DS-9300
Based on 1 Customer Validation
DS-9300 is a potent, orally active, selective EP300/CBP HAT inhibitor with an IC50 value of 28 nM. DS-9300 has anticancer activity and can be used in prostate cancer disease research.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 99.83%
- CAS No.: 2259641-46-6
- Formule: C25H26F3N5O3
- Masse moléculaire:501.50
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Stockage:Powder -20°C, 3 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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CWR22R | GI50 |
6.5 nM
Compound: 16; DS-9300
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Antiproliferative activity against AR-positive human 22Rv1 cells assessed as cell growth inhibition incubated for 7 days by CellTiter-Glo assay
Antiproliferative activity against AR-positive human 22Rv1 cells assessed as cell growth inhibition incubated for 7 days by CellTiter-Glo assay
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[PMID: 36572866] |
| LNCaP | GI50 |
3.4 nM
Compound: 16; DS-9300
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Antiproliferative activity against AR-positive human LNCaP cells assessed as cell growth inhibition incubated for 7 days by CellTiter-Glo assay
Antiproliferative activity against AR-positive human LNCaP cells assessed as cell growth inhibition incubated for 7 days by CellTiter-Glo assay
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[PMID: 36572866] |
| PC-3 | GI50 |
287.2 nM
Compound: 16; DS-9300
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Antiproliferative activity against AR-negative human PC-3 cells assessed as cell growth inhibition incubated for 7 days by CellTiter-Glo assay
Antiproliferative activity against AR-negative human PC-3 cells assessed as cell growth inhibition incubated for 7 days by CellTiter-Glo assay
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[PMID: 36572866] |
| VCaP | GI50 |
0.6 nM
Compound: 16; DS-9300
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Antiproliferative activity against AR-positive human VCaP cells assessed as cell growth inhibition incubated for 7 days by CellTiter-Glo assay
Antiproliferative activity against AR-positive human VCaP cells assessed as cell growth inhibition incubated for 7 days by CellTiter-Glo assay
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[PMID: 36572866] |
In Vitro
DS-9300 inhibits the growth of prostate cancer cell lines with the IC50 values of 0.6, 6.5, 3.4 and 287.2 nM for VCaP, 22Rv1, LNCaP and PC3 cells, respectively, indicating that it could effectively inhibit the growth of prostate cancer cell lines by inhibiting histone acetylation and down-regulating PSA expression[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
The pharmacokinetic parameters of DS-9300 in BALB/c mice
| PO(10 mg/kg) | IV(1 mg/kg) | ||||
| AUC, AUCu (μM*h) | Cmax (μM) | T1/2 (h)< | Vdss (L/kg) | CL, CLu (mL/min/kg) | F% |
| 130, 5.33 | 34 | 2.4 | 0.14 | 1.6, 39 | 62 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2259641-46-6
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Appearance Solid
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Masse moléculaire 501.50
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Formule C25H26F3N5O3
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Color White to off-white
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SMILES
COC1=CC=C(C=C1)C2(CCC(F)(CC2)F)C(N3C[C@@H](C[C@@H]3C(NC4=NC5=C(NN=C5)C=C4)=O)F)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (199.40 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, 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: ≥ 5 mg/mL (9.97 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (9.97 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
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.
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Pureté et documentation
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Fiche technique (276 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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Instruction de manipulation (2659 KB)
Références
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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9940 mL | 9.9701 mL | 19.9402 mL | 49.8504 mL |
| 5 mM | 0.3988 mL | 1.9940 mL | 3.9880 mL | 9.9701 mL | |
| 10 mM | 0.1994 mL | 0.9970 mL | 1.9940 mL | 4.9850 mL | |
| 15 mM | 0.1329 mL | 0.6647 mL | 1.3293 mL | 3.3234 mL | |
| 20 mM | 0.0997 mL | 0.4985 mL | 0.9970 mL | 2.4925 mL | |
| 25 mM | 0.0798 mL | 0.3988 mL | 0.7976 mL | 1.9940 mL | |
| 30 mM | 0.0665 mL | 0.3323 mL | 0.6647 mL | 1.6617 mL | |
| 40 mM | 0.0499 mL | 0.2493 mL | 0.4985 mL | 1.2463 mL | |
| 50 mM | 0.0399 mL | 0.1994 mL | 0.3988 mL | 0.9970 mL | |
| 60 mM | 0.0332 mL | 0.1662 mL | 0.3323 mL | 0.8308 mL | |
| 80 mM | 0.0249 mL | 0.1246 mL | 0.2493 mL | 0.6231 mL | |
| 100 mM | 0.0199 mL | 0.0997 mL | 0.1994 mL | 0.4985 mL |
DS-9300 Related Classifications
HY-152241 Related Classifications
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