Art. -Nr.: HY-181557

SY-589

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SY-589 is an orally active DNA polymerase Polθ helicase domain inhibitor (IC₅₀=2.29 nM) and DNA damage inducer. SY-589 inhibits the ATPase activity of the Polθ helicase domain and blocks the Polθ-mediated microhomology-mediated end joining (MMEJ) DNA repair pathway (IC₅₀=0.85 nM). SY-589 also induces the accumulation of DNA double-strand breaks by increasing γ-H2AX levels. SY-589 exerts antiproliferative effects on BRCA2-deficient cells and is used in the research of HR-deficient tumors.

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Reinheit: 98.50%
CAS. Nr.: 3077714-09-8
Formel: C₂₄H₁₈ClFN₈O₃S
Molecular Weight:552.97

Speicherung:

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

SY-589 Chemical Structure

CAS. Nr.: 3077714-09-8

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target

DNA Polymerase

Helicase

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen :

In Vitro

SY-589 (administered on days 0, 3, and 6) potently inhibits the viability of homologous recombination-deficient DLD1 BRCA2^-/- colon cancer cells, with an IC₅₀ of 2.71 nM^[1].
SY-589 (0.05-12.8 nM; 10 d) induces dose-dependent accumulation of DNA double-strand breaks (detected by γ-H2AX levels) in DLD1 BRCA2^-/- cells, and exerts dose-dependent effects on inhibiting colony formation, inducing cell cycle arrest and triggering apoptosis in DLD1 BRCA2^-/- cells^[1].
SY-589 (0.39-100 nM; 10 d) exerts strong synergistic effects with the PARP inhibitor Olaparib (HY-10162) to inhibit the viability of DLD1 BRCA2^-/- cells, and significantly enhances the antiproliferative activity of Olaparib^[1].

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

Western Blot Analysis^[1]

Cell Line:

DLD1 BRCA2^-/^- cells
Concentration:

0.05, 0.2, 0.8, 3.2, 12.8 nM
Incubation Time:

10 days
Result:

Induced a dose-dependent increase in γ-H2AX protein levels (a biomarker of DNA double-strand breaks), with the highest fold change observed at 12.8 nM.

Apoptosis Analysis^[1]

Cell Line:

DLD1 BRCA2^-/^- cells
Concentration:

0.05, 0.8, 12.8 nM
Incubation Time:

10 days (medium refreshed every 2 days)
Result:

Induced dose-dependent changes in cell cycle distribution, increasing the S-phase population from 18.12% (control) to 28.33% at 12.8 nM.
Induced apoptosis in a dose-dependent manner, with the apoptotic rate increasing from 9.13% (control) to 34.2% at 12.8 nM.

Cell Proliferation Assay^[1]

Cell Line:

DLD1 BRCA2^-/^- cells
Concentration:

0.05, 0.2, 0.8, 3.2, 12.8 nM
Incubation Time:

12 days (medium refreshed every 2 days)
Result:

Suppressed colony formation in a dose-dependent manner, with complete suppression observed at 12.8 nM.

Cell Proliferation Assay^[1]

Cell Line:

DLD1 BRCA2^-/^- cells
Concentration:

0.39, 1.56, 6.25, 25, 100 nM (SY-589); serially diluted (Olaparib)
Incubation Time:

10 days (dosed on day 0, day 3, day 6)
Result:

Exhibited strong synergistic antiproliferative activity with Olaparib, with a Loewe synergy score of >20.
Enhanced the antiproliferative effect of Olaparib, shifting from no suppression to >50% suppression of cell proliferation when paired with low-dose Olaparib (0.15 nM).

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	AUC_0-t	AUC_0-∞	MRT_0-t	MRT_0-∞	V_ss	CL	F
Mice^[1]	2 mg/kg	i.v.	1.38 h	0.08 h	6661.55 ng/mL	11178.99 ng·h/mL	11454.79 ng·h/mL	1.51 h	1.70 h	0.30 L/kg	2.95 mL/min/kg	/
Mice^[1]	30 mg/kg	p.o.	2.51 h	0.58 h	44547.59 ng/mL	185078.88 ng·h/mL	185274.47 ng·h/mL	4.00 h	4.02 h	/	/	107.83 %

In Vivo

SY-589 (0.5-30 mg/kg; p.o.; daily; 27 d) inhibits tumor growth in the DLD1BRCA2^-/- xenograft model; when combined with low-dose Olaparib (HY-10162), the tumor growth inhibition (TGI) rate reaches up to 109% with no significant toxicity^[1].

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

Animal Model:

BALB/c nude mice with Colorectal cancer (female, 6-8 weeks old)^[1]
Dosage:

30 mg/kg (monotherapy TGI); 0.5 mg/kg (combination 99% TGI); 2.5 mg/kg (combination 107% TGI); 12.5 mg/kg (combination 109% TGI)
Administration:

p.o.; daily; 27 days
Result:

Achieved 59% tumor growth inhibition (TGI) as monotherapy.
Achieved 99% TGI in combination with 25 mg/kg Olaparib.
Achieved 107% TGI with marked tumor regression in combination with 25 mg/kg Olaparib.
Achieved 109% TGI with marked tumor regression in combination with 25 mg/kg Olaparib.
Caused no significant body weight changes in any treatment group during the study.

Chemical Information

CAS. Nr. 3077714-09-8
Appearance Solid
Molecular Weight 552.97
Formel C₂₄H₁₈ClFN₈O₃S
Color White to off-white
SMILES

COC1=C(C=C(Cl)N=C1)C2=CC(N3C(C(F)=CC=C3)=O)=NC=C2C(NC4=NC(C5=C(C=NN5C)C)=NS4)=O
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 (180.84 mM; ultrasonic and warming and heat to 60°C; 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

1.8084 mL

9.0421 mL

18.0842 mL

5 mM

0.3617 mL

1.8084 mL

3.6168 mL

10 mM

0.1808 mL

0.9042 mL

1.8084 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 (4.52 mM); Suspended solution

This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.

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 (4.52 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 (281 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]. Ge C, et al. Discovery of SY-589, a Highly Potent and Orally Bioavailable Polθ Helicase Inhibitor for the Treatment of HR-Deficient Tumors. J Med Chem. 2026;69(3):2789-2813. [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	1.8084 mL	9.0421 mL	18.0842 mL	45.2104 mL
	5 mM	0.3617 mL	1.8084 mL	3.6168 mL	9.0421 mL
	10 mM	0.1808 mL	0.9042 mL	1.8084 mL	4.5210 mL
	15 mM	0.1206 mL	0.6028 mL	1.2056 mL	3.0140 mL
	20 mM	0.0904 mL	0.4521 mL	0.9042 mL	2.2605 mL
	25 mM	0.0723 mL	0.3617 mL	0.7234 mL	1.8084 mL
	30 mM	0.0603 mL	0.3014 mL	0.6028 mL	1.5070 mL
	40 mM	0.0452 mL	0.2261 mL	0.4521 mL	1.1303 mL
	50 mM	0.0362 mL	0.1808 mL	0.3617 mL	0.9042 mL
	60 mM	0.0301 mL	0.1507 mL	0.3014 mL	0.7535 mL
	80 mM	0.0226 mL	0.1130 mL	0.2261 mL	0.5651 mL
	100 mM	0.0181 mL	0.0904 mL	0.1808 mL	0.4521 mL

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SY-589

MCE Bioactive Compound Library

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SY-589 Related Classifications

HY-181557 Related Classifications