MS6105
Based on 1 Customer Validation
MS6105 is a PROTAC degrader targeting LDHA and LDHB, with DC50 values of 38 nM and 74 nM for degrading LDHA and LDHB in PANC-1 cells, respectively, and no hook effect is observed at high concentrations. MS6105 inhibits the proliferation of pancreatic cancer cells, and no obvious toxicity is observed after intraperitoneal administration in mice. MS6105 can be used for pancreatic cancer-related research.
(Pink: LDHA and LDHB ligand (HY-175562); Blue: VHL ligand (HY-125845); Black: linker (HY-128421)).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.2%
- No. CAS: 2891709-58-1
- Fòrmula: C65H81N9O9S3
- Peso molecular:1228.59
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Almacenamiento:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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LDHA 38 nM (DC50) |
LDHA 74 nM (DC50) |
MS6105 (compound 22) (10 nM-10 μM; 3 h-48 h) degrades LDHA and LDHB in PANC-1 cells in a concentration- and time-dependent manner, with a DC50 of 38 nM for LDHA degradation and 74 nM for LDHB degradation, and this degradation depends on the ubiquitin-proteasome system[1].
MS6105 (3 μM; 24 h) selectively downregulates the protein levels of LDHA and LDHB in PANC-1 cells, with most of the affected proteins involved in cellular metabolic processes[1].
MS6105 (0.1 μM-60 μM; 24 h-72 h) inhibits the proliferation of PANC-1, MiaPaCa2 and BxPC3 pancreatic cancer cells and degrades LDHA, with potency superior to that of its parent LDH inhibitor 5[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PANC-1 pancreatic cancer cells
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Concentration:10 nM, 30 nM, 100 nM, 300 nM, 1 μM, 3 μM and 10 μM
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Incubation Time:48 h
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Result:The compound potently degraded LDHA with a DC50 of 38 nM and a maximum degradation (Dmax) of 93%. It also degraded LDHB with a DC50 of 74 nM and a Dmax of 86%. No hook effect was observed at concentrations up to 10 μM.
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Cell Line:PANC-1 pancreatic cancer cells
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Concentration:1 μM
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Incubation Time:1, 3, 6, 12, 24, 36 and 48 h
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Result:LDHA and LDHB degradation was observed as early as 24 h, and the maximum degradation was reached at 48 h.
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Cell Line:PANC-1 pancreatic cancer cells
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Concentration:3 μM
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Incubation Time:24 h, post 2 h pretreatment with 20 μM Ac-VHL-Me, 1 μM MG132 (HY-13259), 1 μM MLN4924 (HY-70062)
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Result:The LDHA degradation induced by the degrader was partially rescued by pretreatment with the VHL ligand, a proteasome inhibitor, a neddylation inhibitor, or the parent LDH inhibitor.
| Species | Dose | Route | Cmax |
|---|---|---|---|
| Mice[1] | 5 mg/kg | i.p. | 1800 nM |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Swiss Albino (male)[1]
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Dosage:5 mg/kg
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Administration:i.p.; single dose
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Result:Achieved a peak plasma concentration of 1800 nM at 8 hours.
Maintained measurable exposure over 24 hours.
Showed no clinical signs of toxicity.
Chemical Information
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No. CAS 2891709-58-1
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Appearance Solid
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Peso molecular 1228.59
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Fòrmula C65H81N9O9S3
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Color White to off-white
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SMILES
CC1=C(SC=N1)C2=CC=C(C=C2)CNC([C@@H]3C[C@H](CN3C([C@H](C(C)(C)C)NC(CCCCCCCCCCCC(NCCCCC#CC4=CC=CC(C5=NN(C(CC6CC6)=C5CC7=CC=C(C=C7)S(N)(=O)=O)C8=NC(C(O)=O)=CS8)=C4)=O)=O)=O)O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Pureza y Documentación
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Ficha de datos (272 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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Instrucciones de manejo (2659 KB)
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MS6105 Related Classifications
HY-152261 Related Classifications
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