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Art. -Nr.: HY-189005

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PARP1-IN-60

PARP1-IN-60 is an orally active PARP1 inhibitor with a human IC₅₀ of 2.4 nM. PARP1-IN-60 selectively inhibits PARP1-mediated poly (ADP-ribosylation) (PARylation) compared with PARP2. PARP1-IN-60 induces DNA damage, G2/M phase arrest and antiproliferative activity in BRCA-deficient cells. PARP1-IN-60 can be used in the research of BRCA-mutant cancers and colorectal cancer.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₂₅H₂₅FN₄O₃
Molecular Weight:448.49

Speicherung:

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

PARP1-IN-60 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
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

PARP1

2.4 nM (IC₅₀)

Alle PARP Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC50	2.35 nM	Inhibition of poly(ADP-ribosyl)ation (PARylation) in A549 wild-type cells treated with PARP1-IN-60, exposed to 10 mM H₂O₂ for 5 min to induce DNA damage, followed by a 1 h incubation. Inhibition of poly(ADP-ribosyl)ation (PARylation) in A549 wild-type cells treated with PARP1-IN-60, exposed to 10 mM H₂O₂ for 5 min to induce DNA damage, followed by a 1 h incubation.	42593943
MDA-MB-436	IC50	0.2 nM	Antiproliferative activity against BRCA-mutant MDA-MB-436 cells. Antiproliferative activity against BRCA-mutant MDA-MB-436 cells.	42593943
SUM149PT	IC50	2.82 nM	Antiproliferative activity against BRCA-mutant SUM149PT cells. Antiproliferative activity against BRCA-mutant SUM149PT cells.	42593943
CAPAN-1	IC50	832 nM	Antiproliferative activity against BRCA-wild-type CAPAN-1 cells. Antiproliferative activity against BRCA-wild-type CAPAN-1 cells.	42593943
MDA-MB-231	IC50	197 nM	Antiproliferative activity against BRCA-wild-type MDA-MB-231 cells. Antiproliferative activity against BRCA-wild-type MDA-MB-231 cells.	42593943
Vero	IC50	1845 nM	Antiproliferative activity against normal VERO cells. Antiproliferative activity against normal VERO cells.	42593943
H9c2	IC50	2647 nM	Antiproliferative activity against normal H9C2 cells. Antiproliferative activity against normal H9C2 cells.	42593943

In Vitro

PARP1-IN-60 ((R)-A17) potently inhibits PARP1 with an IC₅₀ of 2.4 nM, and exhibits 65.8-fold selectivity for PARP2 over PARP1 in enzymatic assays^[1].
PARP1-IN-60 exhibits high selectivity for PARP1, with extremely low inhibitory activity against PARP3, PARP5A, PARP5B, PARP6, PARP7, PARP12, PARP14 and PARP15^[1].
PARP1-IN-60 (1 h) selectively inhibits PARP1-mediated PARylation, with an IC₅₀ of 2.35 nM in A549 wild-type cells, an IC₅₀ of 1.22 nM in A549 PARP2-knockout cells, and no significant activity in A549 PARP1-knockout cells^[1].
PARP1-IN-60 exhibits excellent metabolic stability in human liver microsomes, with a half-life of over 120 min and an intrinsic clearance of <12 mL/min/g protein^[1].
PARP1-IN-60 (0.1-100 nM; 10 days) inhibits colony formation in a dose-dependent manner in BRCA-deficient MDA-MB-436 cells and DLD-1 BRCA2 knockout cells, but exerts no such effect on BRCA-proficient DLD-1 wild-type cells^[1].
PARP1-IN-60 selectively inhibits the proliferation of BRCA-deficient MDA-MB-436 and SUM149PT cells, with IC₅₀ values of 0.2 nM and 2.82 nM, respectively, while exhibits much weaker activity against BRCA wild-type cells and normal cells^[1].
PARP1-IN-60 (0.1-1000 nM; 72 h) induces dose-dependent DNA damage in MDA-MB-436 cells, which is evidenced by increased γ-H2AX foci and elevated protein expression^[1].
PARP1-IN-60 (1-100 nM; 72 h) induces dose-dependent G₂/M phase arrest in MDA-MB-436 cells^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

MDA-MB-436 (BRCA-deficient), DLD-1 wild-type, DLD-1 BRCA2-knockout
Concentration:

0.1-100 nM
Incubation Time:

10 days
Result:

Significantly suppressed colony formation in a dose-dependent manner in MDA-MB-436 and DLD-1 BRCA2-knockout cells.
Left DLD-1 wild-type cells largely unaffected even at 10 μM.

