526529 Sigma-AldrichPIM-Kinase Inhibitor X, CX-6258 - Calbiochem
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.
More>> 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. Less<<PIM-Kinase Inhibitor X, CX-6258 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.
Synonyms: (E)-5-Chloro-3-((5-(3-(4-methyl-1,4-diazepane-1-carbonyl)phenyl)furan-2-yl)methylene)indolin-2-one, HCl
Recommended Products
Overview
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Key Spec Table
| Empirical Formula |
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| C₂₆H₂₄ClN₃O₃•HCl |
Products
| Catalogue Number | Packaging | Qty/Pack | |
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| 526529-10MG | Glass bottle | 10 mg |
| Description | |
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| Overview | 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. |
| Catalogue Number | 526529 |
| Brand Family | Calbiochem® |
| Synonyms | (E)-5-Chloro-3-((5-(3-(4-methyl-1,4-diazepane-1-carbonyl)phenyl)furan-2-yl)methylene)indolin-2-one, HCl |
| References | |
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| References | Haddach, M., et al. 2012. ACS Med. Chem. Lett. 3, 135. |
| Product Information | |
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| Form | Orange powder |
| Hill Formula | C₂₆H₂₄ClN₃O₃•HCl |
| Hygroscopic | Hygroscopic |
| Reversible | Y |
| Structure formula Image | |
| Quality Level | MQ100 |
| Applications |
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| Biological Information | |
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| Primary Target | PIM Kimases |
| Primary Target IC<sub>50</sub> | 5, 25 and 16 nM for PIM-1, PIM-2 and PIM-3 |
| Secondary target | Flt3 |
| Purity | ≥99% by HPLC |
| Physicochemical Information | |
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| Cell permeable | Y |
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| Toxicological Information |
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| Safety Information according to GHS |
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| Safety Information |
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| Product Usage Statements |
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| Packaging Information | |
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| Packaged under inert gas | Packaged under inert gas |
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| Specifications |
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| Global Trade Item Number | |
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| Catalogue Number | GTIN |
| 526529-10MG | 04055977270327 |
Documentation
PIM-Kinase Inhibitor X, CX-6258 - Calbiochem SDS
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PIM-Kinase Inhibitor X, CX-6258 - Calbiochem Certificates of Analysis
| Title | Lot Number |
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| 526529 |
References
| Reference overview |
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| Haddach, M., et al. 2012. ACS Med. Chem. Lett. 3, 135. |
| Data Sheet | ||||||||||||||||||||||||||
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Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
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