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.

• Synonim(y): 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
• Wzór empiryczny (zapis Hilla): C₂₆H₂₄ClN₃O₃ · xHCl
• Masa cząsteczkowa: 461.94 (free base basis)
• Kod UNSPSC: 12352200
• NACRES: NA.28

Właściwości

• Poziom jakości: 100
• Próba: ≥99% (HPLC)
• Postać: powder
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; desiccated (hygroscopic); protect from light
• kolor: orange
• rozpuszczalność: DMSO: 25 mg/mL
• Warunki transportu: ambient
• temp. przechowywania: 2-8°C
• ciąg SMILES: O=C(/C1=C/C2=CC=C(C3=CC=CC(C(N4CCCN(C)CC4)=O)=C3)O2)NC5=C1C=C(Cl)C=C5.[xHCl]

Opis

Opis ogólny

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; K_i = 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 Thr^37/46 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.

Działania biochem./fizjol.

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

Opakowanie

Packaged under inert gas

Ostrzeżenie

Toxicity: Standard Handling (A)

Rekonstytucja

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

Inne uwagi

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

Informacje prawne

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

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Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 3
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable