Murizatoclax
Based on 1 publication(s) in Google Scholar
Murizatoclax (AMG 397) is a potent, selective and orally active inhibitor of myeloid leukemia 1 (MCL-1) inhibitor, with a Ki of 15 pM. Murizatoclax competitive binds to the BH3-binding groove of MCL1 with pro-apoptotic BCL-2 family members. Murizatoclax can be used for the research of cancer.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 98.47%
- CAS. Nr.: 2245848-05-7
- Formel: C42H57ClN4O5S
- Molecular Weight:765.44
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Murizatoclax
More
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
MCL1 15 pM (Ki) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| AMO1 | EC50 |
13.5 nM
Compound: AMG 397
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Antiproliferative activity against human AMO1 cells assessed as reduction in cell viability
Antiproliferative activity against human AMO1 cells assessed as reduction in cell viability
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[PMID: 38597264] |
| MV4-11 | EC50 |
43.6 nM
Compound: AMG 397
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Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability
Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability
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[PMID: 38597264] |
| NCI-H929 | EC50 |
13 nM
Compound: AMG 397
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Antiproliferative activity against human NCI-H929 cells assessed as reduction in cell viability
Antiproliferative activity against human NCI-H929 cells assessed as reduction in cell viability
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[PMID: 38597264] |
| OPM-2 | IC50 |
70 nM
Compound: AMG397
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Anticancer activity against human OPM-2 cells assessed as inhibition of cell viability incubated for 24 hrs in presence of 10% FBS by Cell-titer Glo assay
Anticancer activity against human OPM-2 cells assessed as inhibition of cell viability incubated for 24 hrs in presence of 10% FBS by Cell-titer Glo assay
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[PMID: 33253879] |
In Vitro
AMG 397 potently disrupts the interaction between MCL1 and BIM in OPM2 cells, induces clear increases in Caspase-3/7 activity within one hour[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
Murizatoclax (10-60 mg/kg; p.o. twice weekly) achieves 47% MOLM-13 orthotopic tumor growth inhibition (TGI), 99% TGI and 75% regression at the dose of 10, 30 and 60 mg/kg, respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 2245848-05-7
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Appearance Solid
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Molecular Weight 765.44
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Formel C42H57ClN4O5S
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Color White to off-white
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SMILES
O=C(C(C=C1)=CC2=C1OC[C@]3(CCCC4=C3C=CC(Cl)=C4)CN2C[C@@]5([H])[C@](CC5)([H])[C@](CN6C[C@](CCCC7)([H])N7CC6)(OC)/C=C/C[C@H](C)[C@H]8C)NS8(=O)=O
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Synonyms
AMG 397
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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bioRxiv
2024 Nov 20:2024.10.24.620074. PMID: 39484513
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 10 mg/mL (13.06 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Protokoll
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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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
Reinheit & Dokumentation
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Data Sheet (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.3064 mL | 6.5322 mL | 13.0644 mL | 32.6610 mL |
| 5 mM | 0.2613 mL | 1.3064 mL | 2.6129 mL | 6.5322 mL | |
| 10 mM | 0.1306 mL | 0.6532 mL | 1.3064 mL | 3.2661 mL |
Murizatoclax Related Classifications
HY-109184 Related Classifications
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