Duocarmycin SA

Name: Duocarmycin SA
Brand: MedChemExpress
SKU: HY-12456
Rating: 4.5 (1 reviews)

Cat. No.: HY-12456 Purity: 99.55%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Duocarmycin SA is an orally active antitumor antibiotic with an IC₅₀ of 10 pM. Duocarmycin SA is an extremely potent cytotoxic agent capable of inducing a sequence-selective alkylation of duplex DNA. Duocarmycin SA demonstrates synergistic cytotoxicity against glioblastoma multiforme (GBM) cells treated with proton radiation in vitro.

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

Duocarmycin SA Chemical Structure

CAS No. : 130288-24-3

Size	Price	Stock	Quantity
1 mg	USD 840	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 2100	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 3700	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Antibiotic Isoform Specific Products:

View All Isoforms

Aminoglycoside Glycopeptide Lipopeptide Macrolide Oxazolidinone Quinolone Tetracycline β-lactam

View All ADC Cytotoxin Isoform Specific Products:

View All Isoforms

Auristatin Calicheamicins Camptothecins Daunorubicins/Doxorubicins Duocarmycins Maytansinoids Pyrrolobenzodiazepines Traditional Cytotoxic Agents

Biological Activity
Purity & Documentation
References
Customer Review

Description

Duocarmycin SA is an orally active antitumor antibiotic with an IC₅₀ of 10 pM^[1]. Duocarmycin SA is an extremely potent cytotoxic agent capable of inducing a sequence-selective alkylation of duplex DNA. Duocarmycin SA demonstrates synergistic cytotoxicity against glioblastoma multiforme (GBM) cells treated with proton radiation in vitro^[2].

IC₅₀ & Target

Duocarmycins

Cellular Effect

Cell Line	Type	Value	Description	References
L1210	IC₅₀	0.01 nM Compound: 1, natural	Cytotoxicity against mouse L1210 cells assessed as growth inhibition after 72 hrs by phosphatase assay Cytotoxicity against mouse L1210 cells assessed as growth inhibition after 72 hrs by phosphatase assay	[PMID: 23627265]
U138-MG	IC₅₀	0.0018 nM Compound: DSA	Anticlonogenic activity against human U138MG cells assessed as decrease in cell survival after 14 days by methylene blue staining based method Anticlonogenic activity against human U138MG cells assessed as decrease in cell survival after 14 days by methylene blue staining based method	[PMID: 29650288]
U138-MG	IC₅₀	0.4 nM Compound: DSA	Cytotoxicity against human U138MG cells assessed as decrease in cell viability after 72 hrs by trypan blue dye based assay Cytotoxicity against human U138MG cells assessed as decrease in cell viability after 72 hrs by trypan blue dye based assay	[PMID: 29650288]
U138-MG	IC₅₀	0.443 nM Compound: DSA	Anticlonogenic activity against human U138MG cells assessed as decrease in cell survival pretreated for 2 hrs followed by 1 to 8 Gy dose of proton irradiation measured after 10 to 14 days by methylene blue staining based method Anticlonogenic activity against human U138MG cells assessed as decrease in cell survival pretreated for 2 hrs followed by 1 to 8 Gy dose of proton irradiation measured after 10 to 14 days by methylene blue staining based method	[PMID: 29650288]

In Vitro

Duocarmycin SA (DSA) (0.1-1 nM; 72 hours) inhibits U-138 cell viability in a dose-dependent manner and activates apoptotic and necrotic pathways^[2].
Duocarmycin SA (0.1 nM; 72 hours) sensitizes human glioma cells to proton irradiation^[2].

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

Cell Viability Assay^[1]

Cell Line:	U-138 cells
Concentration:	0.1, 0.5, 1 nM
Incubation Time:	72 hours
Result:	Produced a significant concentration-dependent decrease in cell viability, with 65% cell survival observed at 0.1 nM, and plateauing at a minimum of 25% cell survival at 0.5 nM, with no increase in cytotoxicity observed at higher doses. The IC₅₀ of Duocarmycin SA for U-138 MG cells is 0.4 nM. Demonstrated strong cytotoxicity, with an IC₅₀ of 0.0018 nM (1.8 pM).

