellular assays with MV-4-11 human AML cells, caused dose-dependent inhibition of the phosphorylation of 2 pro-survival proteins, Bad and 4E-BP1, at the Pim kinase specific sites S112 and S65 and T37/46, respectively.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
Two pro-survival proteins, Bad and 4E-BP1, are phosphorylated at Pim kinase specific sites S112, S65, and T37/46, respectively, and are inhibited by CX-6258 in a dose-dependent manner[1]. In PC3 cells, CX-6258 treatment (12 mM, 3 h) reduces steady-state levels of ectopic NKX3.1[2]. The half-life of NKX3.1 is significantly shortened by CX-6258 treatment[2].
ln Vivo
In two tumor models driven by Pim kinases, CX-6258 (50–100 mg/kg; po; daily; for 21 days) shows strong in vivo efficacy[1].
Cell Assay
Western Blot Analysis[1]
Cell Types: MV-4-11 human AML cells
Tested Concentrations: 0.1 μM, 1 μM, 10 μM
Incubation Duration: 2 hrs (hours)
Experimental Results: 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.
Animal Protocol
Animal/Disease Models: Nude mice, MV-4-11 xenograft
Doses: 50 mg/kg, 100 mg/kg
Route of Administration: Oral administration; one time/day; over a period of 21 days
Experimental Results: demonstrated dose dependent efficacy, with a 50 mg/kg dose producing 45% tumor growth inhibition ( TGI) and a 100 mg/kg dose producing 75% TGI.
References
[1]. Mustapha Haddach, Jerome Michaux, Michael K, Discovery of CX-6258. A Potent, Selective, and Orally Efficacious pan-Pim Kinases Inhibitor. ACS Med. Chem. Lett., 2012, 3 (2), pp 135-139
[2]. Padmanabhan A, Gosc EB, Bieberich CJ. Stabilization of the prostate-specific tumor suppressor NKX3.1 by the oncogenic protein kinase Pim-1 in prostate cancer cells. J Cell Biochem. 2013 May;114(5):1050-7.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C26H24CLN3O3
Molecular Weight
461.94
CAS #
1202916-90-2
SMILES
O=C1NC2=CC=C(Cl)C=C2/C1=C\C3=CC=C(C4=CC=CC(C(N5CCCN(C)CC5)=O)=C4)O3
Synonyms
CX6258; CX 6258;CX-6258
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 10 mM
Water:<1 mg/mL
Ethanol:<1 mg/mL
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.1648 mL 10.8239 mL 21.6478 mL
5 mM 0.4330 mL 2.1648 mL 4.3296 mL
10 mM 0.2165 mL 1.0824 mL 2.1648 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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