Art. -Nr.: HY-12456

Duocarmycin SA

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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.

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Reinheit: 99.89%
CAS. Nr.: 130288-24-3
Formel: C₂₅H₂₃N₃O₇
Molecular Weight:477.47

Speicherung:

-20°C, stored under nitrogen

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

Duocarmycin SA Chemical Structure

CAS. Nr.: 130288-24-3

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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

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Cellular Effect

Cell Line	Type	Value	Description	References
L1210	IC₅₀	10 pM Compound: (+)-Duocarmycin SA	In vitro cytotoxicity against L1210 cell line In vitro cytotoxicity against L1210 cell line	[PMID: 10743956]
L1210	IC₅₀	10 pM Compound: 1	Cytotoxicity against mouse L1210 cells Cytotoxicity against mouse L1210 cells	[PMID: 19639994]
L1210	IC₅₀	10 pM Compound: (+)-1, (+)-duocarmycin SA	Cytotoxicity against mouse L1210 cells Cytotoxicity against mouse L1210 cells	[PMID: 19879753]
L1210	IC₅₀	10 pM Compound: (+)-1, (+)-duocarmycin SA	Cytotoxicity against mouse L1210 cells Cytotoxicity against mouse L1210 cells	[PMID: 20171886]
L1210	IC₅₀	6 pM Compound: 1	Cytotoxicity against mouse L1210 cells Cytotoxicity against mouse L1210 cells	[PMID: 20381346]
L1210	IC₅₀	0.01 nM Compound: 2, duocarmycin SA	Cytotoxicity against mouse L1210 cells Cytotoxicity against mouse L1210 cells	[PMID: 20942408]
L1210	IC₅₀	0.01 nM Compound: 1	Cytotoxicity against mouse L1210 cells Cytotoxicity against mouse L1210 cells	[PMID: 22650244]
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]
L1210	IC₅₀	10 pM Compound: (+)-1	Cytotoxicity against mouse L1210 cells assessed as cell growth inhibition Cytotoxicity against mouse L1210 cells assessed as cell growth inhibition	[PMID: 27221071]
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.

Chemical Information

CAS. Nr. 130288-24-3
Appearance Solid
Molecular Weight 477.47
Formel C₂₅H₂₃N₃O₇
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, stored under nitrogen

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

Lösungsmittel & Löslichkeit

In Vitro:

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

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

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)}

In Vivo:

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

Stock Solution Working Solution

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: ≥ 2.5 mg/mL (5.24 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.24 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (557 KB)
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- Korean - KR (557 KB)
- Portuguese - PT (557 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)

Verweise

[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]

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.

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

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Duocarmycin SA

Toxins for Antibody-Drug Conjugate Research Library

MCE Bioactive Compound Library

Alle Antibiotic Isoform-spezifische Produkte anzeigen

Alle ADC Payloads Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Duocarmycin SA

Toxins for Antibody-Drug Conjugate Research Library

MCE Bioactive Compound Library

Alle Antibiotic Isoform-spezifische Produkte anzeigen

Alle ADC Payloads Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Duocarmycin SA Related Classifications

HY-12456 Related Classifications