Apoptosis Analysis^[1]

Cell Line:	U-138 cells
Concentration:	0.001, 0.1 nM
Incubation Time:	3 or 14 days
Result:	Increased radio sensitivity of U-138 GBM cells by the activation of apoptotic and necrotic pathways. Greatly reduced survival fractions at different proton radiation doses (1-8 Gy).

In Vivo

Duocarmycin SA (0.143 mg/kg, i.p., single dose) shows antitumor activity in murine lymphocytic leukemia P388 transplanted in CDF₁ mice and shows a significant 30% increase in life span^[3].

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

Animal Model:	Murine lymphocytic leukemia P388 transplanted in CDF₁ mice ^[3]
Dosage:	0.143 mg/kg
Administration:	Intraperitoneal injection (i.p.), single dose
Result:	Showed a significant 30% increase in life span.

Molecular Weight

477.47

Formula

C₂₅H₂₃N₃O₇

CAS No.

130288-24-3

Appearance

Solid

Color

Off-white to light yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (104.72 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.0944 mL	10.4719 mL	20.9437 mL
5 mM	0.4189 mL	2.0944 mL	4.1887 mL
10 mM	0.2094 mL	1.0472 mL	2.0944 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (10.47 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 5 mg/mL (10.47 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.55%

Select Batch:

Data Sheet (276 KB) SDS (251 KB)

COA (252 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[1]. MacMillan KS, et al. Synthesis and evaluation of a thio analogue of duocarmycin SA. Bioorg Med Chem Lett. 2009 Dec 15;19(24):6962-5. [Content Brief]

[2]. Boyle KE, et.al. Duocarmycin SA, a potent antitumor antibiotic, sensitizes glioblastoma cells to proton radiation. Bioorg Med Chem Lett. 2018 Sep 1;28(16):2688-2692. [Content Brief]

[3]. Ichimura M,et.al. Duocarmycin SA, a new antitumor antibiotic from Streptomyces sp. J Antibiot (Tokyo). 1990 Aug;43(8):1037-8. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.0944 mL	10.4719 mL	20.9437 mL	52.3593 mL
	5 mM	0.4189 mL	2.0944 mL	4.1887 mL	10.4719 mL
	10 mM	0.2094 mL	1.0472 mL	2.0944 mL	5.2359 mL
	15 mM	0.1396 mL	0.6981 mL	1.3962 mL	3.4906 mL
	20 mM	0.1047 mL	0.5236 mL	1.0472 mL	2.6180 mL
	25 mM	0.0838 mL	0.4189 mL	0.8377 mL	2.0944 mL
	30 mM	0.0698 mL	0.3491 mL	0.6981 mL	1.7453 mL
	40 mM	0.0524 mL	0.2618 mL	0.5236 mL	1.3090 mL
	50 mM	0.0419 mL	0.2094 mL	0.4189 mL	1.0472 mL
	60 mM	0.0349 mL	0.1745 mL	0.3491 mL	0.8727 mL
	80 mM	0.0262 mL	0.1309 mL	0.2618 mL	0.6545 mL
	100 mM	0.0209 mL	0.1047 mL	0.2094 mL	0.5236 mL

Duocarmycin SA Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Duocarmycin SA130288-24-3AntibioticADC CytotoxinDNA Alkylator/CrosslinkerNecroptosisApoptosisADC PayloadDuocarmycinU-138 cellglioma cellsGBMantitumorantibioticlymphocytic leukemiaInhibitorinhibitorinhibit

Your Recently Viewed Products:

Product Name

Salutation

Applicant Name *

Email Address *

Phone Number *

Organization Name *

Department *

Requested quantity *

Country or Region *

Remarks

Product Name

Lot #

Applicant Name *

Email Address *

Phone Number

Department *

Organization Name *

Country or Region *

Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

Duocarmycin SA

Customer Review

Duocarmycin SA Related Antibodies

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Antibiotic Isoform Specific Products:

View All ADC Cytotoxin Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Duocarmycin SA Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Duocarmycin SA Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report