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Art. -Nr.: HY-181787

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DOT1L705

DOT1L705 is a PROTAC degrader that targets DOT1L. DOT1L705 recruits the VHL E3 ubiquitin ligase to induce proteasomal degradation of DOT1L. DOT1L705 reduces the viability of leukemia cells. DOT1L705 inhibits H3K79 methylation. DOT1L705 can be used in studies related to MLL-rearranged leukemia.
(Pink: DOT1L ligand (HY-135127); Blue: VHL E3 ligase ligand; Black: linker).

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CAS. Nr.: 3050756-34-5
Formel: C₆₁H₇₂ClF₃N₁₂O₁₃S₂
Molecular Weight:1337.88

Speicherung:

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

DOT1L705 Chemical Structure

CAS. Nr.: 3050756-34-5

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Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
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Biologische Aktivität

Beschreibung

DOT1L705 is a PROTAC degrader that targets DOT1L. DOT1L705 recruits the VHL E3 ubiquitin ligase to induce proteasomal degradation of DOT1L. DOT1L705 reduces the viability of leukemia cells. DOT1L705 inhibits H3K79 methylation. DOT1L705 can be used in studies related to MLL-rearranged leukemia^[1]. (Pink: DOT1L ligand (HY-135127); Blue: VHL E3 ligase ligand; Black: linker).

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen :

In Vitro

DOT1L705 (0.026-1 μM) inhibits H3K79 methylation, reduces viability of MLL-rearranged acute myeloid leukemia cell lines.
DOT1L808 (5-46.6 nM) inhibits H3K79 methylation, reduces viability of MLL-rearranged acute myeloid leukemia cell lines.

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

Western Blot Analysis^[1]

Cell Line:

MV-4-11
Concentration:

0-10 μM
Incubation Time:

6 h-96 h
Result:

Induced dose-dependent degradation of DOT1L in MV-4-11 cells with a DC₅₀ of 0.33 μM, achieving near-complete degradation within 4-6 hours (sustained for 96 hours).
Reduced H3K79me2 levels in MV-4-11 cells with an IC₅₀ of 0.026 μM, 13-fold more potent than its effect on DOT1L protein levels.

Cell Viability AssayWestern Blot AnalysisCell Proliferation AssayApoptosis AnalysisCell Cytotoxicity AssayCell Cycle AnalysisRT-PCRCell Autophagy AssayImmunofluorescenceCell Differentiation AssayCell Invasion AssayCell Migration Assay Real Time qPCRELISA Assay^[1]

Cell Line:

MLL-rearranged cell lines
Concentration:

0.01-100 μM
Incubation Time:

5 days
Result:

Selectively inhibited viability of MLL-rearranged cell lines (MV-4-11 IC₅₀ = 0.29 μM; EOL-1 IC₅₀ = 0.39 μM; Pfeiffer IC₅₀ = 0.80 μM) while showing minimal activity against non-MLL-rearranged lines (KG-1 IC₅₀ > 50 μM).

In Vivo

DOT1L705 (1-10 mg/kg; i.p.; BID) demonstrates in vivo efficacy in an MV-4-11 xenograft model with favorable pharmacokinetic properties^[1].

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

Animal Model:

C57 BL/6 female mice ( 7−8 week old)^[1]
Dosage:

1 mg/kg (pharmacokinetics); 10 mg/kg (in vivo efficacy)
Administration:

in vitro; i.p. (single dose, pharmacokinetics); i.p. (BID, in vivo efficacy)
Result:

Reduced tumor volumes by >50% relative to vehicle control in an MV-4-11 subcutaneous xenograft model at 10 mg/kg BID i.p., with no significant body weight loss.
Showed reduced H3K79me2 levels in tumor lysates from the MV-4-11 subcutaneous xenograft model, confirming on-target activity.

Chemical Information

CAS. Nr. 3050756-34-5
Molecular Weight 1337.88
Formel C₆₁H₇₂ClF₃N₁₂O₁₃S₂
SMILES

ClC1=C(N=CC=C1)[C@H](C2=C3OC(F)(OC3=CC=C2)F)NC4=C(C=C(C=C4)S(C)(=O)=O)NC5=NC(N6CCNCC6)=NC(OCCOCCOCCOCCOC7=CC(C8=C(N=CS8)C)=CC=C7CNC([C@@H]9C[C@H](CN9C([C@@H](NC(C%10(CC%10)F)=O)C(C)(C)C)=O)O)=O)=N5
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.

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100 mg

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Biologische Aktivität
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DOT1L705

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

DOT1L705 Related Classifications

HY-181787 Related Classifications