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Merck

526529

PIM-Kinase Inhibitor X, CX-6258

The PIM-Kinase Inhibitor X, CX-6258 controls the biological activity of PIM-Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Synonym(s):

PIM-Kinase Inhibitor X, CX-6258, ( E)-5-Chloro-3-((5-(3-(4-methyl-1,4-diazepane-1-carbonyl)phenyl)furan-2-yl)methylene)indolin-2-one, HCl

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About This Item

Empirical Formula (Hill Notation):
C26H24ClN3O3 · xHCl
Molecular Weight:
461.94 (free base basis)
UNSPSC Code:
12352200
NACRES:
NA.28
Assay:
≥99% (HPLC)
Form:
powder
Quality level:
100
Storage condition:
OK to freeze, desiccated (hygroscopic), protect from light

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SMILES string

O=C(/C1=C/C2=CC=C(C3=CC=CC(C(N4CCCN(C)CC4)=O)=C3)O2)NC5=C1C=C(Cl)C=C5.[xHCl]

assay

≥99% (HPLC)

form

powder

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, desiccated (hygroscopic), protect from light

color

orange

solubility

DMSO: 25 mg/mL

shipped in

ambient

storage temp.

2-8°C

Quality Level

100

Related Categories

General description

An orally bioavailable oxindolo-furanyl compound that acts as a potent, reversible and ATP-competitive inhibitor of pan PIM-kinases (IC50 = 5, 25 and 16 nM for PIM-1, PIM-2 and PIM-3, respectively; Ki = 5 nM for PIM-1) with excellent selectivity over 107 kinases (IC80 >500 nM). Shown to arrest the proliferation of several human cancer cells (IC50 = 20 and 452 nM for MV-4-11 and PC3 cells) and block phosphorylation of Bad-Ser112, 4E-BP1-Ser65 and Thr37/46 with an IC50 of ~ 1.0 µM. Displays favorable pharmacokinetic profile and efficacy in mice, and suppresses tumor growth in MV-4-11 and PC3 xenograft murine model (50 mg/kg, p.o.). Further, potentiates doxorubicin (Cat. No. 324380 ) and paclitaxel (Cat. No. 580555 ) toxicity in PC3 cells.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
PIM Kimases
Reversible: yes
Secondary Target
Flt3
Target IC50: 5, 25 and 16 nM for PIM-1, PIM-2 and PIM-3

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 6 months at -70°C.

Other Notes

Haddach, M., et al. 2012. ACS Med. Chem. Lett.3, 135.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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