Art. -Nr.: HY-178496

DDO3602

DDO3602 is a PARP1 HSPTAC (HSP90-mediated proteolysis-targeting chimera) degrader, with a DC₅₀ of 490.3 nM against PARP1; its K_d values for PARP1 and HSP90 are 66.5 nM and 1.64 nM, respectively. DDO3602 induces the formation of an unnatural PARP1-HSP90 ternary complex, recruits E3 ubiquitin ligase, and promotes PARP1 degradation via the ubiquitin-proteasome pathway. DDO3602 induces G2/M cell cycle arrest, DNA damage, inhibits cell migration, and exhibits antiproliferative activity in breast cancer cells. DDO3602 can be used in breast cancer-related research.
(Pink: PARP1 ligand (HY-75706); Blue: HSP90 ligand (HY-179203); Black: linker (HY-W015300)).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit : 96.42%
Formel: C₅₁H₅₈FN₇O₇
Molecular Weight:900.05

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

DDO3602 Chemical Structure

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Use of MCE Products

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

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

Biologische Aktivität

Beschreibung

DDO3602 is a PARP1 HSPTAC (HSP90-mediated proteolysis-targeting chimera) degrader, with a DC₅₀ of 490.3 nM against PARP1; its K_d values for PARP1 and HSP90 are 66.5 nM and 1.64 nM, respectively. DDO3602 induces the formation of an unnatural PARP1-HSP90 ternary complex, recruits E3 ubiquitin ligase, and promotes PARP1 degradation via the ubiquitin-proteasome pathway. DDO3602 induces G2/M cell cycle arrest, DNA damage, inhibits cell migration, and exhibits antiproliferative activity in breast cancer cells. DDO3602 can be used in breast cancer-related research^[1]. (Pink: PARP1 ligand (HY-75706); Blue: HSP90 ligand (HY-179203); Black: linker (HY-W015300)).

IC₅₀ & Target

^[1]

Hsp90TACs

PARP1

490.3 nM (DC₅₀)

Alle Hsp-targeting Chimeras Isoform-spezifische Produkte anzeigen :

Alle PARP Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
MCF7	DC₅₀	490.3 nM	PARP1 protein degradation in human MCF-7 breast cancer cells assessed via Western blot with GAPDH as loading control after 9 h incubation. PARP1 protein degradation in human MCF-7 breast cancer cells assessed via Western blot with GAPDH as loading control after 9 h incubation.	41004278
MCF7	IC₅₀	0.189 μM	Inhibition of cell viability in human MCF-7 breast cancer cells measured via CCK-8 assay after 72 h incubation. Inhibition of cell viability in human MCF-7 breast cancer cells measured via CCK-8 assay after 72 h incubation.	41004278
MCF-10A	IC₅₀	0.744 μM	Inhibition of cell viability in human MCF-10A normal breast epithelial cells measured via CCK-8 assay after 72 h incubation. Inhibition of cell viability in human MCF-10A normal breast epithelial cells measured via CCK-8 assay after 72 h incubation.	41004278

In Vitro

DDO3602 (0-3 μM; 9 h) degrades PARP1 in human breast cancer MCF-7 cells in a dose-dependent manner, with a DC₅₀ of 490.3 nM, and the degradation rate reaches 70.6% after incubation at 1 μM for 9 h^[1].
DDO3602 (1 μM; 0-24 h) induces significant degradation of PARP1 in human breast cancer MCF-7 cells within 3 h, with nearly complete depletion achieved by 9 h^[1].
DDO3602 (1 μM; 0-24 h) degrades the pre-existing PARP1 protein in MCF-7 human breast cancer cells, rather than inhibiting its synthesis^[1].
DDO3602 (0-1 μM) exerts a stronger inhibitory effect on colony formation in human breast cancer MCF-7 cells than in normal mammary epithelial MCF-10A cells^[1].
DDO3602 (0-10 μM; 72 h) inhibits the viability of MCF-7 human breast cancer cells with an IC₅₀ of 0.189 μM; its potency is approximately 4-fold higher than that against MCF-10A normal mammary epithelial cells (IC₅₀ = 0.744 μM) after 72 h of treatment^[1].
DDO3602 (0.5-1 μM; 24 h) induces dose-dependent G₂/M cell cycle arrest in human breast cancer MCF-7 cells^[1].
DDO3602 (1 μM; 24 h) induces significant DNA double-strand break formation in MCF-7 human breast cancer cells (detected by γ-H2A.X accumulation)^[1].
DDO3602 (0.1-1 μM; 48 h) significantly inhibits the migration of MCF-7 cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

MCF-7 human breast cancer cells
Concentration:

0, 0.1, 0.2, 0.3, 0.4, 0.6, 0.8, 1, 1.5, 2, 2.5 and 3 μM
Incubation Time:

9 h
Result:

Reduced PARP1 protein levels in a dose-dependent manner, achieving a degradation half-maximal effective concentration (DC₅₀) of 490.3 nM, and causing 70.6% PARP1 degradation at 1 μM.

