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Cat. No.: 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 ligand (HY-150802); Black: linker).

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

CAS No.: 3050756-34-5
화학식: C₆₁H₇₂ClF₃N₁₂O₁₃S₂
분자량:1337.88

보관:

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

DOT1L705 Chemical Structure

CAS No.: 3050756-34-5

Amount: USD 0.00

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Use of MCE Products

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

Biological Activity
- 제품 설명
- In Vitro
- In Vivo
Chemical Information
Protocol (1)
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

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 ligand (HY-150802); Black: linker).

All PROTACs Isoforms :

All Histone Methyltransferase Isoforms :

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. Further protocols information, click here.

Western Blot Analysis^[1]

View Protocol

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 Assay^[1]

View Protocol

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 No. 3050756-34-5
분자량 1337.88
화학식 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
선적

Room temperature in continental US; may vary elsewhere.
보관

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

Protocol

All Cell Biology

Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.

순도&문서

Handling Instructions (2659 KB)

References

[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

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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