530758 Sigma-AldrichBMX/BTK Inhibitor II, QL47 - CAS 1469988-75-7 - Calbiochem
A cell-permeable, highly potent, selective, irreversible inhibitor of BTK (IC₅₀ = 6.6 nM).
More>> A cell-permeable, highly potent, selective, irreversible inhibitor of BTK (IC₅₀ = 6.6 nM). Less<<SDB (Sicherheitsdatenblätter), Analysenzertifikate und Qualitätszertifikate, Dossiers, Broschüren und andere verfügbare Dokumente.
Synonyme: 1-(1-Acryloylindolin-6-yl)-9-(1-methyl-1H-pyrazol-4-yl)benzo[h][1,6]naphthyridin-2(1H)-one, BMX Inhibitor II, TEC Inhibitor II, Brutonʹs Tyrosine Kinase Inhibitor V, PI 3-K Inhibitor XXI, BTK Inhibitor V, BLK Inhibitor II
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Übersicht
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Key Spec Table
| CAS # | Empirical Formula |
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| 1469988-75-7 | C₂₇H₂₁N₅O₂ |
Preis & Verfügbarkeit
| Bestellnummer | Verfügbarkeit | Verpackung | St./Pkg. | Preis | Menge | |
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| 5.30758.0001 |
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Glasflasche | 5 mg |
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| Description | |
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| Overview | A cell-permeable tricyclic quinoline-acrylamide analog of BMX-IN-1 (Cat. No. 505021) that covalently modifies Cys481 in the kinase hinge region of Bruton's tyrosine kinase (BTK) and acts as a highly potent, selective, irreversible, and time-dependent inhibitor (IC50 = 6.6 nM). Also, inhibits the activity of bone marrow kinase on chromosome X (BMX) with equal potency (IC50 = 6.7 nM). Shown to be about 300-fold less potent against Cys496Ser mutated BTK. Displays excellent selectivity against a panel of 456 protein kinases, including JAK3, BLK, TEC, ITK, and EGFR and does not affect PI 3-K/mTOR and Raf/MEK/ERK signaling pathways. Diminishes autophosphorylation of BTK on Tyr223 in cells (EC50 = 475 nM) and promotes proteasome-mediated degradation of BTK (EC50 ~ 1 µM in HEK293T cells). Shown to induce cell cycle arrest at G1 phase and induce apoptotic cell death in Ramos cells. Also blocks the proliferation of several B-cell lymphoma cell lines (GI50 = 370, 200, 260,120, and 120 nM for Ramos, U2932, MM1S, RPMI8226, and BCWM.1, respectively). Please note that the molecular weight for this compound is batch-specific due to variable water content. |
| Catalogue Number | 530758 |
| Brand Family | Calbiochem® |
| Synonyms | 1-(1-Acryloylindolin-6-yl)-9-(1-methyl-1H-pyrazol-4-yl)benzo[h][1,6]naphthyridin-2(1H)-one, BMX Inhibitor II, TEC Inhibitor II, Brutonʹs Tyrosine Kinase Inhibitor V, PI 3-K Inhibitor XXI, BTK Inhibitor V, BLK Inhibitor II |
| References | |
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| References | Wu, H., et al. 2014. ACS Chem. Biol. 9, 1068. |
| Product Information | |
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| CAS number | 1469988-75-7 |
| Form | Yellow powder |
| Hill Formula | C₂₇H₂₁N₅O₂ |
| Chemical formula | C₂₇H₂₁N₅O₂ |
| Reversible | N |
| Quality Level | MQ100 |
| Applications |
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| Biological Information | |
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| Primary Target | BMX & BTK |
| Purity | ≥98% by HPLC |
| Physicochemical Information | |
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| Cell permeable | Y |
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| Toxicological Information |
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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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| Bestellnummer | GTIN |
| 5.30758.0001 | 04055977242966 |
Documentation
BMX/BTK Inhibitor II, QL47 - CAS 1469988-75-7 - Calbiochem SDB
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Literatur
| Übersicht |
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| Wu, H., et al. 2014. ACS Chem. Biol. 9, 1068. |
Broschüre
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| NPI Flyer- Epigenetics and Nuclear Function Feature |
| New Products - Antibodies, Small Molecule, Inhibitors |
Technische Informationen
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| White Paper: Further considerations of antibody validation and usage. |
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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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