MU380
Based on 1 Customer Validation
MU380 is a potent and selective CHK1 inhibitor that induces apoptosis and has anticancer activity.
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- Pureté : 99.6%
- CAS No.: 2109805-78-7
- Formule: C15H15BrF3N7
- Masse moléculaire:430.23
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Activité biologique
Description
In Vitro
MU380 (100 nM, 24 h) potently inhibits CHK1 kinase and sensitizes lymphoid tumor cells to gemcitabine[1].
MU380 (400 nM, 24 h) can significantly affect the cell cycle profile and induce the death of dividing and non-dividing primary chronic lymphocytic leukemia lymphocytes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:MEC-1and MEC-2 cells
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Concentration:400 nM
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Incubation Time:24 h
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Result:Showed accumulation in S phase as well as reduction in G2/M phase, greatly reduced rate of DNA synthesis, and marked induction of apoptosis (PARP protein cleavage).
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Cell Line:Chronic lymphocytic leukemia cells
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Concentration:100 nM or 200 nM
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Incubation Time:24 h
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Result:Potently blocked CHK1 activation while enhancing ATR kinase signaling to CHK1 (pS317 and pS345), and resulted in decreased levels of total CDC25A and CDC25C, pY15 CDK1, cyclin B1 and cyclin E1.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD-scid IL2Rγnull mice[1]
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Dosage:20 mg/kg
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Administration:In 20% aqueous Kolliphor solution, every three days from day 14 to day 28
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Result:Significantly inhibit the growth of tumors and gradually reduce their volume, with an average reduction of about 61%.
Chemical Information
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CAS No. 2109805-78-7
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Appearance Solid
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Masse moléculaire 430.23
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Formule C15H15BrF3N7
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Color White to off-white
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SMILES
NC1=C(Br)C([C@H]2CNCCC2)=NC3=C(C4=CN(C(F)(F)F)N=C4)C=NN13
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Protocole
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Detection of Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
Pureté et documentation
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Fiche technique (274 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Instruction de manipulation (2659 KB)
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)