OPB-171775
Based on 1 Customer Validation
OPB-171775 is an orally active molecular glue. OPB-171775 forms ternary complex with phosphodiesterase 3A (PDE3A) and schlafen family member 12 (SLFN12). OPB-171775 causes SLFN12 RNase-mediated cell death, activates SLFN12 RNase-associated GCN2 signaling pathway. OPB-171775 exhibits significant efficacy against gastrointestinal stromal tumor.
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- Pureté : 99.80%
- CAS No.: 2131210-15-4
- Formule: C15H18F2N2O3
- Masse moléculaire:312.31
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Stockage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
In Vitro
OPB-171775 (0.01-100 nM) shows a delayed onset of cytotoxicity compared to Imatinib (HY-15463) and induces significant cell death in SLFN12-expressing GIST-T1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
OPB-171775 (0.03 mg/kg; p.o.; once daily; 21 days) combined Imatinib can lead to complete tumor regression in all mice bearing GS11353 PDX tumors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female C.B-17/Icr-scid/scidJcl mice with subcutaneous xenograft models derived from PFSK-1 cells[1]
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Dosage:0.003, 0.01, 0.03, 0.1, 0.3 mg/kg
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Administration:Orally administered once daily for 14 days
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Result:Inhibited tumor growth in a dose-dependent manner.
Had no significant adverse effects on animal body weight.
Chemical Information
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CAS No. 2131210-15-4
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Appearance Solid
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Masse moléculaire 312.31
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Formule C15H18F2N2O3
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Color White to off-white
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SMILES
FC1=C(C([C@H](C)C2)=NNC2=O)C=CC(OCC(O)(C)C)=C1F
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (320.19 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 (protect from light). 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Mammalian live/dead viability and cytotoxicity staining
Live/dead viability and cytotoxicity staining assays are based on the simultaneous detection of intracellular esterase activity in metabolically active (viable) cells and membrane integrity loss in non-viable cells. In commonly used dual-staining approaches, membrane-permeant fluorogenic substrates are converted by intracellular esterases into fluorescent products in live cells, while impermeant DNA-binding dyes selectively enter cells with compromised plasma membranes and label nucleic acids in dead or dying cells, enabling discrimination between viable and non-viable populations by fluorescence microscopy or flow cytometry.
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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 (271 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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Instruction de manipulation (2659 KB)
Références
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 (protect from light). 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 |
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| DMSO | 1 mM | 3.2019 mL | 16.0097 mL | 32.0195 mL | 80.0487 mL |
| 5 mM | 0.6404 mL | 3.2019 mL | 6.4039 mL | 16.0097 mL | |
| 10 mM | 0.3202 mL | 1.6010 mL | 3.2019 mL | 8.0049 mL | |
| 15 mM | 0.2135 mL | 1.0673 mL | 2.1346 mL | 5.3366 mL | |
| 20 mM | 0.1601 mL | 0.8005 mL | 1.6010 mL | 4.0024 mL | |
| 25 mM | 0.1281 mL | 0.6404 mL | 1.2808 mL | 3.2019 mL | |
| 30 mM | 0.1067 mL | 0.5337 mL | 1.0673 mL | 2.6683 mL | |
| 40 mM | 0.0800 mL | 0.4002 mL | 0.8005 mL | 2.0012 mL | |
| 50 mM | 0.0640 mL | 0.3202 mL | 0.6404 mL | 1.6010 mL | |
| 60 mM | 0.0534 mL | 0.2668 mL | 0.5337 mL | 1.3341 mL | |
| 80 mM | 0.0400 mL | 0.2001 mL | 0.4002 mL | 1.0006 mL | |
| 100 mM | 0.0320 mL | 0.1601 mL | 0.3202 mL | 0.8005 mL |
OPB-171775 Related Classifications
HY-162730 Related Classifications
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