PD 407824
Based on 1 Customer Validation
PD 407824 is a checkpoint kinase Chk1 and WEE1 inhibitor with IC50s of 47 and 97 nM, respectively. PD 407824 is a chemical BMP sensitizer and increases the sensitivity of cells to sub-threshold amounts of BMP4.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.00%
- CAS No.: 622864-54-4
- 화학식: C20H12N2O3
- 분자량:328.32
-
보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
용액&용해도
- 순도&문서
- References
-
Help & FAQs
-
Cell Cycle/DNA Damage Compound Library
HY-L004
-
Immunology/Inflammation Compound Library
HY-L007
-
Kinase Inhibitor Library
HY-L009
-
Anti-Cancer Compound Library
HY-L025
-
Anti-Aging Compound Library
HY-L034
-
Anti-Pulmonary Fibrosis Compound Library
HY-L125
-
Osteogenesis Compound Library
HY-L131
-
Cancer Stem Cells Compound Library
HY-L135
-
Highly Selective Inhibitors Library
HY-L158
-
Serine/Threonine Kinase Inhibitor Library
HY-L164
-
Multi-Target Compound Library
HY-L176
-
Bioactive Compound Library Max
HY-L181
-
Anti-Aging Compound Library Mini
HY-L034M
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
Anti-Brain Cancer Compound Library
HY-L188
-
Protein Kinase Compound Library
HY-L196
-
High-Throughput Bioactive Compound Library
HY-L205
-
Posttranslational Modification Library
HY-L226
Biological Activity
|
Chk1 47 nM (IC50) |
WEE1 97 nM (IC50) |
PD 407824 is sufficient to block CHK1, leading to a significant down-regulation of p21, causing activation of CDK8/9, which in turn causes depletion of SMAD2/3[1].
PD 407824 is selective for Chk1 and WEE1 over PKC and Cdk4 with IC50s of 3.4 μM and 3.75 μM, respectively[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 622864-54-4
-
Appearance Solid
-
분자량 328.32
-
화학식 C20H12N2O3
-
Color Light yellow to yellow
-
SMILES
O=C1NC(C2=C1C3=C(C=C2C4=CC=CC=C4)NC5=C3C=C(O)C=C5)=O
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
용액&용해도
DMSO : 250 mg/mL (761.45 mM; Need ultrasonic; 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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: ≥ 2.08 mg/mL (6.34 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (6.34 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal 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
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
-
Data Sheet (278 KB)
-
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
-
Handling Instructions (2659 KB)
References
[1]. Palmer BD, et al. 4-Phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione inhibitors of the checkpoint kinase Wee1. Structure-activity relationships for chromophore modification and phenyl ring substitution. J Med Chem. 2006 Aug 10;49(16):4896-911. [Content Brief]
[2]. Feng L, et al. Discovery of a Small-Molecule BMP Sensitizer for Human Embryonic Stem Cell Differentiation. Cell Rep. 2016 May 31;15(9):2063-75. [Content Brief]
[3]. Smaill JB, et al. Synthesis and structure-activity relationships of N-6 substituted analogues of 9-hydroxy-4-phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-diones as inhibitors of Wee1 and Chk1 checkpointkinases. Eur J Med Chem. 2008 Jun;43(6):1276-96. Epub 2007 Aug 6. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.0458 mL | 15.2290 mL | 30.4581 mL | 76.1452 mL |
| 5 mM | 0.6092 mL | 3.0458 mL | 6.0916 mL | 15.2290 mL | |
| 10 mM | 0.3046 mL | 1.5229 mL | 3.0458 mL | 7.6145 mL | |
| 15 mM | 0.2031 mL | 1.0153 mL | 2.0305 mL | 5.0763 mL | |
| 20 mM | 0.1523 mL | 0.7615 mL | 1.5229 mL | 3.8073 mL | |
| 25 mM | 0.1218 mL | 0.6092 mL | 1.2183 mL | 3.0458 mL | |
| 30 mM | 0.1015 mL | 0.5076 mL | 1.0153 mL | 2.5382 mL | |
| 40 mM | 0.0761 mL | 0.3807 mL | 0.7615 mL | 1.9036 mL | |
| 50 mM | 0.0609 mL | 0.3046 mL | 0.6092 mL | 1.5229 mL | |
| 60 mM | 0.0508 mL | 0.2538 mL | 0.5076 mL | 1.2691 mL | |
| 80 mM | 0.0381 mL | 0.1904 mL | 0.3807 mL | 0.9518 mL | |
| 100 mM | 0.0305 mL | 0.1523 mL | 0.3046 mL | 0.7615 mL |
PD 407824 Related Classifications
HY-18961 Related Classifications
Powered by Bioz