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Art. -Nr.: HY-181789

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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).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₆₁H₇₂ClF₃N₁₄O₉S₂
Molecular Weight:1301.89

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

DOT1L808 Chemical Structure

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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^[1]. (Pink: DOT1L ligand (HY-181790); Blue: VHL ligand (HY-181791); Black: linker).

IC₅₀ & Target^[1]

VHL	DOT1L 5 nM (DC₅₀)

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen :

In Vivo

DOT1L808 (25 mg/kg; i.p.; twice daily; 5 days per week for 2 weeks) significantly inhibits tumor growth in the MV-4−11-Luc acute myeloid leukemia model of NSG mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

NSG mice (female, 6-8 weeks old, tail vein injection of 1.5 × 10⁶ MV-4−11-Luc cells)^[1]
Dosage:

25 mg/kg
Administration:

i.p.; twice daily; 2 weeks (5 days per week)
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

Molecular Weight 1301.89
Formel C₆₁H₇₂ClF₃N₁₄O₉S₂
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Quan S, et al. Development of DOT1L-Targeted Protein Degraders for Treating MLL-r Leukemia. J Med Chem. 2026;69(4):4439-4468. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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Amount: USD 0.00

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

Produktname:
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Menge:
MCE Japan Authorized Agent:

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DOT1L808

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

DOT1L808 Related Classifications

HY-181789 Related Classifications