Art. -Nr.: HY-155993

YCH1899

Kundenbewertung

Based on 1 Customer Validation

YCH1899 is an orally active PARP inhibitor, with an IC₅₀< 0.001 nM for PARP1/2. YCH1899 exhibits distinct antiproliferation activity against Olaparib (HY-10162)-resistant and Talazoparib (HY-16106)-resistant Capan-1 cells (Capan-1/OP and Capan-1/TP cells) , with IC₅₀ values of 0.89 and 1.13 nM, respectively. YCH1899 has acceptable pharmacokinetic properties in rats.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.39%
CAS. Nr.: 3032451-66-1
Formel: C₂₅H₁₈BrFN₆O₃
Molecular Weight:549.35

Speicherung:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

YCH1899 Chemical Structure

CAS. Nr.: 3032451-66-1

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

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

IC₅₀ & Target

PARP-1

<0.001 nM (IC₅₀)

PARP-2

<0.001 nM (IC₅₀)

PARP3

1.1 nM (IC₅₀)

PARP4

1.0 nM (IC₅₀)

TNKS1

3.8 nM (EC₅₀)

TNKS2

12.4 nM (IC₅₀)

PARA6

9.5 nM (IC₅₀)

PARP-7

7.3 nM (IC₅₀)

ARTD10/PARP10

10.8 nM (IC₅₀)

PARA11

2.166 μM (IC₅₀)

human PARP12

14.1 nM (IC₅₀)

PARP14

35.914 μM (IC₅₀)

PARP15

51.623 nM (IC₅₀)

Alle PARP Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CAPAN-1	IC₅₀	0.1 nM Compound: 12; YCH1899	Antiproliferative activity against human CAPAN-1 cells assessed as cell proliferation inhibition incubated for 7 days by SRB assay Antiproliferative activity against human CAPAN-1 cells assessed as cell proliferation inhibition incubated for 7 days by SRB assay	[PMID: 37605459]
CAPAN-1	IC₅₀	0.89 nM Compound: 12; YCH1899	Antiproliferative activity against human Olaparib-resistant CAPAN-1 cells assessed as cell proliferation inhibition incubated for 7 days by SRB assay Antiproliferative activity against human Olaparib-resistant CAPAN-1 cells assessed as cell proliferation inhibition incubated for 7 days by SRB assay	[PMID: 37605459]
CAPAN-1	IC₅₀	1.13 nM Compound: 12; YCH1899	Antiproliferative activity against human Talazoparib-resistant CAPAN-1 cells assessed as cell proliferation inhibition incubated for 7 days by SRB assay Antiproliferative activity against human Talazoparib-resistant CAPAN-1 cells assessed as cell proliferation inhibition incubated for 7 days by SRB assay	[PMID: 37605459]
HCC1937	IC₅₀	4.54 nM Compound: 12; YCH1899	Antiproliferative activity against HR-deficient human HCC1937 cells harboring BRCA1 mutant assessed as cell proliferation inhibition incubated for 7 days by SRB assay Antiproliferative activity against HR-deficient human HCC1937 cells harboring BRCA1 mutant assessed as cell proliferation inhibition incubated for 7 days by SRB assay	[PMID: 37605459]
HCT-15	IC₅₀	44.24 nM Compound: 12; YCH1899	Antiproliferative activity against HR-deficient human HCT-15 cells harboring BRCA2 mutant assessed as cell proliferation inhibition incubated for 7 days by SRB assay Antiproliferative activity against HR-deficient human HCT-15 cells harboring BRCA2 mutant assessed as cell proliferation inhibition incubated for 7 days by SRB assay	[PMID: 37605459]
IMR-90	IC₅₀	1.24 μM Compound: 12; YCH1899	Antiproliferative activity against human IMR-90 cells assessed as cell proliferation inhibition incubated for 7 days by SRB assay Antiproliferative activity against human IMR-90 cells assessed as cell proliferation inhibition incubated for 7 days by SRB assay	[PMID: 37605459]
MDA-MB-436	IC₅₀	0.52 nM Compound: 12; YCH1899	Antiproliferative activity against HR-deficient human MDA-MB-436 cells harboring BRCA1 mutant assessed as cell proliferation inhibition incubated for 7 days by SRB assay Antiproliferative activity against HR-deficient human MDA-MB-436 cells harboring BRCA1 mutant assessed as cell proliferation inhibition incubated for 7 days by SRB assay	[PMID: 37605459]
U-251	IC₅₀	1.97 nM Compound: 12; YCH1899	Antiproliferative activity against human Olaparib-resistant U-251 cells assessed as cell proliferation inhibition incubated for 7 days by SRB assay Antiproliferative activity against human Olaparib-resistant U-251 cells assessed as cell proliferation inhibition incubated for 7 days by SRB assay	[PMID: 37605459]
U-251	IC₅₀	1.97 nM Compound: 12; YCH1899	Antiproliferative activity against human Talazoparib-resistant U-251 cells assessed as cell proliferation inhibition incubated for 7 days by SRB assay Antiproliferative activity against human Talazoparib-resistant U-251 cells assessed as cell proliferation inhibition incubated for 7 days by SRB assay	[PMID: 37605459]
V79	IC₅₀	29.32 nM Compound: 12; YCH1899	Antiproliferative activity against Chinese hamster V79 cells harboring wild type BRCA2 assessed as cell proliferation inhibition incubated for 7 days by SRB assay Antiproliferative activity against Chinese hamster V79 cells harboring wild type BRCA2 assessed as cell proliferation inhibition incubated for 7 days by SRB assay	[PMID: 37605459]
WI-38	IC₅₀	0.53 μM Compound: 12; YCH1899	Antiproliferative activity against human WI-38 cells assessed as cell proliferation inhibition incubated for 7 days by SRB assay Antiproliferative activity against human WI-38 cells assessed as cell proliferation inhibition incubated for 7 days by SRB assay	[PMID: 37605459]

