DOT1L808
DOT1L808 is a potent and highly selective DOT1L PROTAC degrader with a DC50 value of 5 nM. DOT1L808 can promote the ubiquitination and degradation of DOT1L. DOT1L808 exhibits antitumor activity in an orthotopic leukemia model.
(Pink: DOT1L ligand (HY-181790); Blue: VHL ligand (HY-181791); Black: linker).
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- Formule: C61H72ClF3N14O9S2
- Masse moléculaire:1301.89
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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VHL |
DOT1L 5 nM (DC50) |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NSG mice (female, 6-8 weeks old, tail vein injection of 1.5 × 106 MV-4−11-Luc cells)[1]
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Dosage:25 mg/kg
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Administration:i.p.; twice daily; 2 weeks (5 days per week)
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Result:Markedly reduced bioluminescent signal (total photon flux per second) relative to vehicle-treated mice, indicating significant inhibition of disseminated leukemia growth.
Showed no significant body weight changes compared to vehicle controls.
Chemical Information
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Masse moléculaire 1301.89
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Formule C61H72ClF3N14O9S2
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SMILES
CC1=C(SC=N1)C2=CC=C(C(OCCN3CCN(CC3)CCN4CCN(CC4)C5=NC=NC(NC6=C(C=CC(S(C)(=O)=O)=C6)N[C@H](C7=C(C=CC=N7)Cl)C8=C9OC(F)(OC9=CC=C8)F)=N5)=C2)CNC([C@@H]%10C[C@H](CN%10C([C@H](C(C)(C)C)NC(C%11(CC%11)F)=O)=O)O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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