YCH1899
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.39%
- No. CAS: 3032451-66-1
- Fòrmula: C25H18BrFN6O3
- Peso molecular:549.35
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Cell Cycle/DNA Damage Compound Library
HY-L004
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HY-L005
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HY-L034
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HY-L061
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HY-L077
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Anti-Drug-Resistant Compound Library
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High-Throughput Bioactive Compound Library
HY-L205
Actividad biológica
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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) |
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Cell Line
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Type | Value | Description | References |
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| CAPAN-1 | IC50 |
0.1 nM
Compound: 12; YCH1899
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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
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[PMID: 37605459] |
| CAPAN-1 | IC50 |
0.89 nM
Compound: 12; YCH1899
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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
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[PMID: 37605459] |
| CAPAN-1 | IC50 |
1.13 nM
Compound: 12; YCH1899
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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
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[PMID: 37605459] |
| HCC1937 | IC50 |
4.54 nM
Compound: 12; YCH1899
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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
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[PMID: 37605459] |
| HCT-15 | IC50 |
44.24 nM
Compound: 12; YCH1899
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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
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[PMID: 37605459] |
| IMR-90 | IC50 |
1.24 μM
Compound: 12; YCH1899
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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
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[PMID: 37605459] |
| MDA-MB-436 | IC50 |
0.52 nM
Compound: 12; YCH1899
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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
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[PMID: 37605459] |
| U-251 | IC50 |
1.97 nM
Compound: 12; YCH1899
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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
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[PMID: 37605459] |
| U-251 | IC50 |
1.97 nM
Compound: 12; YCH1899
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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
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[PMID: 37605459] |
| V79 | IC50 |
29.32 nM
Compound: 12; YCH1899
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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
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[PMID: 37605459] |
| WI-38 | IC50 |
0.53 μM
Compound: 12; YCH1899
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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
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[PMID: 37605459] |
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.
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Cell Line:HCC1937, HCT-15, MDA-MB-436, UWB1.289, UWB1.289+BRCA1, V–C8, V79 cells
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Concentration:0-1 μM approximately
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Incubation Time:24 h
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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.
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Cell Line:Capan-1, Capan-1/OP cells, Capan-1/TP cells
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Concentration:0.01, 0.1, 1 μM
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Incubation Time:24 h
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Result:Increased γH2AX level in a dose-dependent manner.
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Cell Line:Capan-1 and Capan-1/OP cells
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Concentration:1, 10, 100 nM
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Incubation Time:4 h
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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.
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.
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Animal Model:MDA-MB-436/OP xenografts and Capan-1/R-in vivo xenografts mice[1]
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Dosage:12.5 and 25 mg/kg
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Administration:Oral administration
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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.
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Animal Model:rats[1]
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Dosage:5 mg/kg
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Administration:Intravenous injection
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Result:Had a moderate clearance rate (24.5 mL/min/kg) and half-life (3.25 h).
Chemical Information
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No. CAS 3032451-66-1
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Appearance Solid
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Peso molecular 549.35
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Fòrmula C25H18BrFN6O3
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Color White to off-white
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SMILES
O=C1NN=C(C2=CC=CC=C21)CC3=CC=C(C(C(N4CCN5C(C4)=NN=C5C6=CC=C(O6)Br)=O)=C3)F
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (281 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
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.
| 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 |
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