In Vitro

YCH1899 (7 days) shows obvious anti-proliferation activity on Capan-1, Capan-1/OP and Capan-1/TP cells, with IC₅₀ of 0.10, 0.89 and 1.13 nM, respectively.^[1].
YCH1899 (0.001-1 μM, 4 h) stabilizes PARP1-DNA complexes and suppresses PARP formation^[1].
YCH1899 (3.5 h) inhibits the proliferation of BRCA mutant/wild-type cells (V-C8, V79, HCT-15, HCC1937) with IC₅₀s ranging from 1.19-44.24 nM^[1].
YCH1899 (1 μM, 24 h) causes a large increase in the number of γH2AX foci in Capan-1、Capan-1/OP、Capan-1/TP cells^[1].
YCH1899 (1 μM, 48 h) induces a dramatic decrease in HR (Homologous Recombination) repair activity in U2OS-DR-GFP cells^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

HCC1937, HCT-15, MDA-MB-436, UWB1.289, UWB1.289+BRCA1, V–C8, V79 cells
Concentration:

0-1 μM approximately
Incubation Time:

24 h
Result:

Inhibited the proliferation of BRCA-Deficient/Wild-Type Cells and IC₅₀s value were 4.54, 44.24, 0.52, 0.02, 0.34, 1.19, 29.32nM, respectively.

Immunofluorescence^[1]

Cell Line:

Capan-1, Capan-1/OP cells, Capan-1/TP cells
Concentration:

0.01, 0.1, 1 μM
Incubation Time:

24 h
Result:

Increased γH2AX level in a dose-dependent manner.

Western Blot Analysis^[1]

Cell Line:

Capan-1 and Capan-1/OP cells
Concentration:

1, 10, 100 nM
Incubation Time:

4 h
Result:

Improved stability of PARP1-DNA complexes and induced chromatin-bound PARP1 accumulation in the presence of MMS (methanesulfonate).
Inhibited PARP formation in the presence of 0.1% H₂O₂.

In Vivo

YCH1899 (5 mg/kg, intravenous injection ) has a moderate clearance rate in rats^[1].
YCH1899 overcomes acquired Talazoparib resistance and has a significant regression of tumor volume in MDA-MB-436/OP (6.25, 12.5, and 25 mg/kg, orally, once a day for 27 days) and Capan-1/R-in vivo xenografts (12.5 and 25 mg/kg, orally, once a day for 21 days ) ^[1].

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

Animal Model:

MDA-MB-436/OP xenografts and Capan-1/R-in vivo xenografts mice^[1]
Dosage:

12.5 and 25 mg/kg
Administration:

Oral administration
Result:

Inhibited MDA-MB-436/OP xenografts tumor growth with T/C of 36.74% and 15.29% at 12.5 and 25 mg/kg
Inhibited Capan-1/R xenografts tumor growth with T/C of 48.92% and 13.87% at 12.5 and 25 mg/kg.

Animal Model:

rats^[1]
Dosage:

5 mg/kg
Administration:

Intravenous injection
Result:

Had a moderate clearance rate (24.5 mL/min/kg) and half-life (3.25 h).

Chemical Information

CAS. Nr. 3032451-66-1
Appearance Solid
Molecular Weight 549.35
Formel C₂₅H₁₈BrFN₆O₃
Color White to off-white
SMILES

O=C1NN=C(C2=CC=CC=C21)CC3=CC=C(C(C(N4CCN5C(C4)=NN=C5C6=CC=C(O6)Br)=O)=C3)F
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 20 mg/mL (36.41 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

1.8203 mL

9.1017 mL

18.2033 mL

5 mM

0.3641 mL

1.8203 mL

3.6407 mL

10 mM

0.1820 mL

0.9102 mL

1.8203 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 (protect from light). 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 mg/mL (3.64 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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 mg/mL (3.64 mM); Clear solution

This protocol yields a clear solution of ≥ 2 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 (20.0 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 (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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]. Sun Y, et al. YCH1899, a Highly Effective Phthalazin-1(2H)-one Derivative That Overcomes Resistance to Prior PARP Inhibitors. J Med Chem. 2023 Aug 21. [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	1.8203 mL	9.1017 mL	18.2033 mL	45.5083 mL
	5 mM	0.3641 mL	1.8203 mL	3.6407 mL	9.1017 mL
	10 mM	0.1820 mL	0.9102 mL	1.8203 mL	4.5508 mL
	15 mM	0.1214 mL	0.6068 mL	1.2136 mL	3.0339 mL
	20 mM	0.0910 mL	0.4551 mL	0.9102 mL	2.2754 mL
	25 mM	0.0728 mL	0.3641 mL	0.7281 mL	1.8203 mL
	30 mM	0.0607 mL	0.3034 mL	0.6068 mL	1.5169 mL

Keywords

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

YCH1899

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Highly Selective Inhibitors Library

Anti-Drug-Resistant Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle PARP Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

YCH1899

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Highly Selective Inhibitors Library

Anti-Drug-Resistant Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle PARP Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

YCH1899 Related Classifications

HY-155993 Related Classifications