Western Blot Analysis^[1]

Cell Line:

MCF-7 human breast cancer cells
Concentration:

1 μM
Incubation Time:

0, 3, 6, 9, 12 and 24 h
Result:

Significantly reduced PARP1 protein levels within 3 h, with near-complete depletion of PARP1 observed at 9 h.

Cell Cycle Analysis^[1]

Cell Line:

MCF-7 human breast cancer cells
Concentration:

0.5 and 1 μM
Incubation Time:

24 h
Result:

Induced G2/M phase cell cycle arrest in a dose-dependent manner; 0.5 μM increased the percentage of cells in G2/M phase to 59.0%, and 1 μM increased this percentage to 62.7%, compared to 24.9% in control cells.

Western Blot Analysis^[1]

Cell Line:

MCF-7 human breast cancer cells
Concentration:

1 μM
Incubation Time:

24 h
Result:

Induced a greater accumulation of γ-H2A.X than an equivalent concentration of Olaparib (HY-10162), indicating stronger induction of DNA damage.

Cell Migration Assay ^[1]

Cell Line:

MCF-7 human breast cancer cells
Concentration:

0.1 and 1 μM
Incubation Time:

48 h
Result:

Diminished wound healing capacity of MCF-7 cells more effectively than an equivalent concentration of Olaparib, indicating stronger inhibition of cell migration.

Parmacokinetics

Species	Dose	Route	C_max	AUC_0-t	T_1/2
Rat^[1]	10 mg/kg	i.p.	2370.00 ng/mL	16261.40 ng·h/mL	2.78 h

In Vivo

DDO3602 (10-20 mg/kg; i.p.; every other day; 21 days) potently inhibits MCF-7 xenograft tumor growth in immunocompromised mice^[1].
DDO3602 (20 mg/kg; i.v.; single dose) exhibits tumor-targeted pharmacokinetics in MCF-7 xenograft mice, with significantly higher accumulation in tumor tissue than normal tissues following a single 20 mg/kg intravenous dose^[1].

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

Animal Model:

Immunocompromised mice (MCF-7 xenograft model)^[1]
Dosage:

10 mg/kg; 20 mg/kg
Administration:

i.p.; every other day; 21 days
Result:

Suppressed tumor growth in a dose-dependent manner.
Achieved significant tumor regression at the 20 mg/kg dose.
Reduced mean tumor weights significantly compared to the control group at study endpoint.
Caused no significant body weight loss or organ toxicity via H&E staining of heart, liver, spleen, lung, and kidney tissues.

Animal Model:

Immunocompromised mice (MCF-7 xenograft model)^[1]
Dosage:

20 mg/kg
Administration:

i.v.; single dose
Result:

Reached a concentration in tumor tissue 13-fold higher than in spleen and over 33-fold higher than in liver, kidney, lung, heart, plasma, muscle, and intestinal tissues at 12 h post-dose.
Maintained significantly higher concentrations in tumor tissue than all other tissues at 24 h post-dose.

Related Protocols :

Chemical Information

Appearance Solid
Molecular Weight 900.05
Formel C₅₁H₅₈FN₇O₇
SMILES

CC(C1=C(C=C(C(C(N2CC3=C(C2)C=CC(CN4CCN(CC4)C(CCCCCCC(N5CCN(C(C6=CC(CC7=NNC(C8=CC=CC=C87)=O)=CC=C6F)=O)CC5)=O)=O)=C3)=O)=C1)O)O)C
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (111.10 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

1.1110 mL

5.5552 mL

11.1105 mL

5 mM

0.2222 mL

1.1110 mL

2.2221 mL

10 mM

0.1111 mL

0.5555 mL

1.1110 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. 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 (2.78 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 (2.78 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 (283 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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]. Liu W, et al. HSP90 Mediates Targeted Degradation of Nonclient Protein PARP1 for Breast Cancer Treatment. Journal of medicinal chemistry. 2025 Oct 09;68(19):19933-19954. [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

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.1110 mL	5.5552 mL	11.1105 mL	27.7762 mL
	5 mM	0.2222 mL	1.1110 mL	2.2221 mL	5.5552 mL
	10 mM	0.1111 mL	0.5555 mL	1.1110 mL	2.7776 mL
	15 mM	0.0741 mL	0.3703 mL	0.7407 mL	1.8517 mL
	20 mM	0.0556 mL	0.2778 mL	0.5555 mL	1.3888 mL
	25 mM	0.0444 mL	0.2222 mL	0.4444 mL	1.1110 mL
	30 mM	0.0370 mL	0.1852 mL	0.3703 mL	0.9259 mL
	40 mM	0.0278 mL	0.1389 mL	0.2778 mL	0.6944 mL
	50 mM	0.0222 mL	0.1111 mL	0.2222 mL	0.5555 mL
	60 mM	0.0185 mL	0.0926 mL	0.1852 mL	0.4629 mL
	80 mM	0.0139 mL	0.0694 mL	0.1389 mL	0.3472 mL
	100 mM	0.0111 mL	0.0556 mL	0.1111 mL	0.2778 mL

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DDO3602

Alle Hsp-targeting Chimeras Isoform-spezifische Produkte anzeigen

Alle PARP Isoform-spezifische Produkte anzeigen