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Referencia número: 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).

Para uso exclusivo en investigación. No vendemos a pacientes.

Fòrmula: C₆₁H₇₂ClF₃N₁₄O₉S₂
Peso molecular:1301.89

Almacenamiento:

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

DOT1L808 Chemical Structure

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Use of MCE Products

Fluorescent Dye

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

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vivo
Chemical Information
Pureza y Documentación
Referencias
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Bioz

Actividad biológica

Descripciòn

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)

Ver todos los productos específicos de isoformas PROTACs :

Ver todos los productos específicos de isoformas Histone Methyltransferase :

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

Peso molecular 1301.89
Fòrmula 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
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

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

Pureza y Documentación

Instrucciones de manejo (2659 KB)

Referencias

[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]

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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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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vivo
Chemical Information
Pureza y Documentación
Referencias

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DOT1L808

Ver todos los productos específicos de isoformas PROTACs

Ver todos los productos específicos de isoformas Histone Methyltransferase

Actividad biológica

Chemical Information

Pureza y Documentación

Referencias

Calculators

Help & FAQs

DOT1L808 Related Classifications

HY-181789 Related Classifications