Cell Cycle Analysis^[1]

Cell Line:

MDA-MB-436
Concentration:

1-100 nM
Incubation Time:

72 h
Result:

Induced a dose-dependent decrease in S-phase cells.
Caused a corresponding accumulation of cells in G2/M phase.

Parmacokinetics

Species	Dose	Route	C_max	T_max	T_1/2	V_z	CL	AUC_0-t	F
Mice^[1]	1 mg/kg	i.v.	1342.55 μg/L	0.12 h	3.28 h	0.86 L/kg	0.18 L/h/kg	5500.51 μg/L·h	100 %
Mice^[1]	1 mg/kg	p.o.	962.65 μg/L	1.00 h	3.18 h	0.79 L/kg	0.17 L/h/kg	5681.56 μg/L·h	/

In Vivo

PARP1-IN-60 ((R)-A17) (0.3-3 mg/kg; p.o.; every other day) produces dose-dependent, well-tolerated antitumor efficacy in MDA-MB-436 xenograft mice, achieving a maximum tumor growth inhibition of 91.3% at 3 mg/kg^[1].
PARP1-IN-60 (1-3 mg/kg; p.o.; once daily) synergizes with liposomal irinotecan (Irinotecan liposome) (HY-185371) to produce dose-dependent enhanced antitumor efficacy in HCT116 xenograft mice, achieving a maximum tumor growth inhibition of 86.6% at 3 mg/kg combined with liposomal irinotecan^[1].
PARP1-IN-60 (30-300 mg/kg; p.o.; once daily; 14 days) is well-tolerated in healthy Balb/c mice with no observed adverse effects on body weight, blood counts, or serum chemistry^[1].
PARP1-IN-60 (500-1000 mg/kg; p.o.; single dose) is well-tolerated in healthy Balb/c mice with no observed mortality or adverse body weight effects^[1].

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

Animal Model:

NOD/SCID (female, 4-6 weeks old, 18-20 g, subcutaneous breast cancer xenograft model)^[1]
Dosage:

0.3 mg/kg; 1 mg/kg; 3 mg/kg
Administration:

p.o.; every other day
Result:

Achieved tumor growth inhibition (TGI) values of 57.8%, 86.3%, and 91.3% at doses of 0.3, 1, and 3 mg/kg, respectively.
Markedly reduced Ki67-positive tumor cell rate.
Caused no significant body weight loss across all doses.
Showed no apparent pathological abnormalities in major organs (heart, liver, spleen, lung, kidney) via hematoxylin and eosin (H&E) staining.

Animal Model:

Nu/Nu (female, 4-6 weeks old, subcutaneous colorectal cancer xenograft model)^[1]
Dosage:

1 mg/kg; 3 mg/kg (in combination with liposomal irinotecan 2 mg/kg)
Administration:

p.o.; once daily; liposomal irinotecan: i.v.; twice weekly
Result:

Achieved tumor growth inhibition (TGI) values of 77.2% at 1 mg/kg and 86.6% at 3 mg/kg when combined with liposomal irinotecan.
Caused no significant body weight changes, indicating good tolerability.

Animal Model:

Balb/c (female, subacute toxicity study)^[1]
Dosage:

30 mg/kg; 100 mg/kg; 300 mg/kg
Administration:

p.o.; once daily; 14 days
Result:

Caused no mortality or significant body weight loss in any treatment group.
Showed no significant decreases in complete blood count or serum biochemical parameters at doses of 100 and 300 mg/kg.

Animal Model:

Balb/c (acute toxicity study)^[1]
Dosage:

500 mg/kg; 1000 mg/kg
Administration:

p.o.; single dose
Result:

Caused no mortality or significant body weight changes over the 14-day observation period.

Chemical Information

Molecular Weight 448.49
Formel C₂₅H₂₅FN₄O₃
SMILES

FC1=CC=CC(C(CO[C@@H](CN2CCC(C3=CC=C(C(NC)=O)N=C3)=CC2)C4)=C4N5)=C1C5=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Guo Z, et al. Discovery, Synthesis, and Biological Evaluation of 1,3,4,5-Tetrahydro-6H-pyrano[4,3-c]isoquinolin-6-one Derivatives as Novel and Highly Selective PARP1 Inhibitors. Journal of medicinal chemistry. 2026 Aug 13;69(15):18051-18075.

Calculators

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)}

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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