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Duocarmycin A

Duocarmycin A is an antitumor antibiotic and DNA alkylating agent with broad-spectrum antibacterial activity, and can be used as a payload for the synthesis of antibody-drug conjugates (ADCs). Duocarmycin A selectively binds to AT-rich DNA minor grooves and forms covalent adducts through alkylation of adenine N3 residues, thereby disrupting DNA structure and inhibiting its replication and transcription. Duocarmycin A induces apoptosis, sub-G1 phase accumulation, and chromatin condensation, reduces pro-caspase-3/9 levels, and induces p53-independent p21 expression. Duocarmycin A is widely used in research on various malignant tumors, including leukemia, sarcoma, glioblastoma, and various solid tumor models such as lung cancer, breast cancer, and colorectal cancer.

For research use only. We do not sell to patients.

CAS No.: 118292-34-5
Formula: C₂₆H₂₅N₃O₈
Molecular Weight:507.49

Storage:

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

Data Sheet (286 KB)

Duocarmycin A Chemical Structure

CAS No.: 118292-34-5

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Use of MCE Products

One-Stop Platform：From Independent R&D to Pilot-Scale Production

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[2]

Procaspase-3

Caspase-9

All ADC Payloads Isoforms :

All Antibiotic Isoforms :

All Caspase Isoforms :

All DNA/RNA Synthesis Isoforms :

In Vitro

ApoptosisCell Cycle RegulationOthers

Apoptosis

Duocarmycin A (0.003-0.03 μg/ml; 72 h) induces concentration-dependent apoptosis in HLC-2 cells, with 27% apoptosis at 0.003 μg/ml and 51% apoptosis at 0.03 μg/ml after 72 h of treatment, accompanied by characteristic apoptotic nuclear morphology^[3].
Duocarmycin A (0.003-0.03 μg/ml; 24-72 h) induces time- and concentration-dependent accumulation of apoptotic sub-G1 phase cells in HLC-2 cultures, with higher sub-G1 populations observed at 0.03 μg/ml compared to 0.003 μg/ml across 24, 48, and 72 h treatments^[3].

Apoptosis

Cell Cycle Regulation

Duocarmycin A (0.003-0.03 μg/mL) induces intrinsic pathway apoptosis and G₁ phase cell cycle arrest in HLC-2 cells in vitro in a dose-dependent manner, with altered expression of key apoptotic proteins (caspase-3, caspase-9, Bax) at 0.03 μg/mL^[2].

Others

Duocarmycin A (0.0016-0.0064 μg/ml; 0.032-42 μg/ml) potently inhibits the growth of Gram-positive bacterial strains (MIC 0.0016-0.0064 μg/ml) and exhibits variable inhibitory activity against Gram-negative bacterial and fungal strains (MIC 0.032-42 μg/ml)^[1].

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

Apoptosis Analysis^[2]

Cell Line:

human acute myeloid leukemia HL-60 (H2O2-sensitive) and HP100 (H2O2-resistant) cells
Concentration:

10 nM
Incubation Time:

30 min, 1 h, 2 h, 3 h, 4 h
Result:

Induced DNA fragments in both cell lines at 30 min. Triggered DNA ladder formation at 2 h in HL-60 cells and at 3-4 h in HP100 cells.
Reached maximal caspase-3 activity at 3 h in HL-60 cells and 4 h in HP100 cells; did not induce detectable caspase-1 activity in either cell line.

Cell Cycle Analysis^[3]

Cell Line:

human lung carcinoma (HLC-2) cells
Concentration:

0.003 μg/ml; 0.03 μg/ml
Incubation Time:

24 h; 48 h; 72 h
Result:

Resulted in sub-G1 phase (apoptotic) cell populations of 3.94% at 24 h, 12.37% at 48 h, and 6.86% at 72 h at 0.003 μg/ml. Resulted in sub-G1 phase cell populations of 5.56% at 24 h, 15.26% at 48 h, and 20.72% at 72 h at 0.03 μg/ml.

Western Blot Analysis^[3]

Cell Line:

human lung carcinoma (HLC-2) cells
Concentration:

0.003 μg/ml; 0.03 μg/ml
Incubation Time:

72 h (procaspase-3, procaspase-9, procaspase-8, Bax, Bcl-2); 24, 48, 72 h (p53, p21)
Result:

Decreased levels of the 32-kDa procaspase-3 and 47-kDa procaspase-9 precursors, and increased levels of pro-apoptotic Bcl-2 family protein Bax after 72 h of treatment; showed no change in procaspase-8 or Bcl-2 levels. Induced relatively high expression of p21, with extremely low accumulation of p53 across 24, 48, and 72 h of treatment.

In Vivo

Anti-cancer

Duocarmycin A (0.0075-0.04 mg/kg; i.p., i.v.; single dose) exhibits potent in vivo anti-tumor activity against murine sarcoma 180 in ddY mice; at a single intravenous (i.v.) dose of 0.03 mg/kg, its T/C ratio can be as low as 0.26^[1].
Duocarmycin-based B2M-ADC selectively targets senescent cancer cells and reduces their viability in in vivo models, with its activity exhibiting senescence phenotype specificity^[2].
Galactose-modified Duocarmycin can selectively induce cell death in senescent cancer cells in mice by targeting SA-β-gal activity^[2].

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

Animal Model:

ddY mice with Murine sarcoma 180^[1]
Dosage:

0.04 mg/kg (i.p.);
0.03 mg/kg (i.v.);
0.015 mg/kg (i.v.);
0.0075 mg/kg (i.v.)
Administration:

i.p. or i.v.; single dose
Result:

Achieved a T/C ratio of 0.35 at 0.04 mg/kg i.p. single dose.\nExhibited T/C ratios ranging from 0.26 to 0.42 at 0.03-0.0075 mg/kg i.v. single doses.

Related Protocols :

Chemical Information

CAS No. 118292-34-5
Molecular Weight 507.49
Formula C₂₆H₂₅N₃O₈
SMILES

O=C([C@@](N1)(C)C(C([C@@]23[C@@](C3)([H])CN(C(C(N4)=CC5=C4C(OC)=C(OC)C(OC)=C5)=O)C2=C6)=C1C6=O)=O)OC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (286 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. TAKAHASHI I, et al. Duocarmycin A, a new antitumor antibiotic from Streptomyces[J]. The Journal of antibiotics, 1988, 41(12): 1915-1917.

[2]. Morcos A, et al. A Comprehensive Review of the Antitumor Properties and Mechanistic Insights of Duocarmycin Analogs. Cancers (Basel). 2024;16(19):3293. Published 2024 Sep 27. [Content Brief]

[3]. Hirota M, et al. Distamycin A enhances the cytotoxicity of duocarmycin A and suppresses duocarmycin A-induced apoptosis in human lung carcinoma cells. Int J Biochem Cell Biol. 2007;39(5):988-996. [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.

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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Duocarmycin A

All ADC Payloads Isoforms

All Antibiotic Isoforms

All Caspase Isoforms

All DNA/RNA Synthesis Isoforms