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CX-6258

In stock
Catalog No.
A3337
Pan-Pim kinases Inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$132.00
In stock
5mg
$90.00
In stock
10mg
$140.00
In stock
25mg
$270.00
In stock
50mg
$450.00
In stock

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Email: [email protected]

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Background

Pim kinases (Provirus Integration site for Moloney murine leukemia virus) are a family of serine/threonine kinases that regulate cell survival. This family of kinases is composed of three different isoforms (Pim-1, Pim-2, and Pim-3). The simultaneous inhibition of Pim-1, Pim-2, and Pim-3 kinases is emerging as a promising strategy for anticancer drug development. CX-6258 is a potent, selective, and orally efficacious pan-Pim kinases inhibitor.

In vitro: CX-6258 exhibited in vitro synergy with chemotherapeutics. The antiproliferative activity of CX-6258 was examined against a panel of cell lines derived from human solid tumors and hematological malignancies. CX-6258 demonstrated robust antiproliferative potencies against all cell lines tested [1].

In vivo: CX-6258 was evaluated in two human tumor xenograft growth efficacy models, acute myeloid leukemia MV-4-11, and prostate adenocarcinoma PC3. The drug exhibited dose dependent efficacy, with a 50 mg/kg dose producing 45% tumor growth inhibition (TGI) and a 100 mg/kg dose producing 75% TGI. In addition, CX-6258 displayed significant efficacy in vivo in two xenograft models representing the diseases where Pim kinases had been shown to play an important role [1].

Clinical trial: No clinical data are available

Reference:
[1] Haddach M, Michaux J, Schwaebe MK, et al.  Discovery of CX-6258. A Potent, Selective, and Orally Efficacious pan-Pim Kinases Inhibitor. ACS Med Chem Lett. 2011;3(2):135-9.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt461.94
Cas No.1202916-90-2
FormulaC26H24ClN3O3
SynonymsCX6258;CX 6258
Solubility≥11.15 mg/mL in DMSO, ≥2.575 mg/mL in H2O with gentle warming, <2.43 mg/mL in EtOH
Chemical Name(E)-5-chloro-3-((5-(3-(4-methyl-1,4-diazepane-1-carbonyl)phenyl)furan-2-yl)methylene)indolin-2-one
SDFDownload SDF
Canonical SMILESCN1CCCN(C(C2=CC(C3=CC=C(/C=C4C(C=C(Cl)C=C5)=C5NC\4=O)O3)=CC=C2)=O)CC1
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description CX-6258 HCl is a potent, orally efficacious inhibitor of pan-Pim kinase with IC50 of 5 nM, 25 nM and 16 nM for Pim1, Pim2, and Pim3, respectively.
Targets Pim1 Pim3 Pim2      
IC50 5 nM 16 nM 25 nM      

Quality Control

Chemical structure

CX-6258