XP-524
Based on 1 Customer Validation
XP-524 is a potent BET and EP300 inhibitor. XP-524 shows great tumoricidal activity in vivo. XP-524 prevents KRAS-induced, neoplastic transformation in vivo and extends survival in two transgenic mouse models of aggressive PDAC. XP-524 also enhances the presentation of self-peptide and tumor recruitment of cytotoxic T lymphocytes. XP-524 has the potential for the research of pancreatic ductal adenocarcinoma (PDAC).
For research use only. We do not sell to patients.
- Purity: 98.02%
- CAS No.: 2344825-52-9
- Formula: C30H28N6O3S
- Molecular Weight:552.65
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Heterocyclic Compound Library
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Anti-Hematopathy Compound Library
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
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Bioactive Compound Library
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High-Throughput Bioactive Compound Library
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF7:CFR | IC50 |
0.9 nM
Compound: 27; XL-223
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Growth inhibition of fulvestrant-resistant human MCF7:CFR cells measured after 5 days by Hoechst 33342 dye based imaging analysis
Growth inhibition of fulvestrant-resistant human MCF7:CFR cells measured after 5 days by Hoechst 33342 dye based imaging analysis
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[PMID: 32453591] |
| MCF7:TAM1 | IC50 |
<10 nM
Compound: 27; XL-223
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Growth inhibition of tamoxifen-resistant human MCF7:TAM1 cells measured after 5 days by Hoechst 33342 dye based imaging analysis
Growth inhibition of tamoxifen-resistant human MCF7:TAM1 cells measured after 5 days by Hoechst 33342 dye based imaging analysis
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[PMID: 32453591] |
| T47D | IC50 |
<10 nM
Compound: 27; XL-223
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Growth inhibition of tamoxifen-sensitive human T47D cells measured after 5 days by Hoechst 33342 dye based imaging analysis
Growth inhibition of tamoxifen-sensitive human T47D cells measured after 5 days by Hoechst 33342 dye based imaging analysis
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[PMID: 32453591] |
XP-524 (5 mg/kg; i.p.; daily for 250 days) Cooperates with PD-1 inhibition to further extends survivalin KPC Mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:15 weeks KPC mice[1]
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Dosage:5 mg/kg
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Administration:I.p., daily for 150 days
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Result:Significantly delayed mortality in KPC mice, extending median survival from 43- to 108-d postenrollment and reduced ERK activation, with parallel reductions in cell prolif-eration and uniform increases in apoptosis.
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Animal Model:15 weeks KPC mice[1]
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Dosage:5 mg/kg
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Administration:I.p.; daily (200-μg dose of anti–PD-1 every other day) for 250 days
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Result:Increased in cell-mediated cytotoxicity andreduction in T cell exhaustion, the combination of XP-524 andanti–PD-1 enhanced expression of the surrogate marker of cyto-toxicity perforin-1 in tumor-infiltrating CD8+T cell.
Chemical Information
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CAS No. 2344825-52-9
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Appearance Solid
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Molecular Weight 552.65
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Formula C30H28N6O3S
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Color Light yellow to light brown
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SMILES
O=C1NC=CC2=C1N(C)C=C2C3=CC4=C(C=CN4C(C5=NC=CC=C5)(C)C6=NC=CC=C6)C(NS(=O)(CC)=O)=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 33.33 mg/mL (60.31 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)
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 (4.52 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (4.52 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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.
Purity & Documentation
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Data Sheet (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)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
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 | 1.8095 mL | 9.0473 mL | 18.0946 mL | 45.2366 mL |
| 5 mM | 0.3619 mL | 1.8095 mL | 3.6189 mL | 9.0473 mL | |
| 10 mM | 0.1809 mL | 0.9047 mL | 1.8095 mL | 4.5237 mL | |
| 15 mM | 0.1206 mL | 0.6032 mL | 1.2063 mL | 3.0158 mL | |
| 20 mM | 0.0905 mL | 0.4524 mL | 0.9047 mL | 2.2618 mL | |
| 25 mM | 0.0724 mL | 0.3619 mL | 0.7238 mL | 1.8095 mL | |
| 30 mM | 0.0603 mL | 0.3016 mL | 0.6032 mL | 1.5079 mL | |
| 40 mM | 0.0452 mL | 0.2262 mL | 0.4524 mL | 1.1309 mL | |
| 50 mM | 0.0362 mL | 0.1809 mL | 0.3619 mL | 0.9047 mL | |
| 60 mM | 0.0302 mL | 0.1508 mL | 0.3016 mL | 0.7539 mL |
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