PV-1019
Based on 3 publication(s) in Google Scholar
PV-1019 (NSC 744039) is a potent, selective Chk2 inhibitor with an IC50 value of 24 nM. PV-1019 inhibits the Topotecan (HY-13768)-induced Chk2 autophosphorylation. PV-1019 inhibits IR-induced apoptosis.
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- Purity : 98.66%
- CAS No.: 1093793-05-5
- 화학식: C18H17N7O3
- 분자량:379.37
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) PV-1019
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Biological Activity
제품 설명
IC50 & Target
[1]|
Chk2 24 nM (IC50) |
In Vitro
PV-1019 (NSC 744039; 0.1-100 μM; 48 h) has antiproliferative effect in human tumor cells[1].
PV-1019 inhibits Chk2 autophosphorylation and histone H1 phosphorylation with an IC50 value of 138 nM[1].
PV-1019 (1-50 μM; 1 h; OVCAR-5 cells) inhibits the Topotecan-induced Chk2 autophosphorylation with an IC50 value of 2.8 μM[1].
PV-1019 (1 μM; 16 h) abrogates IR-induced apoptosis in mouse thymocytes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human tumor cells
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Concentration:0.1-100 μM
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Incubation Time:48 hours
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Result:Inhibited cell growth in a dose-dependent manner.
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Cell Line:OVCAR-5 cells
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Concentration:1, 5, 10, and 25 μM
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Incubation Time:1 hours
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Result:Decreased the level of Chk2 autophosphorylation (Ser516) in a dose-dependent manner.
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Cell Line:mouse thymocytes
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Concentration:1 μM
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Incubation Time:16 hours
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Result:Decreased in the sub-G1 fraction (56%).
Chemical Information
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CAS No. 1093793-05-5
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Appearance Solid
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분자량 379.37
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화학식 C18H17N7O3
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Color Light yellow to yellow
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SMILES
O=C(C(N1)=CC2=C1C([N+]([O-])=O)=CC=C2)NC3=CC=C(/C(C)=N/NC(N)=N)C=C3
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Synonyms
NSC 744039
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
용액&용해도
In Vitro:
DMSO : 40 mg/mL (105.44 mM; ultrasonic and adjust pH to 3 with 1 M HCl; 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. 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. 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)
In Vivo:
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: ≥ 2.5 mg/mL (6.59 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
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.
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.
순도&문서
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Data Sheet (274 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
[1]. Jobson AG, et, al. Cellular inhibition of checkpoint kinase 2 (Chk2) and potentiation of camptothecins and radiation by the novel Chk2 inhibitor PV1019 [7-nitro-1H-indole-2-carboxylic acid {4-[1-(guanidinohydrazone)-ethyl]-phenyl}-amide]. J Pharmacol Exp Ther. 2009 Dec;331(3):816-26. [Content Brief]
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. 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 |
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| DMSO | 1 mM | 2.6359 mL | 13.1797 mL | 26.3595 mL | 65.8987 mL |
| 5 mM | 0.5272 mL | 2.6359 mL | 5.2719 mL | 13.1797 mL | |
| 10 mM | 0.2636 mL | 1.3180 mL | 2.6359 mL | 6.5899 mL | |
| 15 mM | 0.1757 mL | 0.8786 mL | 1.7573 mL | 4.3932 mL | |
| 20 mM | 0.1318 mL | 0.6590 mL | 1.3180 mL | 3.2949 mL | |
| 25 mM | 0.1054 mL | 0.5272 mL | 1.0544 mL | 2.6359 mL | |
| 30 mM | 0.0879 mL | 0.4393 mL | 0.8786 mL | 2.1966 mL | |
| 40 mM | 0.0659 mL | 0.3295 mL | 0.6590 mL | 1.6475 mL | |
| 50 mM | 0.0527 mL | 0.2636 mL | 0.5272 mL | 1.3180 mL | |
| 60 mM | 0.0439 mL | 0.2197 mL | 0.4393 mL | 1.0983 mL | |
| 80 mM | 0.0329 mL | 0.1647 mL | 0.3295 mL | 0.8237 mL | |
| 100 mM | 0.0264 mL | 0.1318 mL | 0.2636 mL | 0.6590 mL |
PV-1019 Related Classifications
HY-125203 Related Classifications
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